Abemaciclib

Abemaciclib is an oral, small-molecule, selective inhibitor of cyclin-dependent kinases (CDK) 4 and 6. By blocking CDK4/6 activity, it prevents cell cycle progression from G1 to S phase, thereby inhibiting cancer cell proliferation.

Indications

Hormone receptor (HR)-positive, HER2-negative advanced or metastatic breast cancer: -In combination with an aromatase inhibitor or fulvestrant in postmenopausal women or in men. - As monotherapy after disease progression following endocrine therapy and chemotherapy.

Dosage

- 150 mg orally twice daily in combination therapy. - 200 mg orally twice daily for monotherapy.

Contra-Indications

- Known hypersensitivity to abemaciclib - Severe hepatic impairment.

Special Precautions

- Safety and efficacy not established in patients <18 years.

Side Effects

Diarrhea, neutropenia, nausea, fatigue, abdominal pain, infection, Anemia, thrombocytopenia, decreased appetite, vomiting, elevated liver enzymes, blood clots, Pulmonary embolism, ILD/pneumonitis, hepatotoxicity.

Drug Interactions

CYP3A inhibitors (e.g., ketoconazole) , CYP3A inducers (e.g., rifampicin, carbamazepine) ,Avoid concomitant use with strong CYP3A modulators,May increase exposure of drugs transported by BCRP or P-gp (e.g., digoxin).