HIGHLIGHTS OF PRESCRIBING INFORMATION
These highlights do not include all the information needed to use PIQRAY safely and effectively. See full prescribing information for PIQRAY.
PIQRAYïż½ (alpelisib) tablets, for oral use
Initial U.S. Approval: 2019
INDICATIONS AND USAGE
PIQRAY is a kinase inhibitor 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, PIK3CA-mutated, advanced or metastatic breast cancer as detected by an FDA-approved test following progression on or after an endocrine-based regimen. (1)
DOSAGE AND ADMINISTRATION
Recommended dose: 300 mg (two 150 mg tablets) taken orally once daily with food. (2.2)
For adverse reactions, consider dose interruption, dose reduction, or discontinuation. (2.3)
DOSAGE FORMS AND STRENGTHS
Tablets: 50 mg, 150 mg, 200 mg (3)
CONTRAINDICATIONS
Severe hypersensitivity to PIQRAY or to any of its components (4).
WARNINGS AND PRECAUTIONS
Severe Hypersensitivity: Permanently discontinue PIQRAY. Promptly initiate appropriate treatment. (5.1)
Severe Cutaneous Reactions: Cases of severe cutaneous reactions, including Stevens-Johnson syndrome (SJS) and Erythema Multiforme (EM) were reported. Do not initiate treatment in patients with a history of SJS, EM, or Toxic Epidermal Necrolysis (TEN). Interrupt PIQRAY if signs or symptoms of severe cutaneous reactions are present, until etiology of the reaction has been determined. Consider consultation with a dermatologist. Permanently discontinue PIQRAY if SJS, EM, or TEN is confirmed. (5.2)
Hyperglycemia: Severe hyperglycemia, including ketoacidosis, was reported. The safety of PIQRAY in patients with Type 1 or uncontrolled Type 2 diabetes has not been established. Before initiating treatment with PIQRAY, test fasting plasma glucose (FPG), HbA1c, and optimize blood glucose. After initiating treatment, monitor periodically. Initiate or optimize anti-hyperglycemic medications as clinically indicated. Interrupt, reduce dose, or discontinue PIQRAY if severe hyperglycemia occurs. (2.3, 5.3)
Pneumonitis: Severe cases of pneumonitis and interstitial lung disease have been reported. Monitor for clinical symptoms or radiological changes. Interrupt or discontinue PIQRAY if severe pneumonitis occurs. (2.3, 5.4)
Diarrhea: Severe cases of diarrhea, including dehydration and acute kidney injury, have been reported. Most patients experience diarrhea (Grade ≤ 2) during treatment with PIQRAY. Advise patients to start antidiarrheal treatment, increase oral fluids, and notify their healthcare provider if diarrhea occurs. Interrupt, reduce dose, or discontinue PIQRAY if severe diarrhea occurs. (2.3, 5.5)
Embryo-Fetal Toxicity: PIQRAY can cause fetal harm. Advise patients of potential risk to a fetus and to use effective contraception (5.6, 8.1, 8.3). Also, refer to the Full Prescribing Information of fulvestrant for pregnancy and contraception information.
ADVERSE REACTIONS
Most common adverse reactions including laboratory abnormalities (all grades, incidence ≥ 20%) were glucose increased, creatinine increased, diarrhea, rash, lymphocyte count decreased, GGT increased, nausea, ALT increased, fatigue, hemoglobin decreased, lipase increased, decreased appetite, stomatitis, vomiting, weight decreased, calcium decreased, glucose decreased, aPTT prolonged, and alopecia (6.1).
To report SUSPECTED ADVERSE REACTIONS, contact Novartis Pharmaceuticals Corporation at 1-888-669-6682 or FDA at 1-800-FDA-1088 or WWW.FDA.GOV/MEDWATCH.
DRUG INTERACTIONS
CYP3A4 Inducers: Avoid coadministration of PIQRAY with a strong CYP3A4 inducer. (7.1)
BCRP Inhibitors: Avoid the use of BCRP inhibitors in patients treated with PIQRAY. If unable to use alternative drugs, closely monitor for increased adverse reactions. (7.1)
CYP2C9 Substrates: Closely monitor when PIQRAY is coadministered with CYP2C9 substrates where decreases in the plasma concentration of these drugs may reduce activity. (7.2)
USE IN SPECIFIC POPULATIONS
Lactation: Advise not to breastfeed. (8.2)
See 17 for PATIENT COUNSELING INFORMATION and FDA-approved patient labeling.
Revised: 5/2019