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.

What is the mechanism of action of VERZENIO® (abemaciclib)?

Verzenio (abemaciclib) is an inhibitor of CDK4 and CDK6 and with continuous exposure resulted in senescence and apoptosis.

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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 a Food and Drug Administration (FDA) approved test,
  • in combination with an AI inhibitor 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, and
  • 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

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 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

Related Video

An animation of the mechanism of action of abemaciclib is available here: Abemaciclib Mechanism of Action.

Reference

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

Date of Last Review: March 22, 2022


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