PIM447

PIM447 (also known as LGH447) is an orally available small molecule inhibitor that targets all three isoforms of the serine/threonine kinases PIM1, PIM2, and PIM3 with high potency. It acts as a pan-PIM kinase inhibitor and has demonstrated antitumor activity in preclinical models and early clinical trials for hematological malignancies such as multiple myeloma. The drug works by binding to and inhibiting the activities of these kinases, leading to cell cycle arrest at the G1/S phase transition, induction of apoptosis through upregulation of pro-apoptotic proteins like Bcl2, downregulation of c-MYC levels, inhibition of mTORC1 signaling via TSC2 modulation, and disruption of bone disease associated with myeloma. Developed by Novartis for oral administration in relapsed/refractory multiple myeloma patients, it has shown synergy with standard treatments such as bortezomib + dexamethasone or lenalidomide + dexamethasone[1][4][6][7][8].

Other names

1210608-43-7N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)-3-pyridinyl)-6-(2,6-difluorophenyl)-5-fluoro-2-pyridinecarboxamide