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It is indicated for:
• In combination with endocrine therapy (tamoxifen or an aromatase inhibitor) for the 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.
• In combination with an aromatase inhibitor as initial endocrinebased therapy for the treatment of postmenopausal women, and men, 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 adult patients 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 HRpositive, HER2-negative advanced or metastatic breast cancer with disease progression following endocrine therapy and prior chemotherapy in the metastatic setting.
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.
It taken with or without food
The recommended dose is 150 mg taken orally twice daily.
The recommended dose is 150 mg taken orally twice daily.
The metabolism of Abemaciclib can be increased when combined with Aminoglutethimide. The metabolism of Abemaciclib can be decreased when combined with Amiodarone. The metabolism of Abemaciclib can be increased when combined with Amobarbital. The metabolism of Abemaciclib can be decreased when combined with Amprenavir.
None.
Based on findings in animals and its mechanism of action, it can cause fetal harm when administered to a pregnant woman . There are no available human data informing the drug-associated risk.
There are no data on the presence of abemaciclib in human milk, or its effects on the breastfed child or on milk production. Because of the potential for serious adverse reactions in breastfed infants from AbemaciclibAbemaciclib, advise lactating women not to breastfeed during Abemaciclibtreatment and for 3 weeks after the last dose.
Store at 20°C to 25°C