LGB321

LGB321 is an orally available, potent, and selective small molecule pan-PIM kinase inhibitor developed by Novartis. It acts as an ATP-competitive inhibitor of all three PIM family kinases—PIM1, PIM2, and PIM3—demonstrating activity in PIM2-dependent cell lines and effectively inhibiting proliferation in hematologic malignancies, including multiple myeloma, acute myeloid leukemia, chronic myeloid leukemia, non-Hodgkin lymphoma, and chronic lymphocytic leukemia. Mechanistically, LGB321 blocks pathways such as mTOR-C1 and inhibits phosphorylation of BAD, thereby promoting apoptosis and disrupting survival pathways relevant to hematological cancer cell biology. In preclinical models, LGB321 showed therapeutic activity and synergy with other agents (e.g., ibrutinib, cytarabine), but its development was discontinued in the preclinical stage for hematologic malignancies.

Other names

LGB321LGB-321LGB 321LGB-321 dihydrochlorideLGB321 dihydrochlorideLGB 321 dihydrochloride