Verzenios ® (abemaciklib)
Abemaciclib is an inhibitor of CDK 4 and CDK 6 and was most active against cyclin D1/CDK 4 in enzymatic assays. In breast cancer, cyclin D1/CDK 4 has been shown to promote phosphorylation of the Rb, cell proliferation, and tumor growth. Abemaciclib prevents Rb phosphorylation, blocking progression from G1 into S phase of the cell cycle, leading to suppression of tumor growth in preclinical models following short duration target inhibition. In ER+ breast cancer cell lines, sustained target inhibition by abemaciclib prevents rebound of Rb phosphorylation and cell cycle reentry, resulting in senescence and apoptosis. In breast cancer xenograft models, abemaciclib dosed daily without interruption at clinically relevant concentrations, as a single agent or in combination with antiestrogens, resulted in reduction of tumor size.1
CDK = cyclin-dependent kinase
ER+ = estrogen receptor-positive
Rb = retinoblastoma protein
▼ This medicinal product is subject to additional monitoring. This will allow quick identification of new safety information. Healthcare professionals are asked to report any suspected adverse reactions.
Datum fӧr senaste ӧversyn 2020 M01 21