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GSK932121

Development stage: Discontinued
Lead developer: GSK
Modality: Small Molecules
Administration: Oral

Overview

GSK932121 is a small molecule antimalarial drug candidate developed by GSK (GlaxoSmithKline) and Medicines for Malaria Venture. It belongs to the 4(1H)-pyridone chemical class and acts as an inhibitor of the electron transport chain in *Plasmodium falciparum* by binding to the Qi site of cytochrome bc1 (complex III). This mechanism allows it to overcome atovaquone resistance in malaria parasites. Despite its potent antimalarial activity both *in vitro* and *in vivo*, development was halted after phase I clinical trials due to cardiotoxicity concerns[4][6][7][8].

Targets

bc1 complex (Cytochrome bc1 complex (plasmodium))CYTB (Plasmodium falciparum cytochrome bc1 complex (qi site))

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