GSK3117391

GSK3117391 is an investigational small molecule drug developed as a selective histone deacetylase (HDAC) inhibitor using Esterase Sensitive Motif (ESM) technology. This design enables the drug to be selectively activated in myeloid lineage cells, such as monocytes, macrophages, and dendritic cells, by intracellular hydrolysis via human carboxyesterase 1 (hCE-1). The resulting active acid metabolite, GSK3339189, accumulates in these target cells. This targeted approach aims to reduce non-myeloid-related side effects and expand the therapeutic window for chronic inflammatory diseases. The primary indication investigated was rheumatoid arthritis; however, clinical development has been discontinued after reaching Phase 2 trials[5][2][3].

Other names

CKA3P0O1VICKA-3P0O1VICKA 3P0O1VIUNII-CKA3P0O1VIUNII-CKA-3P0O1VIUNII-CKA 3P0O1VIcyclopentyl (2S)-2-cyclohexyl-2-[[6-[3-(hydroxyamino)-3-oxopropyl]pyridin-3-yl]methylamino]acetate