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.

VERZENIO® (abemaciclib): Mechanism of Action

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 ET (tamoxifen or an AI) for the adjuvant treatment of adult patients with HR+, HER2-, node-positive EBC 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
  • in combination with fulvestrant for the treatment of adult patients with HR+, HER2- advanced or metastatic breast cancer with disease progression following ET 
  • as monotherapy for the treatment of adult patients with HR+, HER2- advanced or metastatic breast cancer with disease progression following ET and prior chemotherapy in the metastatic setting.1

Mechanism of Action

Abemaciclib is an inhibitor of CDK4 and CDK6. These kinases are activated upon binding to D-cyclins. In ER+ breast cancer cell lines, cyclin D1 and CDK4/6 promote phosphorylation of the 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

Reference

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

Glossary

AI = aromatase inhibitor

CDK = cyclin-dependent kinase

EBC = early breast cancer

ER+ = estrogen receptor-positive

ET = endocrine therapy

HER2- = human epidermal growth factor receptor 2-negative

HR+ = hormone receptor-positive

MBC = metastatic breast cancer

Rb = retinoblastoma protein

Date of Last Review: March 26, 2021


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