Daily Telegraph - Medicines for Malaria Venture (MMV)



News Clippings of the Synthetic Peroxide (OZ) Story 18-23 August

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Financial Times (UK)

'BETTER, CHEAPER' MALARIA MEDICINE BEGINS HUMAN CLINICAL TRIALS

Geoff Dyer

Scientists will announce today the discovery of a new malaria medicine that could be more effective and considerably cheaper than the best drugs currently available.

In what could be one of the biggest recent breakthroughs in the treatment of malaria, which has been on the rise in much of sub-Saharan Africa for two decades, the drug has entered the first phase of clinical trials in humans.

Researchers in the US, Australia and Switzerland believe they have developed a synthetic version of the powerful artemisinin malaria therapies, which do not suffer from the resistance problems that other drugs face, but which are too expensive for most patients in developing countries.

Details of the discovery - a goal scientists have been working on for 15 years - will be published in today's edition of the science journal Nature.

"This new class [of drugs] could offer the best solution to date for destroying drug-resistant malaria," said Paul O'Neill at the University of Liverpool.

The drug is the flagship project of Medicines for Malaria Venture (MMV), one of a number of public-private partnerships that have been set up in recent years to foster research into medicines for the developing world, which will then be made available at low prices. The Geneva-based non-profit group backed the research and has a patent on the molecule.

It will also be a big test of the drug development expertise of Ranbaxy, the Indian company that is conducting the development work in partnership with MMV.

Artemisinin-based drugs, which are derived from a plant used for centuries in Chinese herbal medicine, have been available for a number of years to treat malaria. Unlike traditional malaria drugs such as the chloroquines, they have encountered no resistance among patients in sub-Saharan Africa.

However, because the raw material has to be derived from a plant, they are 10-20 times more expensive to make than the older drugs. Moreover, as the drugs are short-acting, patients need regular doses, which can lead to poor compliance.

The scientists behind the synthetic version of the artemisinin drugs come from the University of Nebraska in the US, Monash University in Australia, the Swiss Tropical Institute, and the Swiss drugs group Roche.

If the drug - currently known as OZ277 - makes it through clinical trials, it should be much cheaper to produce than the artemisinin derivatives. The scientists believe the compound is also more powerful than the existing medicines, which could mean patients would need fewer drugs.

Malaria causes 1m deaths a year and is the biggest killer of young children in sub-Saharan Africa. International health organisations estimate that 300m-500m treatments are needed each year for the disease. However, the artemisinin-based drugs are not widely used at the moment in Africa because of the cost.

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The Times (UK)

A sweet pill: A new anti-malarial drug promises more than a cure

In the sad task of getting to grips with a global Aids epidemic, the world’s second most deadly disease has been overshadowed. The World Health Organisation (WHO) estimates that 38 million people worldwide were living with HIV in 2003; almost three million were killed by Aids the same year. Malaria, in contrast, is reckoned to have caused the deaths of a million people last year. It is the number one killer of young children in sub-Saharan Africa, where a child dies of malaria every 30 seconds. As a result of the malaria parasite’s daunting ability to evolve to resist new drugs as they become widely used, the number of deaths from the disease in Africa is on the increase. And those who do not die may well be debilitated.

Yesterday’s announcement from the Medicines for Malaria Venture (MMV), an international public-private partnership aimed at developing and delivering new anti-malarial drugs, is at least some welcome news for that sorry region of the world. Scientists sponsored by MMV have developed a new drug, known as OZ, a synthetic compound which copies the molecular structure of the most effective existing anti-malarial medicine but which, because it is synthetic, will be much cheaper to produce. It is expected to cost less than a single dollar to cure an adult of malaria using OZ, putting the treatment within reach of poor countries in Africa, South America and Asia where malaria is endemic. Tests of the new drug’s efficacy will begin next year and scientists are optimistic about its potential.

OZ also represents a breakthrough of a broader kind: it proves the potential for public-private partnership, in pursuit of a common good, on a global scale. The drug was developed by MMV, a non-profit-making body, in partnership with an Indian pharmaceutical company Ranbaxy. Scientists from the University of Nebraska, Monash University in Australia, the Swiss Tropical Institute and F. Hoffman Roche worked together on the original research. Some two thirds of MMV’s funding comes from the US entrepreneur Bill Gates, via the Bill and Melinda Gates Foundation which has donated $65 million (£35million) over eight years. The UK’s Department for International Development gives £1 million a year. The Rockefeller Foundation, WHO, the World Bank and the Swiss, Dutch and US governments all contribute, as well as the Wellcome Trust, ExxonMobil and BHP-Billiton. The international pharmaceutical industry also participates. Profits from OZ, which are expected to be small, will be split between Ranbaxy and MMV, which will plough the money back into further research.

The dispute over treatments for Aids in the Third World has pitted non-governmental organisations, some worthy, some not, against Western goverments and pharmaceutical companies. The latter, particularly in the US, have been accused of conspiring to keep up the price of Aids drugs in the developing world. American politicians and pharmaceutical industry representatives protest that this conveniently overlooks the fact that research into the Aids-tackling drugs was carried out in the US, at the ultimate expense of American consumers who subsidised a multibillion-dollar project.

The excellent work of MMV has the potential, thankfully, to transform the territory. It proves that where the will, the funding and the right organisational skills exist, public and private, voluntary and philanthropic organisations can successfully be linked to tackle some of the world’s great challenges. It is not only the ravaged peoples of sub-Saharan Africa who should today be celebrating an apparent cure which could prove efficacious in unexpected ways.

Daily Telegraph (UK)

Chairman Mao's secret cure for malaria

By Roger Highfield

(Filed: 19/08/2004)

A synthetic version of a drug used for more than 1,500 years in Chinese medicine is hailed today as a breakthrough in efforts to reduce the million deaths caused each year by malaria.

Treatment based on the Chinese herbal remedy qinghaosu was developed during Chairman Mao's Cultural Revolution but tensions with the West delayed its spread.

Today, derivatives of artemisinin, a compound extracted from sweet wormwood, offer the most effective antimalarial therapy available. Malaria parasites have never evolved resistance to it.

Like all drugs, artemisinin-based drugs have drawbacks: relatively expensive extraction - the plant takes about 18 months to grow; treatment regimens can be too long for the Third World and, although it can quickly kill 96 per cent of the parasites, it has to be combined with longer acting variants to be completely effective.

Dr Jonathan Vennerstrom and colleagues say in the journal Nature they have made a fast-acting synthetic counterpart to artemisinin in which many of those problems have been overcome.

Dubbed OZ, the drug has entered clinical trials on 48 people in Britain. Initial studies suggest it is well-tolerated in healthy volunteers. This new class of drug is "a huge breakthrough," said Dr Paul O'Neill, of Liverpool University.

It is being developed by Ranbaxy Laboratories in India after various studies around the world. Because OZ is a synthetic drug, its costs can be significantly reduced as industrial production is easier.

The drug will be tried on malaria patients in January. The non-profit public private partnership driving drug development, Medicines for Malaria Venture, said yesterday it could become the most potent weapon against drug-resistant malaria, which affects 40 per cent of the global population.

Standard cheap malaria drugs are failing as much as 80 per cent of the time as malaria parasites become more resistant to older drugs, such as chloroquine. Standard cheap medicines are rendered useless in sub-Saharan Africa where every 30 seconds, a child dies of malaria.

Prof Andrew Read, of Edinburgh University, welcomed the advance but added: "There is always great optimism when a new 'wonder drug' comes along yet malaria parasites are extremely adept at evolving drug resistance."

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The Guardian (UK)

New drug boosts world fight against malaria

Treatment mimicking herbal remedy could be biggest breakthrough for a generation in combating disease that ravages Africa

Tim Radford, science editor

Thursday August 19, 2004

A new drug developed in India and based on a herb discovered in China could prove to be the biggest breakthrough in malaria treatment for a generation, scientists say today.

Malaria kills a child every 30 seconds in Africa. Worldwide, it kills more than a million people every year and 40% of the planet is always at risk. Malarial parasites have steadily become resistant to older treatments.

But researchers from the US, Switzerland, Australia and Britain report in Nature today on a synthetic drug that mimics a Chinese treatment called artemisinin, itself based on the herb sweet wormwood or Artemisia annua. Because the new drug is entirely factory made it could be cheaper, more consistent and produced more swiftly than any herbal extracts.

Safety tests on the drug, nicknamed OZ277, have begun in Britain. Tests for efficacy in malaria patients will begin in January.

The drug is produced by a partnership called Medicines for Malaria Venture. Although the research began in Europe and the US, the drug was developed by Ranbaxy Laboratories, a partner company in India.

The announcement was hailed by UK scientists as a major advance. Artemisia has been known as a herbal remedy for 1,500 years, but its value in malarial treatments was first observed about 30 years ago. Artemisinin, extracted from artemisia, is now in frequent use.

It works by killing the parasite - spread by a malarial mosquito - as it circulates through the human bloodstream. But its manufacture is both difficult and expensive.

"This is because the plant takes about 18 months to grow and then the drug needs to be extracted," said Brian Greenwood of the London School of Hygiene and Tropical Medicine.

"This new research has produced a drug very similar to that from plants, but without the time and expense of waiting for the plant to grow and extracting the compound. This should make the drug easier to produce and less expensive."

Sick people cannot work, and often cannot feed themselves. Malaria costs Africa an estimated£6-7bn in lost production, and accounts for two fifths of all public health spending in sub-Saharan Africa. Up to 500 million doses of medicine are needed every year.

ACT, based on artemisinin, is not widely used in Africa because it costs 20 to 30 times as much as the previous drugs. The discovery of a way to directly synthesise this family of compounds could cut production costs and therefore increase the availability of these drugs, and was a major step forward, said Robert Sinden, a parasite expert from Imperial College.

But all scientists sounded a note of caution. Malaria is a clever enemy, and difficult to outwit for long.

"There is always great optimism when a new 'wonder drug' comes along, yet malaria parasites are extremely adept at evolving drug resistance," said Andrew Read, a biologist at Edinburgh University.

"Let's hope the optimism is well placed this time, though history is not on our side.

"But a new drug that works even only in the medium term will save many, many lives and is to be greatly welcomed."

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The Independent (UK)

Ancient Chinese remedy may provide new treatment for malaria

By Steve Connor

19 August 2004

Scientists have created a new treatment for malaria which they believe will result in a cheap, mass-produced drug to fight the disease that kills a million people a year.

The researchers said that the drug was a synthetic version of the active ingredient found in a Chinese herbal remedy for malaria that has already proved an astounding success against the disease. The new synthetic drug will begin clinical trials within six months. Its synthesis in the laboratory will mean that it should be cheaper and more effective than its herbal equivalent, the scientists said.

An international research team made the drug, called trioxolane or "OZ", after studying the chemical constituents of artemisinin, a herbal remedy that has been used for 1,500 years.

Artemisinin is extracted from the sweet wormwood plant and, since the 1980s, has been used as the basis for making modern anti-malarial drugs such as artesunate and artemether. However, these are expensive to make and their effects are short term.

Paul O'Neill, a pharmacologist at Liverpool University, said: "These artemisinin derivatives are increasingly important in the treatment of drug-resistant malaria as they are the most potent anti-malarials available."

So far there have been no signs of malaria developing a resistance to artemisinin.

The Herald (Scotland)

Malaria: why make a killing?

[pic]

BETH PEARSON

August 20 2004

[pic]

IN the UK, it is often said there is a postcode lottery for receiving certain health services. In the 41 countries in which malaria is endemic, there isn't even a lottery: nearly everyone's a loser.

Malaria kills an estimated 2.5 million people a year, the majority of these African children aged below five years old. While western pharmaceutical companies have invested approximately £11bn over the past decade in "lifestyle drugs" for impotence, weight loss, baldness, smoking and ageing, the product development budget for the Tropical Disease Research (TDR) programme, a joint effort from the World Health Organisation (WHO), World Bank, and United Nations Development Programme (UNDP), averages £6m per year.

The victims of malaria and other neglected tropical diseases aren't living in the wrong area; they're just poor. It would be impossible for the drugs companies to make a profit in African and Asian countries where the average wage can be as little as £1 per day and, in Africa, economic growth is slowing by 1.3% per year as a direct result of malaria alone. As a result, research into tropical diseases by the pharmaceutical companies themselves is estimated to account for no more than 1% of their budget.

The new generation of malaria treatments, however, may circumvent the large pharmaceutical companies altogether and a new centre opening at Dundee University next year will be in the vanguard of such research.

The publication yesterday of a report detailing the development of a new malaria drug modelled on artemisinin, an extract from the Chinese sweet wormwood herb, demonstrates how scientists working in the field of tropical disease have been forced to innovate if they are to see their research become reality. The drug, known as OZ277 and developed by the Medicines for Malaria Venture (MMV), is a synthetic version of an existing treatment which can be made more cheaply and quickly than its mother drug. It has now entered human trials in the UK and will be tested for efficacy in malaria patients early next year.

From the very beginning, the pharmaceutical industry had little, if any, input in the drug's development. Dr Christopher Hentschel, chief executive of MMV, says that a number of pharmaceuticals were interested in the early stages of the project, which was funded by the TDR. "In terms of pharmaceutical industry interest, essentially there wasn't any because malaria isn't commercial," he says. "The idea has a history which involved a number of pharmaceuticals including Roche. They were interested and supported some of the work at an early stage but, basically, they just did it on the side with interested scientists."

When the project reached the stage of clinical development, it was decided that a pharmaceutical manufacturer should become involved. Rather than approach one of the major companies that were initially interested in the drug, however, the MMV team looked for a generic drugs manufacturer which could produce large quantities of the drug at a low cost. They began a partnership with Ranbaxy, the largest pharmaceutical company in India and one of the top 10 generic drugs companies worldwide, three years ago.

