Abemaciclib
Abemaciclib is indicated for the treatment of patients with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer.
- Used in combination with an aromatase inhibitor as initial endocrine-based therapy.
- Used in combination with fulvestrant in patients with disease progression following endocrine therapy.
- Used as monotherapy for patients who have previously received endocrine therapy and prior chemotherapy in the metastatic setting.
Abemaciclib is a selective and potent inhibitor of cyclin-dependent kinases 4 and 6 (CDK4 and CDK6). These kinases are activated upon binding to D-cyclins. In breast cancer cells, CDK4/6 promote phosphorylation of the retinoblastoma protein (Rb), leading to cell cycle progression and cell proliferation. Abemaciclib inhibits Rb phosphorylation and blocks progression from the G1 to the S phase of the cell cycle, leading to senescence and apoptosis (cell death).
Recommended Dose: The recommended starting dose of Abemaciclib in combination with fulvestrant or an aromatase inhibitor is 150 mg twice daily. For monotherapy, the recommended starting dose is 200 mg twice daily. It should be taken at approximately the same time each day and can be taken with or without food. Swallow tablets whole; do not chew, crush, or split before swallowing.
Common side effects include diarrhea, neutropenia (low white blood cell count), nausea, abdominal pain, infections, fatigue, vomiting, and anemia. Diarrhea is very common and should be managed at the first sign of loose stools with antidiarrheal agents and increased fluid intake.
Patients should be monitored for signs of infection, thrombosis (blood clots), and liver function (ALT/AST levels). It is not recommended during pregnancy as it may cause fetal harm. Avoid concurrent use of strong CYP3A inhibitors (e.g., Ketoconazole) as they can increase Abemaciclib exposure.
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