alpelisib + letrozole

Alpelisib + letrozole is a combination therapy used primarily for the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer with PIK3CA mutations. Alpelisib is a selective oral inhibitor of the class I PI3K catalytic subunit p110α (PI3Kα), which blocks the PI3K/AKT signaling pathway involved in cell proliferation and survival. Letrozole is an aromatase inhibitor that suppresses estrogen production by inhibiting the aromatase enzyme, thereby reducing estrogen-driven tumor growth in HR-positive cancers. This combination has shown efficacy particularly in patients who have progressed on prior endocrine therapies such as CDK4/6 inhibitors plus fulvestrant or chemotherapy[1][2][3][4]. The regimen demonstrates manageable toxicity with common adverse events including hyperglycemia, rash, diarrhea, fatigue, and nausea[1][3]. Clinical benefit appears higher in patients with PIK3CA-mutated tumors but can also be observed regardless of mutation status[1].

Brand names

Piqray + Femara

Other names

alpelisib and letrozolePiqray and Femara