Abemaciclib (2 brand names, 1 dosage form, 1 route)
Available dosage forms: TABLET.
Routes of administration: ORAL.
Brand Names
- ABEMACICLIB
- VERZENIO
Contraindications
None.
Adverse Reactions
The following adverse reactions are discussed in greater detail in other sections of the labeling: Diarrhea [see Warnings and Precautions (5.1)]. Neutropenia [see Warnings and Precautions (5.2)]. Interstitial Lung Disease (ILD) or Pneumonitis [see Warnings and Precautions (5.3)]. Hepatotoxicity [see Warnings and Precautions (5.4)]. Venous Thromboembolism [see Warnings and Precautions (5.5)].
Mechanism of Action
Abemaciclib is an inhibitor of cyclin-dependent kinases 4 and 6 (CDK4 and CDK6). These kinases are activated upon binding to D-cyclins. In estrogen receptor-positive (ER+) breast cancer cell lines, cyclin D1 and CDK4/6 promote phosphorylation of the retinoblastoma protein (Rb), cell cycle progression, and cell proliferation. In vitro, continuous exposure to abemaciclib inhibited Rb phosphorylation and blocked progression from G1 into S phase of the cell cycle, resulting in senescence and apoptosis. In breast cancer xenograft models, abemaciclib dosed daily without interruption as a single agent or in combination with antiestrogens resulted in reduction of tumor size.