MMV's operation exemplifies how drugs for neglected diseases can be developed in the absence of major investment. It is a public-private partnership, which aims to make diseases like malaria more commercially-viable for private investors. This may involve emphasising the market for anti-malarials among western travellers, who are increasingly visiting destinations where malaria is a risk, offering tax credits, reducing research costs through grants or showing that there is considerable public support for a cause.

"The organisation was founded through discussion between the WHO and the representative body of the research-based pharmaceutical industry, the IFPMA (International Federation of Pharmaceutical Manufacturers' Associations), which is like a trade association," says Dr Hentschel. "They said they were willing to work on these kind of problems provided there was a public-private partnership involved in the management and helping fund the projects, because they obviously didn't want to be involved in funding all the projects themselves as they would never get any return on that funding.

"It's much better than what was before, which is almost nothing. Now the funding is shared between the public sector and the private sector. It's certainly a model which works and that's a significant advance on what we had before."

Well-funded research and development of anti-malarials is vital because malaria parasites constantly mutate and become resistant to treatments (Celtic player Bobo Balde, for one, missed Saturday's match thanks to malaria). The growing prevalence of the drug-resistant malarial strain P falciparum, is a particular concern to the WHO and the pressure to find new drugs combined with the lack of interest from pharmaceutical companies has increasingly frustrated scientists.

It's this frustration that has led one Scottish university to go it alone. When the £17.5m Centre for Inter-disciplinary Studies opens at Dundee University in July next year, it will circumvent the major pharmaceutical companies entirely, and therefore revolutionise the way drugs are developed. It is thought to be the only British university to adopt such an approach. Usually, profitable drug "leads" are picked up by pharmaceutical companies from the academic research stage, but this isn't the case with tropical diseases. It's something Mike Ferguson, professor of molecular parasitology, knows only too well. "Other areas of research are very often picked up by the pharmaceutical industry because they see a nice profitable market at the end of developing it through to a medicine you can sell to patients," he says.

"What goes wrong in tropical disease is the industry looks at the marketplace and sees there'd be no profitable market for it, therefore they don't do it. Rather than sitting and wringing our hands about the situation, we've decided to do something about it."

Once the Dundee team has taken the drug to this stage, they will present their work to the TDR, which will put it through the clinical trial phase. "In the normal drug development world, clinical trials are a very expensive and time-consuming component of drug development," says Professor Ferguson, whose department researches African sleeping sickness and Chagas's disease as well as malaria. "Clinical trials in a tropical disease context are somewhat less expensive, not because they're done to lower standards, but because they're being conducted in endemic tropical countries where salaries of doctors and nurses are lower, the logistical costs of carrying out these kind of tests are lower and you don't have to handle any marketing costs."

Without the huge burden of trial and marketing costs, public-sector academics can develop the research to the point that it can be picked up by the WHO. "That's what we're hoping to achieve. It's pretty revolutionary. I wouldn't say we're the only show in town worldwide, but the number of places taking this kind of approach is pretty small."

Like MMV, the drugs developed by Ferguson and his team would be manufactured at low-cost generic drug factories in Africa and Asia, not by big pharmaceutical companies.

It is expected the process will take 10 years from the point of developing drug to clinical trial standard and then from clinical trial phase to manufacturing.

Hentschel welcomes Dundee's approach: "The Dundee model is about getting early stage opportunities, and that's very important and very valuable. All I can do is wish it the best of luck. We need as many of these things as possible."

Ferguson envisages a cottage industry of small-scale pharmaceutical companies producing low-cost treatments for tropical diseases. Others, such as Philippe Kourilsky of the Pasteur Institute, imagine a "global, not-for-profit pharmaceutical industry". In the long term, Medicines Sans Frontieres have said the public need to take more responsibility for healthcare, with pharmaceutical industry moving out of private and into public sector.

For Hentschel, the motivation will be an ethical one but the solution a practical one. "There's a strong feeling among scientists that this ought to happen," he says. "The problem is to find an organisational methodology that will allow it to happen. The pharmaceutical industry itself will

not do it. The public sector, which is interested in it, cannot do it, because it doesn't have the resources and skills. Somehow you've got to get the two together."

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The Scotsman (Scotland)

Drug Breakthrough in Malaria Fight

By Louise Barnett, PA News

A new drug based on an ancient Chinese remedy could revolutionise treatment of malaria.

Clinical trials are under way in the UK to test how effectively it combats the increasingly drug-resistant malaria parasite.

The drug is a synthetic, simpler version of a traditional Chinese cure which could be around five times cheaper to produce than other treatments.

Malaria kills around one million people every year and causes a further 300 million to fall sick.

Drugs based on the Chinese remedy artemisinin have already been developed as a means of tackling chloroquine-resistant strains of the parasite.

Called RBx-11160, the new drug is a simpler, synthetic and slightly altered version of artemisinin, according to a report in Nature magazine published today.

Developed by the non-profit organisation Medicines for Malaria, the drug is soluble and can be given orally or injected intravenously.

In tests already carried out on infected mice, between 95% and 100% of parasites disappeared within four days following treatment with the new drug.

This compares with conventional artemisinin drugs which take a week to clear 95% of parasites.

The new drug entered clinical trials in Britain last month.

Malaria researcher Paul O’Neill, from Liverpool University, said: “This is potentially extremely important.”

Mr O’Neill said that, if the drug was found to be effective, it would probably be given to patients in combination with a second drug.

“The parasites find it more difficult to develop resistance when bombarded by two drugs targeting multiple pathways,” he said.

Malaria can be contracted by those who live in or visit around 100 countries across the tropics and subtropics, with about 40% of the world’s population at risk.

Some 90% of deaths from malaria happen in sub-Saharan Africa – mostly among young children. Malaria kills an African child every 30 seconds.

There are four main types of malaria, which are all spread by mosquitoes.

The main symptoms are high fever, chills, headache and sickness and the illness is often mistaken for flu.

RBx-11160 was produced in collaboration by three academic groups and three biotechnology firms, according to Nature magazine. [pic]

Nature News On-Line

Herbal medicine spawns antimalarial chemical

Helen Pilcher

Potent, cheap dose could tackle drug-resistant parasites.

After more than a decade of research, scientists believe they have come up with a fresh line of defence against the increasingly drug-resistant malaria parasite. Results suggest that the drug, which recently entered clinical trials in Britain, could revolutionize treatment of the disease.

Malaria claims around 1 million lives every year, and causes a further 300 million people to fall sick. In both Africa and Asia, the malaria parasite (Plasmodium falciparum) is becoming resistant to drugs such as chloroquine, which has been a staple of malaria treatment since the 1960s.

More recently, drugs based on the traditional Chinese remedy artemisinin have been developed. They are effective against chloroquine-resistant strains of parasite. But they can be expensive for developing nations and patients often find it difficult to stick to the weeklong course of treatment.

The new medicine, called RBx-11160, is a synthetic, slightly altered version of artemisinin. It only needs to be taken for around three days, and its simple structure means it should be at least five times cheaper to produce. Its development is reported in Nature this week1.

Yuanqing Tang from the University of Nebraska Medical Center, Omaha, helped to develop the drug and is excited by its prospects. "We hope RBx-11160 will prove useful for treating drug-resistant strains of the disease," he says.

Chemical warhead

Artemisinin-based drugs contain a hidden antimalarial warhead: a chemical bridge made of oxygen atoms. When the bridge is ruptured inside the parasite's gut, toxic free radicals are released and the microbe is destroyed.

Tang and colleagues have produced an altered version of the molecule that contains extra chemical groups to make the drug soluble in water and more stable.

Better solubility means the drug can be given orally or injected intravenously. Added stability means that less of the compound is broken down as it travels to the blood plasma, where the parasite lives.

The new version is also more potent. When infected mice are given the drug, 95-100% of parasites disappear within four days. Conventional artemisinin drugs take a week to clear 95% of parasites.

Trial runs

The drug entered preliminary human safety trials in Britain last month. "Initial results are promising," says Tang, but he cautions that it will be some time before the full data are available.

"This is potentially extremely important," says malaria researcher Paul O'Neill from Liverpool University, UK. If the drug works well in people, it would probably be given in combination with a second drug, which would kill any parasites missed by RBx-11160.

As well as curing patients, this strategy would minimize the development of drug-resistant strains. "The parasites find it more difficult to develop resistance when bombarded by two drugs targeting multiple pathways," says O'Neill.

The development of RBx-11160 is a flagship project for the Medicines for Malaria Venture, a non-profit organization that aims to encourage the development of affordable antimalarial drugs by bringing together academic researchers and private companies.

Three academic groups and three biotechnology firms collaborated to produce RBx-11160. "It is an excellent example of how a well managed partnership can have a significant impact on antimalarial product research and development," says O'Neill.

New Scientist

Synthetic drug offers malaria hope

 

18:00 18 August 04

 

news service

 

Clinical trials of a synthetic malaria drug have begun in the UK. The newly developed drug, which has similar properties to the naturally occurring substance artemisinin, could replace expensive plant extracts. Its developers hope it will help counter the resurgence in drug-resistant forms of the disease.

Artemisinin, a compound extracted from sweet wormwood (Artemisia annua), has been used for more than 1500 years in traditional Chinese medicine to treat fevers. Over the past few decades, combinations of artemisinin derivatives such as artesunate and artemether have proved highly effective against malaria.

But in the developing world, where malaria kills more than a million people each year, the natural extracts have serious drawbacks. They are costly to produce, and they quickly degrade, making them difficult to use. And the treatment usually fails if the patient fails to take the extract regularly.

Now, a synthetic drug, with apparently similar properties to artemisinin, has been produced by Jonathan Vennerstrom of the University of Nebraska Medical Center in Omaha, US, and his colleagues. It is cheap to make and is being developed by the pharmaceutical company Ranbaxy of New Delhi, India, and Malaria for Medicines Venture (MMV), a non-profit organisation based in Geneva, Switzerland. The drug is now being tested for safety in humans.

Trojan Horse

“We have tested different doses in more than a dozen healthy volunteers and results have been encouraging,” says Lise Riopel, scientific officer for MMV. Phase II field trials are scheduled for late next year.

The synthetic drug, like the natural product, kills malarial parasites by producing free radicals. It does this by reacting with iron, which is released as the parasite digests the haemoglobin of its human host.

“In some respects this drug can be regarded as a Trojan Horse,” says Paul O'Neill, an expert on synthetic anti-malarial drugs at the University of Liverpool in the UK. Free radicals seem to target several proteins and enzymes that are vital to the parasite's survival, Vennerstrom says.

Parasite proteins

Malaria has become much more common over the past 30 years, largely because the malarial parasite has developed resistance to many cheaper drugs such as chloroquine and quinine. But the parasites do not seem to develop resistance to any of the artemisinin family of compounds, probably because they attack several different parasite proteins. However, Brian Greenwood of the London School of Hygiene and Tropical Medicine says it is possible - though unlikely - that the parasite could build a resistance to the synthetic drug.

Laboratory tests suggest that the synthetic drug should remain active in the body for longer than the natural extracts. A three-day course should be sufficient to completely cure malaria, O'Neill says.

The MMV estimates that about 300 to 500 million malaria treatments are needed each year. “If human trials are successful, the new cheap synthetic drug could prove to be a breakthrough in the fight against malaria,” Riopel says.

Journal reference: Nature (vol 430, p 900)

 Amitabh Avasthi

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New York Times

India Company Develops New Malaria Drug

By THE ASSOCIATED PRESS

[pic]

Published: August 19, 2004

Filed at 1:11 a.m. ET

NEW DELHI (AP) -- India's Ranbaxy Laboratories said Wednesday it's developed a new anti-malarial drug, claiming it would cost less but work as well as drugs now used for the disease that kills more than a million people a year worldwide.

The drug, a synthetic peroxide developed with Geneva-based aid group Medicines for Malaria Venture, is now undergoing clinical trials in Britain, a Ranbaxy statement said.

``Our scientists are excited to be able to work on a drug that could save millions of lives,'' Ranbaxy Chief Executive Officer Brian Tempest said in the statement.

The statement said the new drug will work as well as artemisinin, a currently available anti-malaria drug, and will be much cheaper.

Artemisinin combination therapy costs about US$2 (euros 1.6) per dose, an amount beyond the reach of many in poor countries. Cheap medicines such as chloroquine no longer cure the disease in Africa because malaria parasites have become resistant to it.

Resistance is also spreading in India.

``We know about this synthetic peroxide developed by Ranbaxy. The reports that we have heard about it are certainly very promising,'' said Allan Schapira, coordinator of strategy and policy for the World Health Organization's ``Rollback Malaria'' campaign.

But knowledge about the drug is ``insufficient to make a judgment at the moment,'' Schapira said. ``We hope that it will prove highly efficacious.''

Findings from tests on the new drug are being published in the Aug. 19 issue of the science journal Nature.

Malaria, which is carried by mosquitoes, kills more than 1 million people a year, with 90 percent of the deaths occurring in Africa, according to the United Nations. Most of the victims are children under age 5.

Malaria also costs Africa an estimated US$12 billion (euros 9.73 billion) a year in lost gross domestic product and drains 40 percent of its public health spending.

``The need to develop a low-cost, potent, synthetic anti-malarial drug is more urgent than ever,'' said Christopher Hentschel, chief executive of Medicines for Malaria Venture. ``This could be the biggest breakthrough in malaria treatment of our generation.''

In May 2003, Ranbaxy Laboratories, India's largest pharmaceutical company, entered into an agreement with the Geneva-based body for laboratory testing, clinical trials and commercial development of the drug.

Omaha World Herald

UNMC team aids malaria fight

BY NICHOLE AKSAMIT AND KRISTIN ZAGURSKI

Scientists at the University of Nebraska Medical Center have helped discover a compound that may yield a less-costly treatment for malaria, an increasingly drug-resistant disease that still kills more than a million people worldwide each year.

