Products
Abemaciclib was approved in the form of film-coated tablets in the United States in 2017, in the EU in 2018, and in many countries in 2019 (Verzenios).
Structure and properties
Abemaciclib (C27H32F2N8, Mr = 506.6 g/mol) exists as a white to yellow powder.
Effects
Abemaciclib (ATC L01XE50) has antitumor and antiproliferative properties. The effects are due to potent and selective inhibition of cyclin-dependent kinases (CDK) 4 and 6. Abemaciclib blocks the cell cycle transition from G1 to S phase of cell division. This leads to apoptosis of cancer cells and inhibits cancer cell proliferation. The median half-life is 24.8 hours.
Indications
For the treatment of postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor-2 (HER2)-negative locally advanced or metastatic breast cancer:
- In combination with an aromatase inhibitor as initial endocrine therapy.
- In combination with fulvestrant in women, after prior endocrine therapy.
- As monotherapy after disease progression following endocrine therapy and one or two chemotherapy regimens for metastatic disease when chemotherapy is not appropriate.
In pre- or perimenopausal women, endocrine therapy should be combined with an LHRH agonist.
Dosage
According to the SmPC. Tablets are taken twice daily, independent of meals. Combination with grapefruit juice is not recommended.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Abemaciclib is metabolized by CYP3A4 and appropriate drug-drug interactions must be considered.
Adverse effects
The most common potential adverse effects include diarrhea, infection, neutropenia, anemia, fatigue, nausea, vomiting, and decreased appetite.
