molecules of the month


oral plasmodium eEF2 inhibitor

Ph. I candidate for malaria treatment

from phenotypic screen & optimization

The Lancet

Merck Institute for Pharmacometrics

Chemical structure of molecule M5717 Merck Institute antimalarial compound
1 min read

13.   The Merck Institute antimalarial compound, M5717, is the first plasmodium eEF2 inhibitor to reach clinical development, and is a good example of an orally available dibasic compound as well as an antimalarial with a discrete target identified after traditional phenotypic screening. It was well-tolerated in healthy volunteers and has a long half-life (146-193 h at doses ≥200 mg). Single oral doses of M5717 (150 mg, 400 mg, or 800 mg) resulted in clearance of asexual blood-stage parasites. The molecule may be a valuable component of single-dose antimalarial combination therapy or malaria prophylaxis in the future.

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