The team developing the new drug includes scientists from the university's College of Pharmacy, Monash University in Australia, the Swiss Tropical Institute and the F. Hoffmann- LaRoche pharmaceutical company.

"It was really a far-flung group of collaborators," said Jonathan Vennerstrom, an associate professor of pharmaceutical sciences at the UNMC College of Pharmacy who led the research group.

Some preliminary data was generated beforehand, but work on the compound officially started in July 2000, Vennerstrom said. The group's objective was to develop an inexpensive, conveniently administered drug that can be used widely in sub-Saharan Africa.

"For a drug to treat malaria, cost is a very important issue," said Vennerstrom, who's also the lead author of an article about his group's work that appears in today's issue of the science journal Nature.

Their drug candidate, a synthetic peroxide developed with funding from the Geneva-based aid group Medicines for Malaria Venture, is in the earliest stage of clinical trials in Britain. The compound probably won't be tested on a large number of patients until 2006, Vennerstrom said.

India's largest pharmaceutical company, Ranbaxy Laboratories, is testing the compound and hopes to commercially produce it. Ranbaxy officials think the new drug will work as well as artemisinin, the most effective anti-malarial drug currently available, and will cost less.

Artemisinin combination therapy costs about $2 per dose, an amount beyond the reach of many sufferers in poor countries. Cheaper medicines such as chloroquine no longer cure the disease in Africa because parasites have become resistant. Drug resistance is spreading in India, too.

If the clinical trials are successful, the new and cheaper drug could become a major weapon against malaria.

While the final cost of producing the compound as a drug isn't known, Vennerstrom said, the chemistry is straightforward and could quickly be scaled up for large production.

Yuxiang Dong, a research associate at UNMC's College of Pharmacy and head chemist for the project, said in a statement that he developed the basic compound for the drug in 1999 but didn't think it would progress this far.

The development team produced the drug candidate by applying to malaria new chemistry developed at the lab in Germany where Dong earned his doctorate, Vennerstrom said.

The scientists in Nebraska communicated with their overseas counterparts through e-mails, monthly teleconferences and in-person meetings roughly every six months, he said.

Most cases of malaria in the United States occur in people that contracted the disease while traveling outside the country, Vennerstrom said.

Ninety percent of all malaria deaths occur in Africa, according to the United Nations. Most victims are children under 5.

Malaria costs Africa an estimated $12 billion a year in lost gross domestic product and drains 40 percent of its public health spending.

Voice of America

New Malaria Drug May Help Stem Disease's Growing Resistance

Jessica Berman

Washington

19 Aug 2004, 21:51 UTC

[pic][pic]Listen to Jessica Berman's report (RealAudio)

[pic]Berman report - Download 494k (RealAudio)

 

Malaria, which afflicts an estimated 40 percent of the world's population, is becoming more of a global problem. In an article in this week's journal Science, researchers report creeping resistance to drugs used to fight the disease from Asia to Africa, where malaria is the number one killer of young children. But help may be on the way. In another journal, Nature, scientists say they have developed what appears to be a cheap, effective synthetic drug to combat the mosquito-borne illness.

Malaria strikes 300 to 500 million people every year, and kills one million individuals, most of them children who die of the lethal fevers. Most of the victims live in sub-Saharan Africa, where the disease burden is greatest.

The main reason is that cheap, old-line drugs are now failing to kill the parasite in up to 90 percent of cases, as it mutates to evade the effect of the medicines.

That includes chloroquine and mefloquine, which have been used for years to treat malaria before the parasite became resistant to them. A newer anti-malarial drug, paramethynine, has met with widespread resistance throughout Asia.

As in Asia, researchers had assumed small treatment failures of paramethynine in Africa were confined to the continent, but a genetic analysis concludes otherwise. It appears resistant malaria parasites turning up in Africa had made their way to the sub-Saharan region from Asia. Callie Roper, a researcher with the London School of Hygiene and Tropical Medicine, says "it's showing that the resistance genes are highly mobile and that resistance is a global problem. It was thought previously that resistance to paramethynine had arisen quite a number of times in Africa itself, and now it appears that it didn't. A highly resistant form of the gene was actually introduced outside."

Dr. Roper and colleagues say some travel restrictions may be necessary. "To prevent the importation of resistant parasites from areas where resistance has arisen already," she says.

Dr. Roper adds new drugs are urgently needed to further contain the spread of drug resistant malaria.

Malaria drug researchers are universally pinning hopes on compounds derived from artemisinin, an ancient Chinese herb that has proven to be highly effective in treating malaria. The problem is the herb is expensive to process, putting it out of reach of many families and international aid organizations.

But researchers announced this week that they have developed what they're calling a synthetic artemisinin compound that would cost pennies to make.

Carl Craft is chief scientist of Medicines for Malaria Venture in Geneva, which has been developing the anti-malarial agent, which he says is not subject to the same environmental factors as artemisinin grown in the wild. "Well, for one thing you don't have to worry about planting thousands of [hectares] of plants and harvesting them. It can all be done in a chemical plant, where you don't have to worry about rains and floods and bad weather," he says.

Known as OZ, Dr. Craft says the drug has a similar mode-of-action as artemisinin

He says the new drug would be significantly cheaper than the artemisinin herb. "Which will be combined with another drug to make sure we don't get resistance. The amount of the cost of this drug for that combination would be about 20 cents compared to $1 or more for artemisinin compound. So, significantly better."

Medicines for Malaria Venture of India is conducting human safety trials in Britain. The company plans to test the drug's effectiveness beginning next January.

Radio Canada

Paludisme : percée scientifique porteuse d'espoir

| |

Mise à jour le jeudi 19 août 2004 à 11 h 18

Une équipe internationale a mis au point une molécule obtenue entièrement par synthèse et qui pourrait devenir une arme importante contre le paludisme, cette maladie qui tue un enfant africain toutes les 30 secondes.

Les premiers tests cliniques montrent que la nouvelle molécule OZ 277, inspirée d'un composant d'une plante chinoise, est bien tolérée par l'organisme.

Le médicament est actuellement développé par une organisation sans but lucratif dédiée à la recherche de nouvelles thérapeutiques antipaludisme peu coûteuses.

Cette percée scientifique pourrait devenir une arme majeure contre cette maladie qui touche 600 millions d'humains dans le monde et tue un enfant Africain toutes les 30 secondes.

Le paludisme (malaria) est une maladie parasitaire que l'on peut traiter, et pourtant, chaque année, plus de 1 million de personnes en meurent.

Les résultats complets sont publiés dans la revue Nature.

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The Age (Australia)

A marvel of modern medicine, and more

August 23, 2004

The process of delivering a cure for malaria to the world isn't just a matter of good science.

Victorians commonly associate the high-pitched, elusive whine of a mosquito with sleeplessness. For about 2.4 billion people elsewhere in the world, the sound is more than irritating. It can herald suffering and death. Each year, mosquitoes infect between 300 million and 900 million people with a malaria parasite that kills about 1.1 million of them. Malaria's toll exceeds the losses from all history's wars and plagues. In the past century, the plasmodium parasite that causes malaria has developed resistance to the most widely available drugs, leaving large populations at the mercy of the disease. Malaria debilitates survivors, slashing productivity in affected countries - GDP losses in Africa, the worst-afflicted continent, total $17 billion a year. In contrast, developed nations enjoy the benefits of less mosquito-friendly climates, pest control and expensive treatments. Unsurprisingly, pharmaceutical companies focus on profitable drugs for Western use, rather than cheap drugs for the Third World scourges of malaria and tuberculosis. The interaction of these diseases with AIDS, for which generic drugs only recently became available, compounds their devastating effect.

International research, which involves Monash University, has now produced a drug that might offer the world unprecedented protection. The news is a salutary reminder of the value of several factors in the development: philanthropy, global co-operation, science that considers the common good and ancient cultural knowledge. The project is backed by the non-profit Medicines for Malaria Venture, funded in part by Microsoft founder Bill Gates and BHP Billiton. Monash University professor Bill Charman said: "We set ourselves a target of a brand-new drug costing no more than one dollar a day, and that's a very steep hurdle ... We have been able to achieve that goal by designing a compound that, structurally, is quite simple to synthesise." The drug, dubbed OZ277, is derived from analysis of an ancient Chinese herbal medicine made from the wormwood plant, Artemesia annua. Although a generation of drugs that originated from Inca remedies has been rendered largely ineffective, malaria has not become resistant to natural extracts of artemisinin, but these are costly. With the new synthetic drug, though, a course of treatment could involve taking a $1 tablet a day for only three days.

The tragedy for a generation of victims is that China began productive research on this three decades ago (spurred by malaria's ravages during the Vietnam War). As this was associated with Mao's Cultural Revolution, political tensions delayed the spread of knowledge, but by the mid-1990s researchers understood how the compound worked. Development of OZ277 has progressed rapidly from animal trials to human trials and it could be released in three to four years. When that day comes, which we trust it will, Australian scientists can take pride in being part of a wonderful and noble achievement.

ABC TV (Australian Broadcast Corporation)

New drug shows promise in malaria fight

A new anti-malarial drug may be the biggest breakthrough in the treatment of the disease for a generation, the British scientific review Nature reports.

Codenamed OZ, the synthetic drug works in the same way as the most effective anti-malarial treatment, a Chinese herbal medicine called artemisinin.

Research on the drug was undertaken by a number of universities, including Melbourne's Monash.

Monash University professor Bill Charman says one of the main problems to overcome was drug resistance in the malaria parasite.

"The mechanism of action of this compound is such that we do not believe resistance will be a significant issue for these particular class of compound," Professor Charman said.

The research group, called Medicines for Malaria Venture (MMV), says the drug is a major development in the fight against the disease.

"The drug could be the biggest breakthrough in malarial treatment of our generation and could become the most potent weapon against drug-resistant malaria," the venture said.

"Initial clinical studies in humans have found the drug to be safe and well-tolerated. The synthetic drug could be a much cheaper and more effective alternative to the current malaria cures.

"Because OZ is a synthetic drug and does not require the natural plant, like artemisinin-based combination therapies (ACTs), its costs can be significantly reduced and the production of the drug can be easier and quicker to meet the demand," MMV says.

MMV describes itself as a non-profit organisation established to discover, develop and deliver new affordable anti-malarial drugs through effective public-private partnerships.

The new drug is currently being developed by MMV's industry partner, Ranbaxy Laboratories in India.

Drug resistance is a major problem for malaria, which occurs in more than 100 countries and territories.

The standard cheap medicines are rendered useless in almost every corner of sub-Saharan Africa, where every 30 seconds a child dies of malaria.

Malaria is a treatable disease but every year more than 1 million people die from it.

"OZ is currently being tested in humans in the UK for safety, tolerance and drug activity," MMV says.

"The test for its efficacy in malaria patients will begin in January 2005. If successful, it could be the next major weapon in the fight against malaria."

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Sydney Morning Herald

High hopes for new malaria drug

August 19, 2004 - 9:56AM

A team of international scientists, including from Australia, has created a synthetic drug which could offer new hope in the fight against malaria.

Nearly two billion people live in areas affected by malaria. The disease, transmitted by mosquitoes, is becoming a bigger threat as the parasite that causes it develops immunity to drugs used to fight it.

The new drug is based on a chemical found in traditional Chinese herbal medicine.

Scientists have long been interested in Artemisinin, a herbal fever remedy that comes from the bark of the sweet wormwood tree and has been shown to help kill malaria parasites.

But the naturally occurring drug is expensive to make and requires complicated treatment programs that are difficult to get patients to comply with.

An international team of scientists in Australia, the United States, Britain and Switzerland said in research published in the British science journal Nature they had developed a synthetic drug, OZ277, designed to offer the benefits of Artemisinin that could be cheaper to produce and more potent.

It will require tests before OZ277 can become a commercial drug. But in an accompanying article, Paul O'Neill of the Chemistry and Pharmacology departments of the University of Liverpool said the new class of compounds "could offer the best solution to date for destroying drug-resistant malaria parasites".

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The Age (Australia)

Chinese herb offers hope of malaria breakthrough

By Carol Nader

August 20, 2004

A simple course of three tablets could save the lives of millions of people afflicted with deadly malaria.

Chinese scientists found 20 years ago that a compound from a herb, sweet wormwood, could be effective in treating malaria.

But the compound is complex and expensive and scientists have been trying to find out what part of it could be used to form part of a new drug.

A team of international researchers, including Australians, believe they have worked out what that is. They are developing a synthetic version of the drug that will make it available cheaply for malaria victims, who typically live in poor countries - at $US1 ($A1.40) a tablet.

Bill Charman, professor of pharmaceutics at the Victorian College of Pharmacy at Monash University, said a synthetic version of the drug could be made on a large scale and victims would need to take just one tablet a day for three days.

Professor Charman said that the malaria parasite lived and grew in the red blood cells of infected people. "We have to get the drug to get into the red blood cell, into the parasite, and then kill it," he said.

Professor Charman, who was part of the research team, said one of the key criteria of the drug was making it cheap.

"A lot of the people that die from malaria are young children under five in Africa, so it's an enormous economic burden to Africa," he said. "It's an absolute scourge of a disease."

More than 1 million people die from malaria and there are up to 500 million cases each year. The malaria parasite is passed via mosquito bites. It is rife in sub-Saharan Africa and South-East Asia.

The drug, dubbed OZ277, could be available in three to four years. Clinical trials have started in Britain, and, next year, patients in Africa and Asia will be tested.

Trials in animals showed that those with the disease were cured. The findings were published in the journal Nature.

"It is a significant step along what is ultimately a long pathway, but it's looking very promising," Professor Charman said.

The drug is believed to work similarly to the most effective antimalarial drug available, artemisinin, a herbal remedy. But artemisinin is dearer and access is limited in poor countries.

