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Newly Developed Molecule May Lead To First Synthetic One-Dose Antimalarial

First Posted: May 29, 2017 04:10 AM EDT

A molecule that can become the first fully synthetic and one-dose treatment for malaria has been developed by researchers at LSTM in collaboration with the University of Liverpool. The molecule works against parasites showing the key genetic marker for artemisinin resistance in in vitro studies.

According to Phys.org, the international team of researchers described the molecules known as E209 as meeting the necessary points of the Medicines for Malaria Venture drug candidate profiles. Malaria control and eradication need effective treatment strategies. For many years, this step has been taken by artemisinin-based combination strategies (ACTs). This is basically the combination of artemisinin-based drugs and a drug partner with a longer half-life.

There has been an effective impact on malaria treatment with semi-synthetic artemisinin-based combination strategies; however, the search for a fully synthetic alternative has been going on for over 10 years. Furthermore, there can be a complete treatment failure due to the growing problem of resistance to current ACTs. The scenario made the research team look at alternatives that could hold on to the effectiveness against parasites with the known resistance genetic while at the same time acting fast.

"Extensive molecular investigations have demonstrated that mutations in the K13 gene are makers for artemisinin susceptibility and are linked to drug resistance in some malaria parasites,” study senior author and LSTM's Deputy Director, Professor Steve Ward, said. “These mutations allow the parasite to survive exposure to the drug during the early stages of infection in the red blood cell.”

The professor also added that E209 is a breakthrough molecule that is fully synthetic and keeps the killing efficiency of the artemisinins. The molecule also works against K13 mutant parasites, which raises the hope that it could be used as a single-dose cure. The paper was recently published in the journal Nature Communications.

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