Indications for: 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, PIK3CA-mutated, advanced or metastatic breast cancer as detected by an FDA-approved test following progression on or after an endocrine-based regimen.
Swallow whole. Take with food. 300mg once daily (in combination with fulvestrant 500mg on Days 1, 15, and 29, then once monthly thereafter); continue until disease progression or unacceptable toxicity. Dose modifications and management of adverse reactions: see full labeling.
Severe hyperglycemia. Test fasting plasma glucose (FPG), HbA1c, and optimize blood glucose prior to initiation. After initiating, monitor FPG or blood glucose at least once weekly for the first 2 weeks, then at least once every 4 weeks, and as indicated. Monitor HbA1c every 3 months and as indicated. Monitor FPG more frequently during first few weeks of treatment in those with risk factors for hyperglycemia (eg, obesity, elevated FPG, HbA1c >ULN, or age ≥75). Interrupt, reduce dose, or discontinue therapy based on severity of the hyperglycemia. Diabetes. Permanently discontinue if severe hypersensitivity occurs. Prior history of severe cutaneous reactions (eg, SJS, EM, TEN, DRESS): do not reintroduce. Interrupt therapy if signs/symptoms of severe cutaneous reactions occur; permanently discontinue if confirmed. Interrupt and evaluate if new or worsening respiratory symptoms occur; permanently discontinue if pneumonitis is confirmed. Monitor for diarrhea or colitis; interrupt, reduce dose, or discontinue therapy based on severity. Embryo-fetal toxicity. Pregnancy: exclude status prior to initiation. Advise females of reproductive potential and males (w. female partners) to use effective contraception during and for 1 week after last dose. Nursing mothers: not recommended (during and for 1 week after last dose).
Phosphatidylinositol 3-kinase inhibitor.
Antagonized by strong CYP3A4 inducers; avoid and consider alternatives. May be potentiated by BCRP inhibitors; avoid and use alternatives; if unavoidable, monitor closely for toxicity. May antagonize CYP2C9 substrates (eg, warfarin); monitor closely. Risk for hyperglycemia with concomitant systemic corticosteroids.
Lab abnormalities (eg, glucose increased, creatinine increased, lymphocyte count decreased, GGT increased, ALT increased, hemoglobin decreased, lipase increased, calcium decreased, glucose decreased, aPTT prolonged), diarrhea, rash, nausea, fatigue, decreased appetite, stomatitis, vomiting, weight decreased, and alopecia; ketoacidosis, hypersensitivity reactions, angioedema, interstitial lung disease, dehydration, acute kidney injury.
Fecal (81%), renal (14%). Half-life: 8–9 hours.
Generic Drug Availability:
Blister pack—1×28 (200mg tabs); 2×28 (200mg + 50mg tabs); 2×28 (150mg tabs)