abemaciclib + vepdegestrant

Abemaciclib + vepdegestrant is an investigational oral combination therapy being evaluated for the treatment of locally advanced or metastatic estrogen receptor positive (ER+)/human epidermal growth factor receptor 2 negative (HER2-) breast cancer, particularly in patients previously treated with a CDK4/6 inhibitor. Abemaciclib is a small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which blocks cell cycle progression in cancer cells. Vepdegestrant is an orally bioavailable PROteolysis Targeting Chimera (PROTAC) protein degrader that targets the estrogen receptor for degradation, thereby inhibiting ER-driven tumor growth. The combination has shown encouraging clinical activity and a tolerable safety profile consistent with each agent alone, with no significant drug-drug interactions observed between the two agents[1][3][5]. The recommended Phase 2 dose is abemaciclib 150 mg twice daily plus vepdegestrant 200 mg once daily[1][5]. This regimen is currently under investigation in Phase 2 clinical trials for post-CDK4/6 advanced breast cancer.

Brand names

Verzenio

Other names

vepdegestrant + abemaciclib