The project was organised by the Medicines for Malaria Venture, a non-profit organisation. Its chief executive, Dr Christopher Hentschel, said the need to develop a cheap antimalarial drug was "more urgent than ever".

"This could be the biggest breakthrough in malaria treatment of our generation," he said.

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The Hindu (India)

Ranbaxy begins clinical trials on malarial drug

By N. Gopal Raj

THIRUVANANTHAPURAM, AUG. 18. In what is being described as a major breakthrough in treating malaria, scientists have developed a drug that acts like artemisinin derivatives, which are now the most effective against drug-resistant forms, but will be cheaper and easier to produce. Ranbaxy Laboratories has begun the clinical trials that are necessary to prove the drug's efficacy and safety.

Researchers in the U.S., Australia and Switzerland successfully created a new drug, which has been given the tag `OZ277.' Publishing their work in the latest issue of Nature, the scientists say that OZ277 acts in a similar fashion as artemisinin derivatives (it is pertinent to point out here that as yields from the artemisining extraction process is poor, the derivatives are too expensive for poor countries which need it most) but is even more potent than the latter. As OZ277 is a synthetic drug and does not require natural plant extracts, its costs can be significantly reduced and the production of the drug can be easier and quicker, according to Medicines for Malaria Venture (MMV), the international non-profit organisation based in Geneva, that promotes development of anti-malarial drugs.

In May 2003, MMV signed on Ranbaxy Lab as its industry partner for taking OZ277 to the market. The drug is currently undergoing Phase-I clinical trials in the United Kingdom, according to a press release issued today by Ranbaxy.

The Indian Express

Ranbaxy, MMV make anti-malarial breakthrough

[pic]

Posted online: Thursday, August 19, 2004 at 0117 hours IST

Ranbaxy Labs and Medicines for Malaria Venture (MMV) have taken a potential breakthrough anti-malarial drug into human clinical trial stage. Ranbaxy, MMV’s pharmaceutical partner for the development of this drug, has obtained authorisation from Medicines and Healthcare Products Regulatory Agency (MHPRA) to conduct clinical trials in the UK. This is the first regulatory step in new drug development after safety and drug activity is established in the pre-clinical phase. The drug — codenamed OZ277/RBx11160 — is currently being evaluated in a Phase I study for its safety, tolerability and pharmacokinetics in humans in UK. The drug is believed to have similar mode-of-action as the currently available drug artemisinin.

The Telegraph (Calcutta)

Synthetic malaria drug offers hope

London, Aug. 18 (Reuters): Scientists have created a synthetic drug which could offer new hope in the fight against malaria.

Scientists have long been interested in Artemisinin, a Chinese herbal fever remedy that comes from the bark of the sweet wormwood tree and has been shown to help kill malaria parasites.

But the naturally occurring drug is expensive to make. An international team of scientists said in research published in Nature they had developed a synthetic drug, OZ277, designed to offer the benefits of Artemisinin that could be cheaper to produce and more potent.

It will require tests before OZ277 can become a commercial drug.

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Hindustan Times

Indian, British scientists working on drug to fight malaria

Nabanita Sircar

London, August 21

[pic]At least 27 people are reported to have died of malaria in Alindra, India and 293 are seriously ill with the disease which broke out after the heavy rains and floods. Each year many die of the disease in India, but now British scientists could be on the verge of a breakthrough in a generation against the disease.

A new malaria drug is being tested, based on a traditional Chinese remedy, which could be a victory against the world's second most deadly infectious disease after AIDS, scientists said. The Indian pharmaceutical company Ranbaxy and the non-profit Medicines for Malaria Venture (MMV) are working together on the new drug.

Animal and computer studies of the therapy, known as OZ227 or OZ, suggest that it will be the most potent and effective weapon yet developed against malaria, which kills a million people a year and infects up to 500 million more. Clinical trials of its effectiveness will begin in Africa and Thailand next year. Safety tests in Britain have shown that OZ has no significant side-effects. If all tests prove successful the drug could be given to patients within four years.

OZ is modelled on the action of the most effective known antimalarial, a Chinese herbal fever remedy called artemisinin extracted from the sweet wormwood plant, Artemisia annua. Although artemisinin-based drugs are currently the best available treatment for the disease, the high cost of the refinement process makes them up to 20 times more expensive than standard therapies. That would make it unaffordable for poor countries, where malaria is endemic.

The new drug is based on the molecular structure of artemisinin and kills the malaria parasite in exactly the same way. Research indicates that its antimalarial action is even more powerful. OZ is entirely synthetic, and can thus be mass-produced much more cheaply than natural artemisinin, without the need to extract chemicals from a plant. It also has a longer shelf life than the natural drug, and fewer doses are needed to produce its full effects.

"This could be the biggest breakthrough in malaria treatment in our generation," Christopher Hentschel, chief executive of MMV, said. "The need to develop a low-cost, potent synthetic antimalarial drug is more urgent than ever. This project has surpassed our expectations. The animal models are quite predictive and they show that the drug is much more potent than anything else we have seen. We already know that this class of drug works, so the risk it won't work in humans is very low. The data for this particular group are very convincing indeed."

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The Daily Times (Bangladesh)

New drug boosts malaria fight

AFP, Paris

Tests on a new antimalarial drug suggest it could be the biggest breakthrough in treatment of the disease for a generation, the British scientific review Nature says in its yesterday edition.

Codenamed OZ, the drug is synthetic and works in the same way as the most effective antimalarial treatment, a Chinese herbal medicine called artemisinin.

"The drug could be the biggest breakthrough in malarial treatment of our generation and could become the most potent weapon against drug-resistant malaria," according to the Medicines for Malaria Venture (MMV).

"Initial clinical studies in humans have found the drug to be safe and well-tolerated.

"The synthetic drug could be a much cheaper and more effective alternative to the current malaria cures."

"Because OZ is a synthetic drug and does not require the natural plant, like artemisinin-based combination therapies (ACTs), its costs can be significantly reduced and the production of the drug can be easier and quicker to meet the demand," MMV says.

MMV describes itself as a non-profit organisation established to discover, develop and deliver new affordable anti-malarial drugs through effective public-private partnerships.

The new drug is currently being developed by MMV's industry partner, Ranbaxy Laboratories Ltd. in India. The original drug research was done by a team of researchers from the University of Nebraska, Monash University in Australia, the Swiss Tropical Institute and F. Hoffman Roche of Switzerland.

Drug resistance is a major problem for malaria, which affects nearly 40 percent of the world's population.

The standard cheap medicines are rendered useless in almost every corner of sub-Saharan Africa, where every 30 seconds a child dies of malaria. Malaria is a treatable disease, yet every year more than one million people die from it.

"OZ is currently being tested in humans in the UK for safety, tolerance and drug activity," MMV says.

"The test for its efficacy in malaria patients will begin in January 2005. If successful, it could be the next major weapon in the fight against malaria."

Aljazeera + Agencies

Breakthrough malarial drug on trial

Thursday 19 August 2004, 3:21 Makka Time, 0:21 GMT

India's Ranbaxy Laboratories has said it's developed a new anti-malarial drug, claiming it would cost less but work as well as costlier drugs now being used.

The drug, a synthetic peroxide code named OZ developed with Geneva-based aid group Medicines for Malaria Venture, is now undergoing clinical trials in Britain, a Ranbaxy statement said on Wednesday.

"Our scientists are excited to be able to work on a drug that could save millions of lives," Ranbaxy Chief Executive Officer Brian Tempest said in the statement.

The statement said the new drug will work as well as artemisinin, a currently available anti-malaria drug, and will be much cheaper.

Artemisinin is a herbal remedy based on the Artemisia annua plant. However, because of the costly and lengthy extraction process from the plant, artemisinins are at least 10 times more expensive than the cheap standard antimalarials.

Artemisinin combination therapy costs about US$2 (euros 1.6) per dose, an amount beyond the reach of many in poor countries. Cheap medicines such as chloroquine no longer cure the disease in Africa because malaria parasites have become resistant to it. Resistance is also spreading in India.

"We know about this synthetic peroxide developed by Ranbaxy. The reports that we have heard about it are certainly very promising," said Allan Schapira, coordinator of strategy and policy for the World Health Organization's "Rollback Malaria" campaign.

But knowledge about the drug is "insufficient to make a judgment at the moment," Schapira said. "We hope that it will prove highly efficacious."

Findings from tests on the new drug are being published in the August 19 issue of the science journal Nature.

Malaria, which is carried by mosquitoes, kills more than 1 million people a year, with 90% of the deaths occurring in Africa, according to the United Nations. Most of the victims are children under age 5.

Malaria also costs Africa an estimated US$12 billion (euros 9.73 billion) a year in lost gross domestic product and drains 40% of its public health spending.

"The need to develop a low-cost, potent, synthetic anti-malarial drug is more urgent than ever," said Christopher Hentschel, chief executive of Medicines for Malaria Venture. "This could be the biggest breakthrough in malaria treatment of our generation."

The Independent (South Africa)

Indian company develops new anti-malaria drug

    August 18 2004 at 04:09PM

New Delhi - India's Ranbaxy Laboratories announced on Wednesday it has developed a new anti-malaria drug, which it claimed would be cheaper and as effective as the drugs now used to cure the disease that kills more than a million people worldwide every year.

The drug, a synthetic peroxide developed with Geneva aid group Medicines for Malaria Venture, is now undergoing clinical trials in Britain, a Ranbaxy statement said.

"Our scientists are excited to be able to work on a drug that could save millions of lives," Ranbaxy Chief Executive Officer Brian Tempest said in the company statement.

The new drug will work as well as artemisinin, the most effective anti-malaria drug currently available, and be much cheaper, the statement said, without elaborating.

Artemisinin combination therapy costs about $2 (about R12) per dose, an amount beyond the reach of many sufferers in poor countries, and cheap medicines such as chloroquine no longer cure the disease in Africa because the parasites have become resistant to it.

Resistance is spreading in India, too.

Malaria, which is carried by female mosquitoes, kills more than one million people a year, with 90 percent of the deaths occurring in Africa, according to the United Nations. Most of the victims are children under five.

Malaria also costs Africa an estimated $12-billion (about R77-billion) a year in lost gross domestic product and drains 40 percent of its public health spending.

"The need to develop a low-cost, potent synthetic anti-malarial drug is more urgent than ever," said Christopher Hentschel, chief executive of Medicines for Malaria Venture.

In May 2003, Ranbaxy Laboratories, India's largest pharmaceutical company, entered into an agreement with the Geneva-based body for laboratory testing, clinical trials and commercial development of the drug.

Findings from tests on the new drug are being published in the August 19 issue of the science journal Nature.

The Independent (South Africa)_

Using old and new in the war against malaria

    August 23 2004 at 09:12AM

Liverpool - A new drug based on an ancient Chinese remedy could revolutionise the treatment of malaria.

Clinical trials are under way in Britain to test how effectively it combats the increasingly drug-resistant malaria parasite.

The drug is a synthetic, simpler version of a traditional Chinese cure which could be around five times cheaper to produce than other treatments.

Malaria kills around one million people every year and causes another 300 million to fall sick.

Drugs based on the Chinese remedy artemisinin have already been developed as a means of tackling chloroquine-resistant strains of the parasite.

Called RBx-11160, the new drug is a simpler, synthetic and slightly altered version of artemisinin, according to a report in Nature magazine published on Monday.

Developed by the non-profit organisation Medicines for Malaria, the drug is soluble and can be given orally or injected intravenously.

In tests already carried out on infected mice, between 95 percent and 100 percent of parasites disappeared within four days following treatment with the new drug.

This compares with conventional artemisinin drugs which take a week to clear 95 percent of parasites.

The new drug entered clinical trials in Britain last month.

Malaria researcher Paul O'Neill, from Liverpool University, said: "This is potentially extremely important."

O'Neill said that, if the drug was found to be effective, it would probably be given to patients in combination with a second drug.

"The parasites find it more difficult to develop resistance when bombarded by two drugs targeting multiple pathways," he said.

Malaria can be contracted by those who live in or visit around 100 countries across the tropics and subtropics, with about 40 percent of the world's population at risk.

Ninety percent of deaths from malaria happen in sub-Saharan Africa - mostly among young children. Malaria kills an African child every 30 seconds.

There are four main types of malaria, which are all spread by mosquitoes.

The main symptoms are high fever, chills, headache and sickness and the illness is often mistaken for flu.

RBx-11160 was produced in collaboration by three academic groups and three biotechnology firms, according to Nature magazine. - Sapa-dpa

The Sunday Times (South Africa)

New malaria 'super drug'

A SYNTHETIC version of a drug used for more than 1 500 years in Chinese medicine has been hailed as a breakthrough in efforts to reduce the million deaths caused each year by malaria.

Treatment based on the Chinese herbal remedy qinghaosu was developed during the Cultural Revolution but tensions with the West delayed its spread.

Now derivatives of artemisinin, a compound extracted from sweet wormwood, offer the most effective antimalarial therapy available. Malaria parasites have never evolved resistance to it.

Like all drugs, artemisinin-based drugs have drawbacks: relatively expensive extraction - the plant takes about 18 months to grow; treatment regimens can be too long for the Third World and, although it can quickly kill 96% of the malaria-causing parasites, it has to be combined with longer-acting variants to be completely effective.

Dr Jonathan Vennerstrom and colleagues say in the journal Nature they have made a fast-acting synthetic counterpart to artemisinin in which many of those problems have been overcome.

Dubbed OZ, the drug has just entered clinical trials on 48 people in Britain. Initial studies suggest it is well-tolerated in healthy volunteers.

This new class of drug is "a huge breakthrough," said Dr Paul O'Neill of Liverpool University. It is being developed in India following studies by scientists in the US, Australia, Britain and Switzerland.

