Products
Palbociclib was approved in capsule form in the United States in 2015, in the EU in 2016, and in many countries in 2017 (Ibrance).
Structure and properties
Palbociclib (C24H29N7O2, Mr = 447.5 g/mol) is a pyridopyrimidine and exists as a yellow to orange powder.
Effects
Palbociclib (ATC L01XE33) has antitumor and antiproliferative properties. The effects are due to selective and reversible inhibition of cyclin-dependent kinases (CDK) 4 and 6, enzymes involved in the cell cycle, cell proliferation, DNA replication, and cell growth. Palbociclib inhibits the transition from G1 to S phase of the cell cycle. It has a long half-life of approximately 29 hours.
Indications
For the treatment of hormone receptor-positive and HER2-negative advanced or metastatic breast cancer in combination with fulvestrant in endocrine-pretreated pre/peri- (combined with LHRH analogs) or postmenopausal women.
Dosage
According to the SmPC. Capsules are taken once daily with food (therapy cycle of 21 days, 7 days off).
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Palbociclib is predominantly biotransformed by CYP3A and SULT2A1, and corresponding drug-drug interactions are possible.
Adverse effects
The most common potential adverse effects include neutropenia, leukopenia, infection, fatigue, nausea, anemia, stomatitis, thrombocytopenia, diarrhea, hair loss, vomiting, decreased appetite, and a rash.
