Alpelisib (Piqray)

Mechanism of action

From NCI Drug Dictionary: An orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. Alpelisib specifically inhibits PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway. This may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations.

Diseases for which it is used

• PIK3CA-mutated breast cancer

Patient drug information

• Alpelisib (Piqray) Package Insert

History of changes in FDA indication

• 2019-05-24: Approved in combination with fulvestrant for postmenopausal women, and men, with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA-mutated, advanced or metastatic breast cancer as detected by an FDA-approved test following progression on or after an endocrine-based regimen. (Based on SOLAR-1)

History of changes in EMA indication

• 2020-07-27: Initial authorization as Piqray 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.

History of changes in Health Canada indication

• 2020-03-11: Initial notice of compliance in combination with fulvestrant for the treatment of postmenopausal women, and men, with hormone receptor-positive, HER2-negative, PIK3CA-mutated advanced or metastatic breast cancer after disease progression following an endocrine-based regimen.

Also known as

• Code name: BYL-719
• Brand name: Piqray