ODM-207

ODM-207 is an orally bioavailable small molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins. It acts as a potent and selective pan-BET inhibitor with minimal cross-reactivity to non-BET bromodomains. By binding to acetylated lysine recognition motifs in BET protein bromodomains (including BRD2, BRD3, BRD4, and BRDT), ODM-207 disrupts the interaction between BET proteins and acetylated histones. This leads to altered chromatin remodeling and suppression of oncogenic gene expression critical for tumor cell proliferation and survival. Preclinical studies have shown antiproliferative effects in various cancer models including breast cancer, leukemia, prostate cancer xenografts, and other solid tumors. In a first-in-human Phase 1 trial in patients with advanced malignancies (including castrate-resistant prostate cancer), ODM-207 demonstrated dose-dependent pharmacokinetics but had a narrow therapeutic window due to cumulative toxicity such as thrombocytopenia and fatigue[2][4][5][6][8].

Other names

odm207odm-207odm 207