Chemical formula: C₁₉H₂₂F₃N₅O₂S  Molecular mass: 441.47 g/mol  PubChem compound: 56649450

Therapeutic indications

Alpelisib is indicated for:

HR-positive, HER2-negative locally advanced or metastatic breast cancer with a PIK3CA mutation

Population group: only adults (18 years old or older)

Alpelisib is indicated in combination with fulvestrant for the treatment of postmenopausal women, and men, with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, locally advanced or metastatic breast cancer with a PIK3CA mutation after disease progression following endocrine therapy as monotherapy.

For this indication, competent medicine agencies globally authorize below treatments (click for details):


Alpelisib is contraindicated in the following cases:





History of severe cutaneous reactions

Cutaneous hypersensitivity

Osteonecrosis of the jaw caused by bisphosphonate

Bisphosphonate related osteonecrosis of jaw

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Factors such as age, gender, and health history are evaluated to create a personalized medication regimen.

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