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 cyclin dependent kinases 4 and 6 (CDK4 and CDK6) and with continuous exposure resulted in senescence and apoptosis.

Indication

Abemaciclib is indicated

  • in combination with an aromatase inhibitor as initial endocrine-based therapy for the treatment of postmenopausal women with HR+, HER2- advanced or MBC

  • in combination with fulvestrant for the treatment of women 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 regimens 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

Enclosed Prescribing Information

VERZENIO® (abemaciclib) tablets, for oral use, Lilly

Reference

1. Verzenio [package insert]. Indianapolis, IN: Eli Lilly and Company; 2018.

Glossary

CDK = cyclin-dependent kinase

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: October 11, 2018

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