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 New malaria drug could be a life-saver as the standard drug shows signs of weakness

At the turn of the millennium, a new class of drugs derived from ancient Chinese herbal medicine revolutionized malaria care. Artemisinin's, as they're called, are based on extracts from the sweet wormwood plant. They arrived just as the drugs used since the 1970s were becoming useless for many, as the parasite that causes malaria evolved resistance.

 What's going on with the 'magic' drug for malaria?

Resistance to artemisinin has been seen before. And it makes sense: Diseases evolve to evade drugs. In the past couple years, studies in East Africa have shown partial resistance to artemisinin in children with uncomplicated malaria. Plus, "this is quite similar to what has happened in Southeast Asia, where there has been clinical resistance to [artemisinin]," says Haldar.

Articles of Interest

Artemisinin resistance and malaria elimination: Where are we now?

The emergence of artemisinin resistance is a major obstacle to the global malaria eradication/elimination programs. Artemisinin is a very fast-acting antimalarial drug and is the most important drug in the treatment of severe and uncomplicated malaria. For the treatment of acute uncomplicated falciparum malaria, artemisinin derivatives are combined with long half-life partner drugs and widely used as artemisinin-based combination therapies (ACTs).

The Role of Artemisinin in Combating Malaria: A Global Health Perspective

The World Health Organization (WHO) recommends Artemisinin-based Combination Therapies (ACTs) as the standard first-line treatment for uncomplicated Plasmodium falciparum malaria. ACTs combine an artemisinin derivative with a partner drug, offering a synergistic approach that enhances efficacy and helps to prevent the development of drug resistance. This strategy has been instrumental in reducing the global malaria burden over the past two decades. The widespread availability and use of Artemisinin have significantly contributed to the decrease in malaria cases and deaths worldwide. However, the emergence of artemisinin resistance in some regions poses a serious threat to these gains. Parasites that are partially resistant to artemisinin may clear more slowly, potentially impacting the effectiveness of combination therapies and requiring continuous monitoring and strategic responses from global health organizations and pharmaceutical suppliers

This Chemical Trick Could Turn Losing Malaria Drug Into a Winner

Artefenomel, a newer artemisinin-inspired variant, was intended to replace ACTs in time to stanch the spread of artemisinin resistance. It was potent enough that scientists hoped it could cure malaria in a single dose. This would have been an improvement over ACTs, which must be taken for three days in a row to be effective.

Triple artemisinin-based combination therapy (TACT): advancing malaria control and eradication efforts

Triple artemisinin-based combination therapy (TACT) emerged as a novel approach to combat resistance to ACT. TACT merges an established artemisinin-based combination therapy with a long-lasting partner medication to combat resistance

Anti-malarial drug: the emerging role of artemisinin and its derivatives in liver disease treatment

Artemisinin and its derivatives belong to a family of drugs approved for the treatment of malaria with known clinical safety and efficacy. In addition to its anti-malarial effect, artemisinin displays anti-viral, anti-inflammatory, and anti-cancer effects in vivo and in vitro. Recently, much attention has been paid to the therapeutic role of artemisinin in liver diseases.

Artemisinin kills malaria parasites by damaging proteins and inhibiting the proteasome

Artemisinin kills malaria parasites by damaging proteins and inhibiting the proteasome

Artemisinin, the Magic Drug Discovered from Traditional Chinese Medicine

Artemisinin and its derivatives represent the most important and influential class of drugs in the fight against malaria. Since the discovery of artemisinin in the early 1970s, the global community has made great strides in characterizing and understanding this remarkable phytochemical and its unique chemical and pharmacological properties. Today, even as artemisinin continues to serve as the foundation for antimalarial therapy, numerous challenges have surfaced in the continued application and development of this family of drugs.

Artemisinin: a game-changer in malaria treatment

There are various stages in the lifecycle of the malaria parasite. Artemisinin mainly targets the malaria parasite during its asexual blood ring stage, disrupting the parasite’s ability to replicate within red blood cells. Once the drug is administered, its rapid dual action, reducing the parasite burden and also the fever, quickly make artemisinin-based therapies highly effective within the first few days of treatment. As artemisinin does not remain active in the body for a long time, it is not used for malaria prevention, as it would need to be administered regularly over an extended period. Artemisinin is not able to stop the relapse of Plasmodium vivax, as it does not affect the form of the parasite that lies dormant in the liver and that can reactivate causing a new episode of malaria.

Artemisinin: A Revolutionary Antimalarial Agent

The treatment of malaria has significantly improved with the groundbreaking antimalarial drug artemisinin, which is derived from Artemisia annua. It was found in the 1970s and damages Plasmodium parasites by producing reactive oxygen species. Because of its quick action and effectiveness against drug-resistant strains, artemisinin-based combination treatments (ACTs) are the gold standard. However, long-term efficacy is threatened by resistance, particularly in Southeast Asia. Today, while artemisinin remains the cornerstone of antimalarial therapy, several challenges have emerged in its ongoing use and development. These include the rise of delayed treatment responses to artemisinin in malaria patients and attempts to repurpose these drugs for non-malaria applications.

