Products
Alpelisib was approved in the United States in 2019 and in many countries in 2020 in film-coated tablet form (Piqray).
Structure and properties
Alpelisib (C19H22F3N5O2S, Mr = 441.5 g/mol) exists as a white powder.
Effects
Alpelisib (ATC L01XX65) has antiproliferative and antitumor properties. The effects are due to inhibition of the α-subunit of phosphatidylinositol 3-kinase (PI3Kα). Mutations in the gene , which encodes the catalytic α-subunit, lead to increased activity of PI3Kα and tumorigenesis. The half-life is in the range of 8 to 9 hours.
Indications
In combination with fulvestrant for the treatment of postmenopausal women with HR-positive, HER2-negative advanced breast cancer with a PIK3CA mutation after disease progression, when patients have received prior endocrine therapy including an aromatase inhibitor.
Dosage
According to the SmPC. Tablets are taken once daily immediately after a meal and always at approximately the same time of day.
Contraindications
- Hypersensitivity
- Pregnancy, women of childbearing age. Alpelisib has fertility damaging (teratogenic) properties.
For complete precautions, see the drug label.
Interactions
Alpelisib is metabolized to a minor extent by CYP450 isozymes. It is a substrate of BCRP.
Adverse Effects
The most common potential adverse effects include (combination with fulvestrant):
