GSK2556286

GSK2556286 is an orally active small molecule antitubercular agent developed for the treatment of tuberculosis (TB), including multidrug-resistant (MDR), extensively drug-resistant (XDR), and drug-sensitive (DS) Mycobacterium tuberculosis. It was identified through high-throughput screening for compounds that inhibit intracellular growth of M. tuberculosis in human macrophages, with an IC50 of 0.07 μM[1][2][3][4]. The compound exhibits a novel cholesterol-dependent mechanism of action and has been shown to act as an agonist of mycobacterial Rv1625c, a membrane-bound adenylyl cyclase[5]. Preclinical studies demonstrate efficacy in mouse models and good penetration into granulomas, suggesting potential to shorten TB treatment duration when used in combination regimens[2][8]. GSK2556286 does not show cross-resistance with existing antitubercular drugs and has demonstrated an adequate safety profile in preclinical species[2][3]. Developer: GSK.

Other names

GSK286GSK-286GSK 286