Because OZ is a synthetic drug, its costs can be significantly reduced.

The drug will be tried on malaria patients in January. The non-profit group driving drug development, Medicines for Malaria Venture, said this week it could become the most potent weapon against drug-resistant malaria, which affects 40% of the global population.

Standard cheap malaria drugs are failing as much as 80% of the time as malaria parasites become more resistant to older drugs, such as chloroquine. Standard cheap medicines are rendered useless in sub-Saharan Africa where a child dies of malaria every 30 seconds.

Professor Andrew Read, of Edinburgh University, welcomed the advance but added: "There is always great optimism when a new 'wonder drug' comes along, yet malaria parasites are extremely adept at evolving drug resistance." - © The Telegraph, London

KBC (Kenyan Broadcast Corporation)

New drug to boost malaria fight

BY: Chris Khisa/BBC

DATE: Friday, August 20, 2004

Scientists have developed a new drug which they say could transform the fight against malaria.

The drug is a synthetic version of Artemisinin - a herb extract that has been used for centuries in China.

Artemisinin-based drugs are already available but the manufacturing process makes them expensive.

Writing in Nature, scientists said they had succeeded in developing a drug in the laboratory that can mimic its effects at a fraction of the cost.

Malaria kills around one million people around the world each year, most of them children. The disease is spread by mosquitoes.

The World Health Organization has set a target to reduce malaria deaths by half by 2010.

However, increasing resistance to the cheap drugs used to treat the disease are threatening that plan.

Artemisinin-based drugs are regarded as the most effective weapon against malaria. However, their high cost puts them out of reach of millions of people in the developing world who need them most.

"Making it is difficult and expensive," said Brian Greenwood, professor of tropical medicine at the London School of Hygiene and Tropical Medicine.

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Reuters

Scientists Make Malaria Drug Based on Herbal Remedy

Wed 18 August, 2004 18:30

| |

LONDON (Reuters) - Scientists have created a synthetic drug which could offer new hope in the fight against malaria.

Nearly two billion people live in areas affected by malaria. The disease, transmitted by mosquitoes, is becoming a bigger threat as the parasite that causes it develops immunity to drugs used to fight it.

The new drug is based on a chemical found in traditional Chinese herbal medicine.

Scientists have long been interested in Artemisinin, a herbal fever remedy that comes from the bark of the sweet wormwood tree and has been shown to help kill malaria parasites.

But the naturally occurring drug is expensive to make and requires complicated treatment programs that are difficult to get patients to comply with.

An international team of scientists in the United States, Britain, Switzerland and Australia said in research published in the British science journal Nature they had developed a synthetic drug, OZ277, designed to offer the benefits of Artemisinin that could be cheaper to produce and more potent.

It will require tests before OZ277 can become a commercial drug. But in an accompanying article, Paul O'Neill of the Chemistry and Pharmacology departments of the University of Liverpool said the new class of compounds "could offer the best solution to date for destroying drug-resistant malaria parasites."

Agence France-Presse

Une nouvelle molécule prometteuse contre le paludisme

Agence France-Presse

Paris

Une nouvelle molécule anti-paludisme obtenue entièrement par synthèse et bien tolérée par l'organisme, selon des tests cliniques préliminaires, pourrait devenir une arme majeure contre cette maladie qui touche 600 millions d'humains dans le monde et tue un enfant africain toutes les 30 secondes.

La découverte de cette molécule, inspirée d'une substance provenant d'une herbe médicinale chinoise plus que millénaire, l'artémisinine, est décrite dans la revue scientifique britannique Nature publiée jeudi par une équipe internationale associant notamment des chercheurs des universités du Nebraska, de Monash (Australie), de l'Institut tropical suisse et de la firme pharmaceutique suisse Hoffman Roche.

Depuis une quinzaine d'années, des équipes ont tenté en vain de réaliser la synthèse de cette molécule, peu chère à produire, relève dans la revue Paul O'Neill de l'université de Liverpool en saluant la réussite de Jonathan Vennerstrom (États-Unis), Sergio Witllin (Suisse), William Charman (Australie) et leurs collègues.

Baptisée OZ 277, elle est actuellement développée par la firme pharmaceutique indienne Ranbaxy partenaire du MMV (Medicines for Malaria Venture), une organisation sans but lucratif dédiée à la recherche de nouvelles thérapeutiques anti-paludisme peu coûteuses, grâce à des partenariats entre le public et le privé.

Dans de nombreux endroits, les parasites responsables de la maladie, transmise par les moustiques, sont devenus résistants aux médicaments utilisés depuis très longtemps. L'OMS recommande donc aux pays où l'on enregistre une résistance aux médicaments conventionnels de passer aux puissantes associations médicamenteuses dérivées de l'artémisine (ACT). Mais même à 2 dollars la dose adulte, ces associations sont dix à vingt fois plus chères que les anciennes monothérapies type chloroquine.

D'où l'enjeu de cette recherche. D'autant, soulignent les chercheurs, qu'il n'existe pas de résistance prouvée contre l'artémisinine et ses dérivés.

Contrairement aux dérivés semi-synthétiques d'artémisine actuellement disponibles (artéméter, artésunate), l'OZ peut être totalement synthétisée à grande échelle à un coût plus abordable pour l'Afrique, sans avoir à recourir aux extraits végétaux d'armoise amère.

L'objectif visé est un traitement simple et court, en une seule prise orale par jour pendant trois jours maximum.

Les nouveaux produits de synthèses concoctés par l'équipe internationale sont «plus puissants et agissent plus longtemps in vivo que l'artéméter et l'artésunate», note Paul O'Neill.

Les tests de sécurité et de bonne tolérance d'OZ (pour ozonide) sont conduits en Grande-Bretagne, indique le MMV.

«Les tests d'efficacité sur des patients atteints de paludisme commenceront en janvier 2005», précise cette organisation.

«En cas de succès, ce médicament pourrait devenir la prochaine arme majeure pour combattre la maladie et la plus puissante arme pour combattre les problèmes de résistance aux traitements, estime-t-elle. Il pourrait représenter la plus importante percée thérapeutique anti-paludisme de notre génération», s'enthousiasme le MMV.

Le paludisme est une maladie parasitaire que l'on peut traiter. Pourtant, chaque année plus d'un million de personnes en meurent.

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Le Monde (France)

Une nouvelle molécule suscite l'espoir dans la lutte contre le paludisme

LEMONDE.FR | 18.08.04 | 20h04

La nouvelle molécule baptisée OZ 277 a l'avantage de pouvoir être synthétisée à grande échelle à un coût plus abordable pour l'Afrique. Elle permettrait également un traitement simple et court contre la maladie.

Une nouvelle molécule antipaludisme obtenue entièrement par synthèse et bien tolérée par l'organisme, selon des tests cliniques préliminaires, pourrait devenir une arme majeure contre cette maladie, qui touche 600 millions d'êtres humains dans le monde et tue un enfant africain toutes les 30 secondes.

La découverte de cette molécule, conçue à partir d'une susbstance provenant d'une herbe médicinale chinoise plus que millénaire, l'artémisinine, est décrite dans la revue scientifique britannique Nature publiée jeudi 19 août par une équipe internationale associant notamment des chercheurs des universités du Nebraska (Etats-Unis), de Monash (Australie), de l'Institut tropical suisse et de la firme pharmaceutique suisse Hoffman Roche.

Depuis une quinzaine d'années, des équipes ont tenté en vain de réaliser la synthèse de cette molécule, peu chère à produire, relève dans la revue Paul O'Neill de l'université de Liverpool (Grande-Bretagne) en saluant la réussite de Jonathan Vennerstrom (Etats-Unis), Sergio Witllin (Suisse), William Charman (Australie) et leurs collègues.

Baptisée OZ 277, elle est actuellement développée par la firme pharmaceutique indienne Ranbaxy, partenaire du MMV (Medicines for Malaria Venture), une organisation sans but lucratif consacrée à la recherche de nouvelles thérapeutiques antipaludisme peu coûteuses, grâce à des partenariats entre le public et le privé.

UN COÛT ABORDABLE POUR L'AFRIQUE

Dans de nombreux endroits, les parasites responsables de la maladie, transmise par les moustiques, sont devenus résistants aux médicaments les meilleur marché utilisés depuis très longtemps. L'OMS recommande donc aux pays où l'on enregistre une résistance aux médicaments conventionnels de passer aux puissantes associations médicamenteuses dérivées de l'artémisine (ACT). Mais même à 2 dollars la dose adulte, ces associations sont dix à vingt fois plus chères que les anciennes monothérapies type chloroquine. D'où l'enjeu de cette recherche.

D'autant, soulignent les chercheurs, qu'il n'existe pas de résistance prouvée contre l'artémisinine et ses dérivés. Contrairement aux dérivés semi-synthétiques d'artémisine actuellement disponibles (artéméter, artésunate), l'"OZ" peut être totalement synthétisée à grande échelle à un coût plus abordable pour l'Afrique, sans avoir à recourir aux extraits végétaux d'armoise amère. L'objectif visé est un traitement simple et court, en une seule prise orale par jour pendant trois jours maximum.

Les nouveaux produits de synthèse concoctés par l'équipe internationale sont "plus puissants et agissent plus longtemps in vivo que l'artéméter et l'artésunate", note Paul O'Neill. Les tests de sécurité et de bonne tolérance d'"OZ" (pour "ozonide") sont conduits en Grande-Bretagne, indique le MMV.

"Les tests d'efficacité sur des patients atteints de paludisme commenceront en janvier 2005", précise cette organisation. "En cas de succès, ce médicament pourrait devenir la prochaine arme majeure pour combattre la maladie" et "la plus puissante arme" pour combattre les problèmes de résistance aux traitements, estime-t-elle. Il pourrait représenter "la plus importante percée thérapeutique antipaludisme de notre génération", s'enthousiasme le MMV.

Le paludisme est une maladie parasitaire que l'on peut traiter. Pourtant, chaque année plus d'un million de personnes en meurent.

Avec AFP

Deutche Welle (TV-Radio)

New drug raises hopes for malaria cure

Tests on a new drug for curing malaria suggest it could be the biggest breakthrough in treatment of the disease. Code named OZ, the drug is synthetic and works in the same way as the most effective antimalarial treatment, a Chinese herbal medicine called artemisinin. Initial clinical studies in humans have found the drug to be safe and well-tolerated, according to the Medicines for Malaria Venture (MMV) organisation. Drug resistance is a major problem for malaria, which affects nearly 40 percent of the world's population

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Basler Zeitung (Switzerland)

Die Malaria hat einen neuen Gegner – aus Basel

Basler Forscher haben massgebend dazu beigetragen, dass ein neuer Wirkstoff gegen Malaria entwickelt werden konnte. Er beruht auf der chinesischen Heilpflanze Artemisia. Erstmals ist es mit dieser Verbindung gelungen, das Wirkprinzip der Pflanze im Reagenzglas nachzubauen.

Basel. Manche sprechen von einem grossen Durchbruch, andere äussern sich noch zurückhaltend. Doch alle, die das Projekt kennen, sind des Lobes voll. So auch Reto Brun, Forschungsgruppenleiter am Schweizerischen Tropeninstitut (STI) in Basel. Er hat mit seinem Team am Projekt mitgearbeitet und sagt: «Wir haben endlich eine neue Wirksubstanz gegen Malaria gefunden. Das Potenzial der Substanz ist riesig.»

Von Stefan Stöcklin

Der Stoff mit dem Namen OZ277, der in der heutigen Ausgabe des Fachblattes «Nature» vorgestellt wird, ist äusserst wirksam gegen Plasmodium falciparum, den gefährlichsten Malaria-Erreger. Soweit heute bekannt ist, wird das Produkt von Menschen gut vertragen. Besonders wichtig für die künftige Anwendung in den betroffenen Ländern ist: Der Stoff kann günstig synthetisch hergestellt werden. Bisher mussten die Wirkstoffe in einem aufwändigen und teuren Verfahren aus der Pflanze Artemisia isoliert werden. Die Substanz hat genau das Profil, nach dem Malariaforscher seit Jahren fahnden. Verlaufen die klinischen Studien nach Plan, so dürfte sie zu einem wichtigen Pfeiler im Kampf gegen eine Krankheit werden, die sich in den letzten Jahren immer weiter ausgebreitet hat. Zurzeit erkranken jedes Jahr über

300 Millionen Menschen an Malaria, für mehr als eine Million endet sie tödlich, prekär ist die Lage vor allem in Afrika südlich der Sahara. Resistenzen des Erregers haben alte Medikamente wie Chloroquin oder Sulphadoxin-Pyrimethamin (Fansidar) nutzlos gemacht.

