enobosarm + abemaciclib

Enobosarm + abemaciclib is an investigational combination therapy under clinical development for the treatment of advanced or metastatic breast cancer, specifically in patients with androgen receptor-positive (AR+), estrogen receptor-positive (ER+), and HER2-negative disease who have progressed after prior CDK4/6 inhibitor and endocrine therapy. Enobosarm is an oral selective androgen receptor modulator (SARM) that acts as a first-in-class agonist targeting the androgen receptor to suppress tumor growth in AR+ breast cancer without causing masculinizing side effects. Abemaciclib is a small molecule kinase inhibitor that selectively inhibits cyclin-dependent kinases 4 and 6 (CDK4/6), leading to cell cycle arrest by blocking Rb phosphorylation, thereby inhibiting proliferation of cancer cells. The combination aims to leverage both AR activation and CDK4/6 inhibition for enhanced antitumor efficacy[1][3][5][7].

Brand names

Verzenio (for abemaciclib)