abemaciclib + aromatase inhibitor

Abemaciclib is an orally administered, potent, and selective small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). It is used in combination with an aromatase inhibitor (such as anastrozole, exemestane, or letrozole) for the treatment of hormone receptor-positive (HR+), HER2-negative advanced or metastatic breast cancer. The combination works by blocking CDK4/6-mediated phosphorylation of the retinoblastoma protein, thereby inhibiting cell cycle progression from G1 to S phase and reducing tumor cell proliferation. Aromatase inhibitors reduce estrogen production by inhibiting the enzyme aromatase, further suppressing hormone-driven tumor growth. This dual approach targets both cell cycle regulation and hormonal stimulation in HR+ breast cancer[1][2][3][5][6].

Brand names

VerzenioFemaraArimidex

Other names

abemaciclib + letrozoleabemaciclib + anastrozoleabemaciclib plus aromatase inhibitorsLY2835219 + aromatase inhibitors