BAY1436032

BAY1436032 is an orally available small-molecule inhibitor that targets mutant forms of the metabolic enzyme isocitrate dehydrogenase type 1 (IDH1), specifically those with mutations at arginine 132 (such as IDH1R132H, IDH1R132C, IDH1R132G, IDH1R132L, and IDH1R132S)[1][5][6]. By inhibiting these mutant enzymes, BAY1436032 blocks the production of the oncometabolite (R)-2-hydroxyglutarate (R-2HG), which is implicated in leukemogenesis. The drug induces myeloid differentiation and reduces proliferation in acute myeloid leukemia (AML) cells harboring these mutations[5][6][8]. Preclinical studies have shown efficacy in clearing leukemic blasts and prolonging survival in mouse models. Clinical trials have evaluated its safety and efficacy primarily in patients with advanced AML carrying mIDH1 mutations[4], as well as advanced solid tumors with similar mutations[7]. The developer of this compound is Bayer.

Other names

RNMAUIMMNAHKQR-QFBILLFUSA-N1803274-65-8