Von der Natur abgeguckt

Für die Entwicklung der Substanz haben sich die Forscher die chinesische Heilpflanze Artemisia annua L. (Beifuss) zum Vorbild genommen. Seit 1500 Jahren werden Beifuss-Exktrakte in China zur Linderung von Malariaanfällen eingesetzt. Bereits vor Jahren gelang es, die als Artemisinine bezeichneten Pflanzenwirkstoffe zu isolieren. Sie sind zu unverzichtbaren Medikamenten weiter entwickelt worden und werden bereits eingesetzt (siehe Kasten). Der Naturstoff ist das eine, eine synthetische Variante das andere. Malariaforscher hatten sich bereits vor Jahren das Ziel gesetzt, die Wirkung der natürlichen Artemisinine zu kopieren und falls möglich zu verbessern. Hier kommt die Basler Roche ins Spiel, die einst auf dem Gebiet der Malariaforschung eine wichtige Rolle gespielt hat. Sie konnte sich damals Rechte an den

Artemisininen sichern und erforschte synthetische Kopien. Diese Arbeiten in Zusammenarbeit mit US-Forschern in Nebraska begannen 1998 und waren erfolgreich. Trotzdem gab Roche im Zuge einer Reorganisation Ende der 90er Jahre diese Arbeiten auf und trat Teile davon ans Tropeninstitut ab. Forschungen zu Infektionskrankheiten in Drittwelt-Ländern wurden von Roche gestoppt, da sie wenig lukrativ erschienen. Andere übernahmen das Projekt. Es traf sich gut, dass sich Ende der 90er Jahre die gemeinnützige Organisation MMV (Medicines for Malaria Venture) formierte, die durch Kooperationen geeigneter Partner die vernachlässigte Malariaforschung voran bringen wollte. Sie nahm im Jahr 1999 das laufende Artemisinin-

Projekt der Basler Firma auf. So kam es zum Forschungskonsortium, das hinter OZ277 steckt. Nebst dem Basler Tropeninstitut, Roche und Basilea Pharmaceutica sind daran Forscher in den USA und Australien beteiligt. Eine entscheidende Rolle in der Entwicklung spielte Jonathan Vennerstrom von der Universität Nebraska in Omaha. Er hatte zusammen mit Hugues

Matile von Hoffmann-La Roche die Idee, wie die Aktivität der Artemisinine – es handelt sich um eine Peroxid-Gruppe – in einem synthetischen Präparat konserviert werden könnte. Vor ihnen waren an dieser Aufgabe Dutzende von Forschern gescheitert. Als ihnen eine Lösung gelang, wurden diese Rohpräparate weiter modifiziert, um den Wirkstoff für die medizinischenwendung zu optimieren. Am Tropeninstitut in Basel wurden genau 277 Varianten getestet, bis ein geeigneter Stoff gefunden war – der Namen OZ277 rührt daher.

Studien am Menschen

Im Vergleich zu den natürlichen Artemisininen schneidet OZ277 in den bisherigen Tests hervorragend ab. Es ist wirksamer, die Aktivität dauert länger, und aufgrund bisheriger Studien gibt es keine Anzeichen von Nebenwirkungen. Erste Studien am Menschen in Grossbritannien haben die gute Verträglichkeit belegt – kein Wunder, sind die beteiligten Forscher und MMV äusserst optimistisch. «Wir rechnen mit einem synthetischen Artemisinin-Produkt, das hervorragend wirkt und weniger häufig eingenommen werden muss als die bisherigen

Pflanzenprodukte», so Anna Wang von MMV in Genf. So weit ist es noch nicht. Zunächst muss in grossen Studien gezeigt werden, dass OZ277 Malaria-Patienten effizient heilen kann. Nichts deutet darauf hin, dass es zu Rückschlägen kommen könnte. «Ganz sicher kann man aber nie

sein», sagt Brun. Geht alles nach Plan, so sollten bereits 2008 neue Malaria-Präparate auf den Markt kommen. Wang rechnet mit einem Preis von unter einem Dollar pro Behandlungsset. Kombinationspräparate werden auch bereits angedacht, um die Entwicklung von Resistenzen zu erschweren. Produziert wird OZ277 von der indischen Firma Ranbaxy, an die Hoffmann-La Roche vor einem Jahr alle Rechte abgetreten hat.

TSR (Television Suisse Romand)

Découverte d'une nouvelle molécule prometteuse contre le paludisme

ATS, le 18 août 2004 à 19:29

PARIS - Des scientifiques ont découvert une molécule prometteuse pour lutter contre le paludisme, une maladie qui touche 600 millions d'humains dans le monde. La nouvelle molécule est obtenue entièrement par synthèse.

Elle est bien tolérée par l'organisme, selon des tests cliniques préliminaires. La découverte de cette molécule, inspirée d'un composant d'une plante chinoise, l'artémisine, est décrite dans la revue scientifique britannique «Nature» qui sera publié jeudi.

Elle est le fait d'une équipe internationale associant notamment des chercheurs des universités du Nebraska (Etats-Unis), de Monash (Australie), de l'Institut tropical suisse et de la firme pharmaceutique suisse Hoffmann Roche.

La molécule, baptisée OZ 277, est actuellement développée par une organisation sans but lucratif dédiée à la recherche de nouvelles thérapeutiques anti-paludisme peu coûteuses. Cette dernière fonctionne grâce à des partenariats entre le public et le privé, le MMV (Medicines for Malaria Venture) et la firme pharmaceutique indienne Ranbaxy.

Les tests de sécurité et de bonne tolérance d'»OZ» sont conduits en Grande-Bretagne, indique le MMV. Les tests d'efficacité sur des patients atteints de paludisme commenceront en janvier 2005.

«En cas de succès, ce médicament pourrait devenir la prochaine arme majeure pour combattre la maladie» et «la plus puissante arme» pour combattre les problèmes de résistances aux traitements, estime le MMV.

Le paludisme est une maladie parasitaire que l'on peut traiter et pourtant chaque année plus d'un million de personnes en meurent. Elle tue un enfant Africain toutes les 30 secondes.

Beifuß war Vorbild

Vielversprechendes Malaria-Mittel entwickelt

Nach pflanzlichem Vorbild hat ein internationales Forscherteam einen besonders aussichtsreichen Wirkstoff gegen Malaria hergestellt.

20.08.04 - Die neue Substanz "OZ277" wirkt gegen eines der Schlüsselenzyme der einzelligen Krankheitserreger. Die Forscher orientierten sich an der Substanz "Artemisinin" aus dem Einjährigen Beifuß (Artemisia annua). "OZ277" lässt sich vergleichweise einfach produzieren und wirkt nach Angaben der Forscher im Fachjournal "Nature" (Bd. 430, S. 900) gegen mehrere Stadien der Erreger. Es solle noch in diesem Jahr erste Tests am Menschen geben, nachdem Tierversuche sehr ermutigend verlaufen seien, berichtet die Gruppe um Jonathan Vennerstrom von der Universität von Nebraska in Omaha (USA).

Artemisinin erwies sich bereits vor 30 Jahren als gutes Mittel gegen Malaria, in der chinesischen Naturmedizin wird Beifuß schon seit 1500 Jahren geschätzt. Die Natursubstanz lässt sich jedoch nur mit einem teuren Verfahren aus der Pflanze isolieren, wird vom Körper zudem nicht besonders gut aufgenommen und ist damit in den armen Ländern nicht sehr weit verbreitet. Der synthetische Wirkstoff ist besser wasserlöslich und kann auch in größeren Mengen hergestellt werden.

Die von Mücken übertragenen Malaria-Erreger töten nach UN-Angaben mindestens eine Million Menschen im Jahr. Fast alle der jährlich 300 Millionen Krankheitsfälle treten in den tropischen Ländern auf.

"Kombiniert mit einem zweiten Malariamittel könnte diese neue Klasse (von Medikamenten) die zurzeit beste Lösung sein, um resistente Malariaparasiten zu zerstören", schriebt Paul O'Neill von der Universität in Liverpool in einem begleitenden "Nature"-Kommentar.

Die Welt (Germany)

Ein scharfes Schwert gegen Malaria

Forscher entwickeln Medikament nach Pflanzenvorbild - Keine Resistenzen

von Samiha Shafy

Omaha -  Malaria ist eine globale Gefahr, die sich permanent vergrößert: Rund 40 Prozent der Weltbevölkerung leben in den tropischen und subtropischen Risikogebieten. Über 300 Millionen Menschen infizieren sich laut Weltgesundheitsorganisation (WHO) jedes Jahr mit dem Malaria-Erreger, der durch Anopheles-Mücken übertragen wird. Die heimtückische Tropenkrankheit fordert jährlich eine Million Menschenleben. Damit hat sich die Zahl der malariabedingten Todesfälle in den vergangenen drei Jahrzehnten verdoppelt. Die WHO ist noch weit entfernt von ihrem Ziel, die Zahl der Erkrankten von 2000 bis 2010 zu halbieren. Ein Grund dafür ist, dass der Parasit, der die roten Blutzellen befällt, zunehmend Resistenzen gegen die verfügbaren Medikamente entwickelt.

In der heutigen Ausgabe des Fachjournals "Nature" berichtet nun ein internationales Forscherteam um Jonathan L. Vennerstrom von der Universität von Nebraska in Omaha über eine Entdeckung, die große Hoffnungen weckt: Die Forscher haben einen synthetischen Wirkstoff entwickelt, der ähnliche Eigenschaften besitzt wie eine derzeit verwendete Klasse von Malaria-Medikamenten, deren Wirkstoff Artemisinin aus der chinesischen Heilpflanze Artemisia annua gewonnen wird. Diese so genannten Artesunate und Artemether werden gegenwärtig von der WHO als bestes Mittel gegen Malaria empfohlen, weil sie effektiv wirken und im Gegensatz zu den meisten anderen Medikamenten bisher keine Resistenzen hervorgerufen haben. Sie haben aber auch Nachteile: So sind sie teuer herzustellen und wirken nur für kurze Zeit.

"Das Artemisinin-Molekül ist zu komplex, um es zu einem vernünftigen Preis künstlich herzustellen. Deshalb haben wir den Teil des Moleküls, der für die Wirkung verantwortlich ist, in ein einfacheres Molekül eingebaut", erläutert Reto Brun vom Schweizerischen Tropeninstitut in Basel, der an der Studie beteiligt war. Dieser wirksame Teil ist eine so genannte Peroxidbrücke, die mit einem Stoffwechselprodukt des Erregers reagiert. Dadurch bilden sich im Parasiten aggressive Zellgifte, die ihn töten, die menschliche Wirtszelle aber nicht schädigen.

Bei ihrem 277. Versuch, ein künstliches Molekül mit demselben Wirkmechanismus zu "bauen", waren die Forscher erfolgreich: Der synthetische Wirkstoff, genannt OZ277, bekämpfte den Malaria-Erreger Plasmodium falciparum im Tierversuch sogar effektiver und dauerhafter als die heutigen Medikamente auf Pflanzenbasis. Außerdem eignet er sich besser für eine kostengünstige Massenproduktion. "Wir haben den Stoff gegen 14 verschiedene Stämme des Parasiten getestet, und er wirkte bei allen gleich gut. Deshalb werden wir wohl vorerst auch keine Probleme mit Resistenzen haben", sagt Brun. Zurzeit werde das neue Medikament in klinischen Studien getestet. Verlaufen die Tests erfolgreich, könnte es gemäß Brun im Jahr 2008 auf den Markt kommen.

Artikel erschienen am Do, 19. August 2004

Elmundo (Spain)

ARTEMISINA

Crean una copia sintética de una planta china eficaz contra la malaria

MARÍA VALERIO

Un equipo internacional ha logrado desarrollar una copia sintética de la planta que representa actualmente la esperanza contra la malaria para millones de enfermos. Se trata de la artemisina, una milenaria hierba china empleada tradicionalmente como remedio contra la fiebre y que la Organización Mundial de la Salud reconoce ahora como la terapia farmacológica más eficaz contra la malaria.

Sus descubridores aseguran que este fármaco sintético, con idénticas propiedades que la artemisina, es mucho más barato que la sustancia natural y permite además superar uno de los grandes problemas de los actuales tratamientos, las resistencias.

Los trabajos de un equipo de científicos procedentes de Estados Unidos, Reino Unido, Suiza y Australia acaban de aparecer publicados en la última edición de la revista 'Nature', y aunque aún habrá que esperar hasta que la sustancia, bautizada como 'OZ277' (o bien 'RBx-11160), pueda comercializarse, los especialistas se muestras optimistas con los primeros resultados.

"Hemos probado dosis diferentes en más de una docena de voluntarios sanos y los resultados son prometedores", ha explicado a la revista 'New Scientist' Lise Riopel, miembro de una organización dedicada a la lucha contra la malaria (Medicines for Malaria Venture) que está participando en la iniciativa. Según esta misma publicación, se espera que los ensayos en fase II comiencen el próximo año.

Un tratamiento más fácil de seguir

A diferencia de lo que ocurre con la artemisina natural, las pautas del tratamiento 'sintético' son más sencillas de seguir lo que permitiría combatir el problema de las resistencias, que aparecen cuando los pacientes no siguen regularmente las dosis recomendadas.

Según señalan los autores a la agencia Reuters, la enfermedad se está convirtiendo en una gran amenaza a medida que el parásito que la produce, un mosquito, adquiere inmunidad frente a los medicamentos actualmente empleados, como la cloroquina.

"A pesar del éxito del tratamiento con artemisina", indica el trabajo, "como fármaco, esta planta presenta ciertos inconvenientes químicos, biofarmacológicos y de tratamiento que limitan su potencial terapéutico". Su 'copia' de laboratorio parece superar en parte estos escollos, simplificando el régimen de dosis, y resulta hasta cinco veces más barata de producir gracias a su sencilla estructura molecular.

Según explica la edición 'on line' de la revista 'Nature', en ensayos con ratones la nueva versión ha logrado una reducción del 95-100% de los parásitos causantes de la malaria en sólo cuatro días, mientras que la artemisina necesita al menos siete días para eliminar el 95% de los parásitos.

Por su parte, Paul O'Neill, de la Universidad de Liverpool asegura en un artículo que publica la misma revista y que acompaña al trabajo, que esta sustancia de laboratorio "podría ser la mejor solución para destruir a los parásitos causantes de la malaria resistente". Según explica O'Neill, el mecanismo de OZ277 podría compararse con una especie de 'caballo de Troya' que elimina numerosas proteínas y enzimas esenciales para la supervivencia del parásito.

La artemisina ('Artemisia annua') se emplea en la lejana China desde hace más de 1.500 años, aunque su estudio contra la malaria data de hace sólo unas décadas, precisamente coincidiendo con la rápida expansión de la enfermedad. La organización Malaria for Medicine Ventures estima que cada año se necesitan entre 300 y 500 millones de tratamientos contra esta patología en todo el mundo. "Si los ensayos con humanos tienen éxito el nuevo fármaco sintético podría suponer todo un hito en esta lucha", ha asegurado Lise Riopel.

