Abemaciclib (Verzenio)

Mechanism of action

From NCI Drug Dictionary: An orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. Abemaciclib specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation in early G1.

Diseases for which it is used

• Breast cancer, ER-positive

History of changes in FDA indication

• 9/28/2017: FDA approved in combination with fulvestrant for women with HR-positive, HER2-negative advanced or metastatic breast cancer with disease progression following endocrine therapy. (Based on MONARCH 2)
• 9/28/2017: FDA approved as monotherapy for women and men with HR-positive, HER2-negative advanced or metastatic breast cancer with disease progression following endocrine therapy and prior chemotherapy in the metastatic setting. (Based on MONARCH 1)
• 2/26/2018: FDA approved in combination with an aromatase inhibitor as initial endocrine-based therapy for postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer. (Based on MONARCH 3)
• 10/12/2021: Approved with endocrine therapy (tamoxifen or an aromatase inhibitor) for adjuvant treatment of adult patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, node-positive, early breast cancer at high risk of recurrence and a Ki-67 score ≥20%, as determined by an FDA approved test. (Based on monarchE)

History of changes in EMA indication

• 9/26/2018: Initial authorization

Manufacturer Package Insert

• Abemaciclib (Verzenio) Package Insert

Also known as

• Code name: LY2835219
• Brand names: Verzenio, Verzenios