PIQRAY is a kinase inhibitor indicated in combination with fulvestrant for the treatment of adults 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.

Anticancer- Monoclonal antibodies

Distribution: Vdss: 114 L. Protein binding: 89%. Metabolism: Primarily by chemical and enzymatic hydrolysis to form its metabolite BZG791, and to a lesser extent by CYP3A4. Half-life elimination: 8 to 9 hours. Time to peak: 2 to 4 hours. Excretion: Following a single 400 mg dose: Feces: 81% (36% as unchanged drug, 32% as BZG791); Urine: 14% (2% as unchanged drug, 7% as BZG791). Clearance: 9.2 L/hour (under fed conditions).

Severe hypersensitivity to alpelisib or any component of the formulation.

Based on the mechanism of action, and data from animal reproduction studies, in utero exposure to alpelisib may cause fetal harm. Also refer to the fulvestrant monograph for additional information.

It is not known if alpelisib is present in breast milk. Due to the potential for adverse events in a breastfed infant, breastfeeding is not recommended during therapy and for 1 week after the last alpelisib dose. Also refer to the Fulvestrant monograph for additional information.

glucose increased, creatinine increased, diarrhea, rash, lymphocyte count decreased, gamma-glutamyl transferase (GGT) increased, nausea, alanine aminotransferase (ALT) increased, fatigue, hemoglobin decreased, lipase increased, decreased appetite, stomatitis, vomiting, weight decreased, calcium decreased, glucose decreased, activated partial thromboplastin time (aPTT) prolonged, and alopecia.

The recommended dose of PIQRAY is 300 mg (two 150 mg film-coated tablets) taken orally, once daily, with food. Continue treatment until disease progression or unacceptable toxicity occurs. Dose Modifications for Adverse Reactions: Starting dose 300 mg once daily First-dose reduction 250 mg once daily Second-dose reduction 200 mg once daily

The safety and efficacy of PIQRAY in pediatric patients have not been established.

The effect of severe renal impairment (CLcr < 30 mL/min) on alpelisib pharmacokinetics is unknown. No dose adjustment is recommended for patients with mild to moderate renal impairment (CLcr 30 to < 90 mL/min).

Hepatic impairment prior to treatment initiation: Child-Turcotte-Pugh classes A, B, or C: There are no dosage adjustments provided in the manufacturer's labeling; however, no clinically significant differences in pharmacokinetics are expected. Acute hepatotoxicity during treatment: Grade 2 total bilirubin elevation: Interrupt alpelisib treatment until improvement to ? grade 1, then resume at the same dose level if resolved in ?14 days or resume at the next lower dose level if improved in >14 days. For dosage adjustment levels and other toxicity grades.

store at 20°C to 25°C , excursions permitted between 15°C and 30°C