molecules of the month

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…