Artemisinins: their growing importance in medicine

Artemisinins are derived from extracts of sweet wormwood (Artemisia annua) and are well established for the treatment of malaria, including highly drug-resistant strains. Their efficacy also extends to phylogenetically unrelated parasitic infections such as schistosomiasis. More recently, they have also shown potent and broad anticancer properties in cell lines and animal models.

Drug-resistant malaria is emerging in Africa. Doctors are worried — yet hopeful

ACTs quickly became a mainstay in malaria treatment. But in 2009, researchers observed signs of resistance to artemisinin along the Thailand-Cambodia border. The artemisinin component failed to clear the parasite quickly, which meant that the partner drug had to pick up that load, creating favorable conditions for partner drug resistance, too. The Greater Mekong Subregion now experiences high rates of multi-drug resistance. Scientists have feared that the spread of such resistance to Africa, which accounts for more than 90% of global malaria cases, would be disastrous.

Fears for spread of malaria in Africa as study finds resistance to frontline drug

Signs of resistance to artemisinin in tenth of children with severe malaria similar to situation in Asia, say researchers.

For Intrigue, Malaria Drug Gets the Prize

The Chinese drug artemisinin has been hailed as one of the greatest advances in fighting malaria, the scourge of the tropics, since the discovery of quinine centuries ago.

Old drug, new discovery: Scientists find novel use for ancient malaria remedy

The researchers found that through an entirely different mechanism, the potent antimalarial drug could partially reverse cardiac fibrosis in cells taken from patients with the condition and in lab-grown heart tissue. It also improved heart function in mice with heart failure. In fighting malaria, artesunate binds to the heme protein in red blood cells to generate reactive oxygen species, which help destroy the parasite. But with cardiac fibrosis, artesunate targets a separate molecular pathway involving myeloid differentiation factor 2 and toll-like receptor 4 to inhibit the expression of fibrotic genes.

Parasite resistance imperils our last effective malaria drug

Scientists in France have found how the genes of the malaria parasite adapt to become resistant to artemisinin, one of the most effective remaining antimalarial drugs. Their discovery exposes a serious problem. Malaria is a continuous pandemic, killing over a million people each year. Artemisinin, developed by the Chinese around the time of the Vietnam War, is very effective. But resistance is an issue as the malaria parasite adapts. This is clearly not helped by the proliferation of cheaper counterfeit drugs or ones with very little active ingredient, especially in South-east Asia, a hotbed for the disease.

Review of artemisinin derivatives: An artful approach to malaria treatment

Artemisinin derivatives share a similar mechanism of action against Plasmodium species. They interact with heme iron within the parasite, causing the breakdown of peroxide bridges within the artemisinin molecule, leading to free radical production that damages parasitic proteins. Artemisinin derivatives have the fastest parasite clearance times of any antimalarials because of their preferred place in therapy. Oral options of artemisinin derivatives are coformulated with other antimalarial medications and are available as what is known as “artemisinin-based combination therapy” (ACT). Artesunate is the only IV artemisinin derivative to treat malaria.

Scientists Hijacked Tobacco Plants to Make Malaria Drugs

Malaria is one of the modern world’s most pressing public health challenges—a disease made even trickier by how difficult it has proven to come up with and mass produce new treatments. But now, a scientific breakthrough could change this. Researchers have learned how to hack tobacco plants to manufacture the most effective anti-malarial treatment in quantities that could one day make the drug more widely available.

The discovery of artemisinin and Nobel Prize in Physiology or Medicine

The 2015 Nobel Prize in Physiology or Medicine was awarded to Professor Youyou Tu for her key contributions to the discovery of artemisinin. Artemisinin has saved millions of lives and represents one of the significant contributions of China to global health. Many scientists were involved in the previously unknown 523 Project, and the Nobel Prize given to a single person has not been without controversy.

Triple Artemisinin-Based Combination Therapies for Malaria – A New Paradigm?

Triple ACTs (TACTs), combining an artemisinin and two existing partner drugs, could be a stop-gap therapy for treating multidrug-resistant malaria until new antimalarials are available. Where resistance is not established, deployment of TACTs could delay or prevent emergence of resistance and could prolong the longevity of antimalarial compounds used in any triple-drug combination.

Was the Nobel prize for artemisinin a fatal error?

In 2015 a Nobel Price was attributed to Youyou Tu, almost 50 years after a report describing artemisinin’s structure, pharmacology, and efficacy had been published in 1979 by the “Qinghaosu Anti-Malarial Coordinating Research Group,” where she was a member of. Mr Huang Shuze, Deputy Minister of Health, stated in his 1981 summary report “Project 523 mobilized multiple departments ; thirty scientific research units and medical schools in 1975”. WHO for decades hesitated in considering this traditional medicine approach. Only at the end of the nineties, when chloroquine’s resistance became overwhelming did first clinical trials take place. But artemisinin was not water soluble, hardly bioavailable, metabolized very rapidly and gave premature signs of resistance.

Why Artemisia stems are more important than leaves for antimalarial infusions

There are many anecdotic reports indicating that including stems and twigs with dried Artemisia leaves augments the power of the infusion. Operators of a palm oil plant in Burundi only drink infusions made with stems and stay malaria free. Dried Artemisia annua herb of Chinese origin and sold in European pharmacies contains at least 70 % of stems.