GSK3186899

GSK3186899 (also known as DDD-853651 or GSK899) is a small molecule inhibitor developed for the treatment of visceral leishmaniasis. It acts by inhibiting cdc2-related kinase 12 (CRK12), an enzyme essential for the cell cycle in Leishmania parasites. Inhibition of CRK12 disrupts parasite cell division and leads to parasite death[1][6]. The drug was originally developed through a collaboration between GlaxoSmithKline (GSK), the University of Dundee Drug Discovery Unit (DDU), and Wellcome. After initial development by GSK and completion of Phase I single ascending dose studies in healthy volunteers[3], further development was taken over by Drugs for Neglected Diseases initiative (DNDi). The compound is notable for its novel mechanism targeting CRK12 and its potential as an oral therapy addressing significant unmet needs in visceral leishmaniasis treatment[6].

Other names

3,3,3-trifluoro-N-(4-((3-((2S)-2-methylmorpholin-4-yl)-1H-pyrazolo(3,4-d)pyrimidin-6-yl)amino)cyclohexyl)propane-1-sulfonamide