Our Exciting Journey to ACT-451840

Authors

  • Christoph Boss Idorsia Pharmaceuticals Ltd
  • Sergio Wittlin Swiss Tropical and Public Health Institute; University of Basel

DOI:

https://doi.org/10.2533/chimia.2021.916

PMID:

34798913

Keywords:

Malaria, Drug Discovery, Medicinal Chemistry, Academia-Industry Collaboration, ACT-451840

Abstract

We describe our work resulting in the selection of ACT-451840 (38) as a novel antimalarial drug with a novel mode of action. The compound was broadly characterized in vitro as well as in vivo in rat PK experiments as well as two different mouse malaria models. In the P.berghei infected mouse model cure could be achieved at oral doses of 300 mg / kg over 3 consecutive days. ACT-451840 was clinically investigated up to an experimental human malaria infection model, where therapeutic effects could be shown.

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Published

2021-11-11