molecules of the month


oral blood stage antimalarial

in Ph. I (healthy volunteers)

from 1.5M cmpd phenotypic screen + opt.

J. Med. Chem.

Novartis (NIBR), Emeryville, CA

oral blood stage antimalarial - Novartis (NIBR), Emeryville, CA
4 mins read

Context. INE963 (Novartis Institute for Tropical Diseases) is an oral, single dose, fast-acting blood-stage antimalarial candidate. The molecule was identified using a phenotypic high-throughput screening approach which has been successfully used to identify new antimalarial chemotypes. Phenotypic screens can be preferable to target-based screens in antimalarial drug discovery because the emergence of antimalarial drug resistance to current front-line compounds means identification of first-in-class molecules is imperative. Although a mechanism of action has yet to be identified for the molecule, its activity against multidrug-resistant P. falciparum cell lines and demonstration of high barrier to resistance are suggestive of a first-in-class molecule. Reviewer Comments. Three attributes set INE963 apart from existing antimalarials according to nominator and reviewer Dennis Koester: its ability to…

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