GlaxoSmithKline, TB Drug Accelerator, Bill & Melinda Gates Foundation
GSK 2556286
Chemical Class:
Name of Target:
Cholesterol catabolism of intracellular M. tuberculosis

GSK 2556286 (GSK-286) is a new chemical entity with a novel mechanism of action related to cholesterol catabolism.  GSK-286 selectively kills intracellular Mtb:  MIC H37Rv > 10 uM, intramacrophage activity is < 0.1 uM.  It penetrates into necrotic lesions (MALDI) and reduces inflammation (PET/CT of infected marmosets).  It has been shown to be active in vivo across species (mice, rabbits, monkeys) and reduces relapse rates in mice.  It was selected as a clinical candidate in July 2017.  First in human study anticipated 2Q2019.