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Last Updated: 09/10/21

Information below provided by the Pharmaceutical Company.

Abemaciclib (Verzenio®)

Agent Description

Abemaciclib is an orally administered, potent, and selective small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4 & 6) that is dosed on a continuous, twice daily schedule.

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.

Classification

CDK4/6 inhibitor

Molecular Targets

CDK4 and CDK6

Monograph

Abemaciclib is indicated:

  • in combination with an aromatase inhibitor as initial endocrine-based therapy for the treatment of postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer.
  • in combination with fulvestrant for the treatment of women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer with disease progression following endocrine therapy.
  • as monotherapy for the treatment of adult patients with HR-positive, HER2-negative advanced or metastatic breast cancer with disease progression following endocrine therapy and prior chemotherapy in the metastatic setting.

Package insert: https://uspl.lilly.com/verzenio/verzenio.html#pi

Studies of Interest:

Proposals of Interest:

  • Studies that advance understanding in endometrial, ovarian, or prostate cancers
  • Other indications not under current investigation by the Lilly
  • Novel abemaciclib combination treatments based on a sound molecular hypothesis
  • Translational focused proposals
  • Non-clinical concepts that examine the molecular determinants (and potential biomarkers) of response to abemaciclib in breast cancer and other malignancies

Proposals NOT of Interest:

  • Trials that compete against ongoing Lilly or Lilly-sponsored studies
  • Therapeutic combinations with ill-defined safety profile, significant overlapping toxicity, or unacceptable safety when combined (e.g. Strong/moderate CYP3A inhibitor/inducers and PD-1 inhibitors)
  • Head-to-head studies with other CDK4/6 inhibitors
  • Studies evaluating pediatric patients

Information collaborator would like included in investigator proposals

N/A