Noticias (Spain)

Nuevas drogas avivan la esperanza sobre una cura para la malaria

Los experimentos realizados con la droga sintética Codenamed OZ, denominada artemisinina en la medicina tradicional china, podría convertirse en el mayor hito de esta época en el tratamiento de la malaria, indica la revista científica británica Nature en su edición de este jueves.

"Los estudios clínicos iniciales en humanos han determinado que la droga es segura y bien tolerada", de acuerdo con la Medicines for Malaria Venture (MMV). "Los test para determinar su eficacia en pacientes de malaria comenzarán en enero de 2005. Si son exitosos, podría ser la próxima arma principal en la lucha contra la malaria", agrega.

"La droga sintética podría ser una alternativa mucho más barata y efectiva que las actuales curas de malaria", prosigue. "Como la OZ es una droga sintética y no require la planta natural, como las terapias basadas en la combinación de artemisinina (ACT), sus costes se pueden reducir significativamente y la producción de la droga puede ser más sencilla y rápida para cubrir la demanda", dice la MMV.

La MMV se describe a sí misma como una organización sin ánimo de lucro establecida para descubrir, desarrollar nuevas drogas antimalaria asequibles a través de asociaciones efectivas público-privadas.

Actualmente, los laboratorios Ranbaxy, socios de la MMV, están desarrollando en la India la nueva droga. La investigación inicial fue realizada por un equipo de la Universidad de Nebraska (EEUU), la Universidad de Monash (Australia), el Instituto Tropical Suizo y F. Hoffman Roche, de Suiza.

La resistencia a la droga es un problema que presenta la malaria, que afecta a cerca del 40% de la población mundial y que provoca la muerte de más de un millón de personas al día.

Rozpoczęły się testy kliniczne syntetycznego leku na zimnicę - Naukowcy zapowiadają przełom w walce z chorobą zabijającą 1,5 mln ludzi rocznie

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|ابتكر علماء من الولايات المتحدة وبريطانيا وسويسرا وأستراليا عقارا تركيبيا يمكن أن يبعث أملا جديدا في معركة مكافحة مرض الملاريا. | |

|ويرتكز العقار الجديد على مادة كيميائية تم العثور عليها في دواء عشبي تقليدي صيني. | |

|ويهتم العلماء منذ فترة طويلة بعقار "أرتيميسينين" وهو عبارة عن دواء عشبي للحمى يستخرج من لحاء شجرة الأفسنتين (الشيح) وبدا أنه يساعد | |

|في قتل طفيليات الملاريا. لكن العقار الطبيعي مكلف ويتطلب برامج علاج معقدة من الصعب إخضاع المرضى لها. | |

|ويقول فريق العلماء الدولي الذي نشر دراسته في دورية نيتشر العلمية البريطانية إنهم طوروا عقارا تركيبيا أسموه "OZ277" لتوفير فوائد | |

|"أرتيميسينين" يمكن إنتاجه بشكل أرخص وأكثر فعالية. | |

|ويحتاج العقار الجديد لتجارب قبل إمكانية إنتاجه بشكل تجاري، لكن العالم بول أونيل من قسم الكيمياء والصيدلة بجامعة ليفربول قال إن | |

|العقار المركب الجديد يمكن ان يوفر أفضل حل حتى الآن للقضاء على طفيليات الملاريا المقاومة للعقاقير. | |

|ويعيش مليارا شخص تقريبا في مناطق تتعرض للإصابة بالملاريا. ويمثل المرض الذي ينقله البعوض تهديدا متزايدا ما دام أن الطفيل الذي يسببه | |

|يطور مناعته لمقاومة العقاقير التي تستخدم للقضاء عليه. | |

|المصدر :رويترز | |

| | |

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FOLHA (Brazil)

Pesquisadores testam substância promissora contra a malária

da France Presse, em Paris

Uma nova substância para combater a malária obtida de maneira completamente sintética e bem tolerada pelo organismo, segundo os testes clínicos preliminares, pode se tornar uma importante arma contra a doença, que afeta 600 milhões de pessoas no mundo e mata uma criança africana a cada 30 segundos.

A descoberta desta molécula, inspirada em um componente de uma planta chinesa, a artemisina, é descrita na revista científica britânica "Nature" () que chega às bancas nesta quinta-feira por uma equipe internacional formada por pesquisadores das universidades de Nebraska (Estados Unidos), Monash (Australia), do Instituto Tropical Suíço e da empresa farmacêutica suíça Hoffman Roche.

A substância, batizada de OZ 277, está sendo desenvolvida atualmente por uma organização sem fins lucrativos dedicada à pesquisa de novas terapias baratas contra a malária, graças a parcerias entre os setores público e privado, o MMV (Medicines for Malaria Venture) e a empresa farmacêutica indiana Ranbaxy.

Os testes de segurança e boa tolerância do "OZ" fora realizados no Reino Unido, afirma o MMV. "Os testes de eficácia nos pacientes afetados pela malária começarão em janeiro de 2005", informa a organização.

"Em caso de sucesso, este medicamento pode se tornar a próxima grande arma para combater esta doença" e a mais poderosa para combater problemas de rejeição aos tratamentos, avalia.

"Pode representar o avanço terapêutico no combate à malária mais importante de nossa geração", entusiasma-se o MMV. A malária é uma doença parasitária que pode ser tratada, apesar de matar mais de um milhão de pessoas, a maioria na África.

Ao contrário dos derivados semi-sintéticos da artemisina atualmente disponível, a OZ pode ser sintetizada completamente em grande escala e a um custo acessível para a África. O objetivo perseguido é um tratamento simples e curto, em apenas uma administração oral diária durante um máximo de três dias.

Noticias (Mexico)

Crean prometedora sustancia para combatir malaria

Londres, Reino Unido, 19 de agosto. Un equipo de investigadores internacionales fabricó una sustancia que promete ser efectiva para combatir la malaria, siguiendo el modelo de un compuesto que se extrae de la artemisia (Artemisia annua), una planta anual.

Un equipo de investigadores internacionales fabricó una sustancia que promete ser efectiva para combatir la malaria, siguiendo el modelo de un compuesto que se extrae de la artemisia (Artemisia annua), una planta anual.

La nueva sustancia OZ277 ataca una enzima clave de los agentes patógenos unicelulares causantes de la malaria, los plasmodios, y es relativamente fácil de producir, explica el grupo de científicos encabezado por Jonathan Vennerstrom, de la Universidad de Nebraska en Omaha, Estados Unidos, en un artículo publicado en la revista científica británica Nature (volumen 430) en su edición de mañana jueves.

Además, el nuevo fármaco es efectivo en varios estadios del ciclo de vida del plasmodio. Los científicos esperan poder iniciar aún este año las primeras pruebas en humanos, luego de los alentadores resultados obtenidos en experimentos con animales.

Hace 30 años se descubrió que la artemisia era una buena sustancia para combatir la malaria. En la medicina natural china, la artemisia se utiliza desde hace mil 500 años.

Sin embargo, esta sustancia sólo se puede aislar de la planta a través de un costoso proceso, no es bien incorporada en el cuerpo humano y, por lo tanto, su uso no es extendido en los países pobres.

En cambio, la sustancia sintética es más soluble en agua y puede ser fabricada en grandes cantidades.

Los plasmodios, que son transmitidos por mosquitos, matan al menos a un millón de personas por año, según datos difundidos por la Organización de Naciones Unidas (ONU). Casi la totalidad de los 300 millones de casos anuales se registran en los países tropicales.

"En combinación con una segunda sustancia contra la malaria, esta nueva clase (de medicamentos) podría ser actualmente la mejor solución para destruir a los parásitos resistentes de la malaria", agrega Paul O'Neill, de la Universidad de Liverpool, en un comentario en Nature

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Noticias (Peru)

Desarrollan droga contra la malaria a base de hierbas

Científicos internacionales desarrollaron una droga, basada en la tradicional hierba medicinal china Artemisia annua, que detiene la propagación de la malaria, según un estudio divulgado hoy.

El nuevo fármaco, conocido científicamente como OZ277, ya está siendo probado en laboratorios de Gran Bretaña y podría ponerse en uso en enero del próximo año.

La investigación, realizada por expertos de Estados Unidos, Suiza, Australia y Gran Bretaña, fue publicada hoy en la revista científica Nature.

La nueva droga reproduce el tratamiento chino de artemisinina, basado en una hierba dulce conocida como Artemisia annua.

Ahora, los expertos desarrollaron la droga sintéticamente, lo cual abaratará sus costos al poder producirla en forma masiva.

La droga, que comenzó a ser desarrollada en Europa y Estados Unidos, fue producida por los laboratorios Ranbaxy de la India, en colaboración con el grupo "Medicinas contra la Malaria".

El anuncio fue calificado "de gran importancia médica y de prevención" por la comunidad científica de Gran Bretaña y Estados Unidos.

La hierba Artemisia es conocida como un práctico remedio desde hace más de 1.500 años, pero su valor para los tratamientos contra la malaria, sólo comenzó a estudiarse en los últimos 30 años.

Ese medicamento creado de la extracción de sustancias de la hierba, mataba directamente al parásito de la malaria, propagado por el mosquito Anófeles, que al contaminar la sangre posibilita la entrada del parásito en el sistema circulatorio humano.

Sin embargo, esa primera droga era difícil de producir y muy costosa.

"Esto se debe a que la planta de Artemisia tarda 18 meses en crecer y luego la droga debe ser extraída con mucho cuidado", explicó Brian Greenwood, especialista de la Escuela de Medicina Tropical e Higiene de Londres.

"La nueva investigación ha logrado producir una droga similar que aquella derivada de la planta, pero que deja de ser cara de producir y no tiene que esperar a que la planta crezca", agregó el científico.

En æfrica, donde las últimas cifras oficiales establecen que la malaria mata a un niño cada 30 segundos, se necesitan 500 millones de dosis de medicina contra esa enfermedad, y el costo de tratamientos ascendió en el último año a 13.000 millones de dólares, el 40 por ciento del dinero público destinado a la Salud.

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El Tiempo (Venezuela)

Logran fármaco contra la malaria

      LONDRES - Los científicos crearon un fármaco sintético que puede ofrecer nuevas esperanzas en la lucha contra la malaria.

      Casi 2.000 millones de personas viven en áreas afectadas por la malaria. La enfermedad, transmitida por los mosquitos, se está convirtiendo en una amenaza mayor a medida que el parásito que la causa desarrolla inmunidad a los fármacos utilizados para combatirlo.

      El nuevo medicamento se basa en un químico que se encuentra en la tradicional medicina china de hierbas.

      Desde hace tiempo los científicos están interesados en la artemisinina, un remedio para la fiebre en base a hierbas, que proviene de la corteza del árbol del ajenjo y que se ha demostrado puede servir para matar a los parásitos de la malaria.

      Pero la elaboración de este fármaco natural es caro y requiere unos complicados programas de tratamiento, que es difícil que los pacientes cumplan.

      Un equipo internacional de científicos de Estados Unidos, Gran Bretaña, Suiza y Australia dijo en una investigación que apareció en la publicación científica británica Nature que había desarrollado un fármaco sintético, el OZ277, diseñado para ofrecer los beneficios de la artemisinina y que podría ser más barato de producir, además de tener mayor potencia.

      Antes de que el OZ277 pueda convertirse en un medicamento comercial, deberá superar algunas pruebas.

      Pero, en otro artículo publicado, Paul O'Neill, de los departamentos de Química y Farmacología de la Universidad de Liverpool, dijo que la nueva clase de componentes "podría ofrecer la mejor solución hasta la fecha para destruir a los parásitos de la malaria resistentes a los fármacos."

El Nacional (Venezuela)

Prueban nueva molécula sintética contra el paludismo

Una nueva molécula antipaludismo obtenida de manera completamente sintética y bien tolerada por el organismo, según las pruebas clínicas preliminares, podría convertirse en un importante arma contra esta enfermedad que afecta a 600 millones de personas en el mundo y mata a un niño africano cada 30 segundos.

El descubrimiento de esta molécula, inspirada en un componente de una planta china, la artemisina, se describe en la revista científica británica Nature que sale a la venta el jueves, por un equipo internacional que asocia a investigadores de las universidades de Nebraska (Estados Unidos), Monash (Australia), del Instituto Tropical Suizo y de la firma farmacéutica suiza Hoffman Roche.

La molécula, bautizada como OZ 277, está siendo desarrollada actualmente por una organización sin fines de lucro dedicada a la investigación de nuevas terapias contra el paludismo poco costosas, gracias a asociaciones entre el sector público y privado, el MMV (Medicines for Malaria Venture) y la firma farmacéutica india Ranbaxy.

Las pruebas de seguridad y de buena tolerancia de la "OZ" se realizan en Gran Bretaña, indica el MMV. "Los tests de eficacia en los pacientes afectados por el paludismo comenzarán en enero 2005", precisa esta organización. "En caso de éxito, este medicamento podría convertirse en la próxima gran arma para combatir esta enfermedad" y "el arma más poderosa" para combatir los problemas de resistencias a los tratamientos, estima.

Podría representar "el avance terapéutico antipaludismo más importante de nuestra generación", se entusiasma el MMV. El paludismo es una enfermedad parasitaria que se puede tratar, aunque cada año más un millón de personas mueren debido a ella, en particular en África.

Contrariamente a los derivados semisintéticos de la artemisina atualmente disponible, la OZ puede ser sintetizada completamente a gran escala y a un costo más abordable para Africa. El objetivo perseguido es un tratamiento simple y corto, en una sola administración oral diaria durante un máximo de tres días.

