Verzenio ® (abemaciclib) tablets

50mg, 100mg, 150mg, 200mg

This information is provided in response to your request. Resources may contain information about doses, uses, formulations and populations different from product labeling. See Prescribing Information above, if applicable.

How does the mechanism of action of VERZENIO® (abemaciclib) compare to other CDK 4 & 6 inhibitors?

Verzenio® (abemaciclib) has not been studied in head to head clinical trials with other CDK4 & 6 inhibitors.

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Indication

Abemaciclib is indicated

  • in combination with endocrine therapy (ET) (tamoxifen or an aromatase inhibitor [AI]) for the adjuvant treatment of adult patients with hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-), node-positive early breast cancer at high risk of recurrence and a Ki-67 score ≥20% as determined by an FDA approved test
  • in combination with an AI as initial endocrine-based therapy for the treatment of postmenopausal women, and men, with HR+, HER2- advanced or metastatic breast cancer (MBC)
  • in combination with fulvestrant for the treatment of adult patients with HR+, HER2- advanced or MBC with disease progression following ET 
  • as monotherapy for the treatment of adult patients with HR+, HER2- advanced or MBC with disease progression following ET and prior chemotherapy in the metastatic setting.1

Mechanism of Action and Other CDK 4 and 6 Inhibitors

Abemaciclib is an inhibitor of cyclin-dependent kinase (CDK) 4 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.1

For information on other CDK 4 and 6 inhibitors in this class, please contact the individual manufacturers of these drugs.

Reference

1Verzenio [package insert]. Indianapolis, IN: Eli Lilly and Company; 2021.

Date of Last Review: January 21, 2020


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