Bosa (S. Korea)

|합성 아테미시닌 말라리아약 임상 착수 |

|  말라리아약 '아테미시닌'(artemisinin)의 완전 합성형 'OZ277'(trioxolane 7)의 임상시험이 영국서 시작됐다고 인도 제약사 |

|랜백시(Ranbaxy)가 18일 밝혔다. |

| |

|  지난 65년 처음 중국 과학자들이 쑥(sweet wormwood, Artemisia annua)에서 분리한 아테미시닌은 현재 효능이 가장 강력하면서 부작용은 |

|적은 말라리아약으로, 아시아와 아프리카에서 다제 내성 말라리아의 치료에 쓰이고 있다. |

| |

|  제네바 소재 비영리 구호단체 MMV(Medicines for Malaria Venture)의 후원으로 미국, 영국, 스위스와 호주 연구팀이 발견하고 랜백시가 작 |

|년 5월 MMV로부터 개발·판권을 인수한 OZ277은 과학전문지 '네이처' 19일자에 게재된 전임상 결과에 따르면, 합성 용이, 생산비, 약동학 및 |

|생체흡수율 면에서 기존 아테미시닌을 능가하는 것으로 나타났다. |

| |

Xinhua News (China)

新华网巴黎8月20日专电 法国报刊20日主要新闻摘要如下:     

    《费加罗报》:疟疾每年都夺走世界上,尤其是非洲和东南亚地区100万人的生命,并使5亿人,即每12个地球居民中就有一人遭受疟疾高烧的痛苦。为此,联合国和很多大型国际机构都发起了防治疟疾的斗争。

通过蚊子传染的的疟疾是一种致命疾病,其死亡率从1998年到2002年已经提高了10%。令人担忧的是传统抗虐药已经产生了抗药性,治效甚微。经过15年的共同努力,美国大学的化学家和瑞士、印度的制药厂家终于获得了一种从篙属植物提取的新型抗虐药,取名为OZ277。这种篙属植物是中国在1500多年前就认识并用来治病的。

|Vietnam News Agency |

|Anh: Bào chế loại thuốc chữa sốt rét mới |

|   20/08/2004 -- 11:39(GMT+7) |

| |Luân Đôn (TTXVN) - Tờ "Thời báo" của Anh ngày 19/8 cho biết việc thử nghiệm đối với OZ, một loại thuốc chữa sốt rét mới, được bào chế |

| |theo phương thuốc cổ truyền của Trung Quốc đã tạo ra bước đột phá lớn nhất trong quá trình điều trị căn bệnh này và OZ sẽ là loại thuốc|

| |hiệu nghiệm chưa từng có để chống lại bệnh sốt rét. |

| |Theo tờ báo trên, các cuộc thử nghiệm ở Anh cho thấy OZ không có những phản ứng phụ đáng kể nào và những thử nghiệm lâm sàng đối với |

| |bệnh nhân sẽ được bắt đầu ở châu Phi và Thái Lan vào năm 2005. Nếu thành công, thuốc OZ có thể sẽ được sử dụng rộng rãi để điều trị |

| |bệnh sốt rét trong vòng 4 năm tới. |

| |Thuốc OZ, do tổ chức chống sốt rét MMV (Medicines for Malaria Venture) và Công ty dược phẩm Ranbaxy của Ấn Độ hợp tác, bào chế dựa theo|

| |tác dụng chống sốt rét của thuốc nam atêmixinin - thuốc chiết xuất từ ngải đắng trong y học cổ truyền Trung Quốc. |

| |Tuy nhiên, OZ là một loại thuốc hoàn toàn nhân tạo và do đó có thể được sản xuất đại trà với giá rẻ hơn nhiều so với phương pháp chiết |

| |xuất atêmixinin từ thiên nhiên. OZ có thời hạn sử dụng dài hơn so với atêmixinin và có tác dụng điều trị tốt hơn./. |

Rzeczpospolita (Poland)

Pokonamy malarię

Jest nadzieja dla 300 milionów osób cierpiących na malarię - opracowano syntetyczny, dobrze tolerowany przez organizm ludzki lek, walczący z pasożytami powodującymi tę chorobę. Udało się to, czego na próżno od piętnastu lat usiłowali dokonać naukowcy z wielu krajów.

Testy kliniczne nowego leku już rozpoczęły się w Wielkiej Brytanii. Substancja uzyskana syntetycznie otrzymała nazwę OZ 277. Osiągnięcie to jest dziełem międzynarodowego zespołu naukowców z Centrum Medycznego Uniwersytetu Stanowego Nebraski, australijskiego Uniwersytetu Monash, Szwajcarskiego Instytutu Tropikalnego oraz laboratorium szwajcarskiej firmy farmaceutycznej Hoffman Roche. Wiadomość o sukcesie publikuje brytyjski tygodnik naukowy "Nature".

Przygotowania do użycia substancji na szerszą skalę prowadzi indyjska firma farmaceutyczna Ranbaxy - partner Medicines for Malaria Venture, organizacji non profit zajmującej się poszukiwaniem nowych niedrogich środków przeciw malarii. MMV ułatwia współpracę na tym polu między instytucjami publicznymi i prywatnymi.

Malaria - obok AIDS i gruźlicy - uznawana jest przez Światową Organizację Zdrowia (WHO) za najniebezpieczniejszą chorobę zakaźną na świecie. Szacuje się, że na zimnicę choruje dziś 300 mln ludzi (niektóre dane mówią o 500 mln). Z jej powodu umiera każdego roku 1 - 1,5 mln chorych, w tym 800 tys. dzieci.

Sprawdzona

Uzyskana syntetycznie substancja jest podobna do naturalnie występującej artemisyny. Artemisynę zawiera doskonale znana w lecznictwie roślina, tzw. bylica jednoroczna (Artemisia annua), krewna piołunu. Roślinę tę chińska medycyna stosuje w leczeniu malarii już od 1500 lat. W walce z tą chorobą wykorzystuje się też pochodne artemisyny - artemeter i artesunian. Jednak w rejonach, gdzie występuje najwięcej zachorowań na malarię, produkcja i przechowywanie leków pochodzenia naturalnego jest niezwykle trudne. Do tego ich wytwarzanie jest dość kosztowne. I tu przychodzi z pomocą chemia.

- Przetestowaliśmy różne dawki u ponad tuzina ochotników i rezultaty są bardzo zachęcające - powiedziała Lise Riopel z MMV. Podobnie jak naturalna artemisyna nowy preparat zabija zarodźce, wchodząc w reakcję z żelazem i produkując wolne rodniki. - Wolne rodniki atakują zaś białka i enzymy, które są kluczowe dla życia pasożytów - tłumaczy Jonathan Vennerstrom z Uniwersytetu Stanowego Nebraski, jeden z twórców preparatu. - Można powiedzieć, że to lekarstwo jest swego rodzaju koniem trojańskim - powiedział magazynowi "New Scientist" Paul O'Neill, ekspert w dziedzinie walki z malarią na Uniwersytecie Liverpool.

Tania

W wielu regionach kuli ziemskiej pasożyty wywołujące malarię, roznoszone przez komary, zdążyły się uodpornić na leki używane od wielu lat - przede wszystkim chininę i chlorochinę. Dlatego Światowa Organizacja Zdrowia zalecała krajom, w których występuje zjawisko uodpornienia malarycznych pasożytów przeciw konwencjonalnym lekom, stosowanie substancji pochodnych od artemisyny. Dotychczasowe badania wskazują, że pasożyty nie uodporniły się na artemisynę - prawdopodobnie dlatego, że atakuje ona kilka białek jednocześnie.

Niestety, mimo że jedna dawka dla osoby dorosłej kosztuje dwa dolary, jest to i tak zbyt wiele dla krajów zacofanych; dla porównania, jedna porcja tradycyjnej chininy kosztuje od dziesięciu do dwudziestu razy mniej. Właśnie na takim poziomie będzie się kształtować cena leku nowej generacji.

Dlatego naukowcy tak intensywnie prowadzili prace zmierzające do syntetycznego, czyli taniego, uzyskiwania artemisyny (ACT). W przeciwieństwie do aktualnie dostępnych półsyntetycznych pochodnych artemisyny nowa cząsteczka OZ 277 może być uzyskiwana w sposób całkowicie syntetyczny, na skalą przemysłową, bez korzystania z drogich wyciągów roślinnych.

Skuteczna

Celem międzynarodowego zespołu było uzyskanie substancji umożliwiającej leczenie tanie i szybkie. Zakładano, że musi to być lek podawany zwyczajnie, doustnie, raz dziennie. Przeprowadzone wstępne testy kliniczne wskazują, że cel został osiągnięty. Wystarczy kuracja trwająca jedynie trzy dni, aby całkowicie wyleczyć malarię.

Nowa substancja działa silniej i dłużej "in vivo" niż artemeter czy artesunian. Testy przeprowadzone w Wielkiej Brytanii wykazały, że OZ 277 nie powoduje skutków ubocznych. Kolejna tura testów, na większej grupie chorych, rozpocznie się w styczniu 2005 roku.

- Jeżeli i tym razem zakończą się one sukcesem - podkreśla Paul O'Neill - substancja ta wreszcie może stać się skuteczną, powszechnie dostępną bronią przeciw uodpornionym na medykamenty pasożytom wywołującym malarię. Być może otrzymujemy do ręki najbardziej skuteczną terapię antymalaryczną w naszym pokoleniu. - Nowy tani lek syntetyczny może okazać się przełomem w walce z malarią - wtóruje mu Lisa Riopel.

KRZYSZTOF KOWALSKI, PIOTR KOŚCIELNIAK

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Plivazdravlje (Hungary)

Novi sintetički lijek protiv malarije

Međunarodna skupina nanstvenika je razvila sintetički lijek koji može ponuditi novu nadu u borbi protiv malarije.

Malarija je postala velika prijetnja nakon što su njeni prijenosnici komarci razvili imunitet na lijekove kojima se bolest suzbijala.

U područjima svijeta gdje ima malarije živi gotovo 2 milijarde ljudi.

Novi je lijek baziran na kemikaliji pronađenoj u tradicionalnoj kineskoj biljnoj medicini.

Znanstvenici su se dugo zanimali za biljni lijek koji se dobiva od kore slatkog pelina, a za koji se pokazalo da pomaže u ubijanju parazita malarije.

Prirodni lijek je skupo proizvesti i zahtijeva komplicirane programe liječenja.

Međunarodni tim znanstvenika iz SAD-a, Britanije, Švicarske i Australije je razvio sintetički lijek nazvan OZ277, s djelovanjem sličnim onom kod biljnog lijeka, no jeftinijeg za proizvodnju i učinkovitijeg.

Prije nego što OZ277 postane komercijalni lijek bit će potrebno dodatno ga ispitati, dodaju znanstvenici.

Otkriven sintetički lijek protiv malarije

četvrtak, 19.8.2004 04:44

[pic]ZNANSTVENICI su otkrili sintetički lijek koji može ponuditi novu nadu u borbi protiv malarije, bolesti koja je postala velika prijetnja nakon što su njeni prijenosnici komarci razvili imunitet na lijekove kojima se bolest suzbijala.

U područjima svijeta gdje ima malarije živi gotovo dvije milijarde ljudi. Novi je lijek baziran na kemikaliji pronađenoj u tradicionalnoj kineskoj biljnoj medicini.

Znanstvenici su se dugo zanimali za Artemisinin, biljni lijek koji se dobiva od kore slatkog pelina, a za koji se pokazalo da pomaže u ubijanju parazita malarije.

Prirodni lijek je skupo proizvesti i zahtijeva komplicirane programe liječenja. Međunarodni tim znanstvenika iz SAD-a, Britanije, Švicarske i Australije ustvrdio je u istraživanju objavljenom u britanskom naučnom časopisu "Nautre" da je razvio sintetički lijek "OZ277", s dobrobiti Artemisinina, jeftiniji za proizvodnju i učinkovitiji.

Prije nego što "OZ277" postane komercijalni lijek bit će potrebno dodatno ga ispitati. No, u pratećem članku Paul ONeill s Kemijskog i farmakološkog odsjeka Sveučilišta u Liverpoolu kaže da novi spoj moće ponuditi najbolje rješenje za uništenje prijenosnika malarije imunih na postojeće lijekove.

RTS Vesti (Radio-Television Serbia)

NOVI LEK PROTIV MALARIJE

NAUKA - Četvrtak, Avgust 19, 2004 12:46  RTS

Grupa američkih, australijskih i švajcarskih istraživača nada se da je sintetizovala novu vrstu leka protiv malarije koji ljudi dobro podnose, što bi najzad omogućilo efikasnu borbu protiv te bolesti koja u Africi svakih 30 sekundi ubije po jedno dete.

U pitanju je molekul nazvan OZ 277. Sintetizovan je po uzoru na jedan sastojak kineske biljke artemizine, objavila je britanska naučna revija 'Nejčer', zajedno sa rezultatima istraživanja stručnjaka iz Nebraske [SAD], Monaša [Australije], Švajcarskog instituta za tropske bolesti i farmakološke firme Hofman Roš.

Lek se trenutno se proizvodi u neprofitnoj organizaciji MMV [Medicine for Malaria Venture], koja radi na pronalaženju novih jeftinih lekova protiv malarije, uz pomoć indijske farmaceutske kuće Ranbaksi.

Testiranje podnošenja i neštetnosti novog leka obavlja se u Velikoj Britaniji. Ispitivanje na obolelima počeće u januaru 2005. godine i naučnici se nadaju da će to biti do sada najefikasniji lek protiv malarije, koja je izlečiva bolest - ali od nje godišnje umre više od milion ljudi.

Do sada su dobijani polusintetički lekovi od biljke artemizine, a prednost OZ 277 je što može da se sintetiše u potpunosti. Cena njegove prozivodnje je toliko niska da je dostupna i afričkim državama. Lek se uzima se oralno, jednom dnevno, najviše tri dana.

   

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