Piqray:

• Treatment of postmenopausal women and men with hormone receptor-positive, human epidermal growth factor receptor 2-negative, PIK3CA-mutated, advanced or metastatic breast cancer (in combination with fulvestrant).

Vijoice:

• Severe manifestations of PIK3CA-related overgrowth spectrum in patients who require systemic therapy.

Contraindicated in:

• History of serious hypersensitivity reactions including anaphylaxis, Stevens-Johnson syndrome, erythema multiforme, or toxic epidermal necrolysis
• Concurrent use of strong CYP3A inducers
• OB: Pregnancy
• Lactation: Lactation.

Use Cautiously in:

• Diabetes or risk factors for hyperglycemia (obesity, elevated fasting plasma glucose, elevated HbA1c, concurrent use of systemic corticosteroids or age ≥75 yr)
• Severe renal impairment (CCr ≤30 mL/min) (Piqray only)
• Rep: Women of reproductive potential and men with female partners of reproductive potential
• Pedi: Safety and effectiveness not established in children <18 yr (breast cancer) or <2 yr (PIK3CA-related overgrowth spectrum)
• Geri: Older adults may be more sensitive to drug effects.

CV: peripheral edema.

Derm: Stevens-johnson syndrome (SJS), alopecia, drug reaction with eosinophilia and systemic symptoms (dress), dry skin, erythema Multiform (EM), pruritus, rash, toxic epidermal necrolysis (TEN), cellulitis, eczema.

Endo: hyperglycemia, hypoglycemia, hyperglycemic hyperosmolar non-ketotic syndrome, KETOACIDOSIS.

F and E: hyperkalemia, hypocalcemia, hypokalemia, hypomagnesemia, hyponatremia, hypophosphatemia.

GI: ↓ appetite, ↑ lipase, ↑ liver enzymes, abdominal pain, diarrhea, hyperbilirubinemia, metallic taste, nausea, stomatitis, vomiting, colitis.

GU: ↑ serum creatinine, ↓ fertility, acute kidney injury.

Hemat: anemia, lymphocytopenia, thrombocytopenia.

Metab: ↓ weight, hypercholesterolemia, hypertriglyceridemia, hypoalbuminemia.

Neuro: fatigue, headache, insomnia.

Resp: cough, PNEUMONITIS.

Misc: fever, infection, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA).

Drug-Drug:

• Strong CYP3A4 inducers may ↓ levels and effectiveness; avoid concurrent use.
• breast cancer resistance protein inhibitors may ↑ levels and risk of toxicity; avoid concurrent use.
• May ↓ levels of CYP2C9 substrates, including warfarin.

• Tablets (Piqray): 50 mg; 150 mg; 200 mg;
• Tablets (Vijoice): 50 mg; 125 mg; 200 mg;

Breast Cancer

• PO (Adults): 300 mg once daily until disease progression or unacceptable toxicity.

PIK3CA-Related Overgrowth Spectrum

• PO (Adults): 250 mg once daily until disease progression or unacceptable toxicity.
• PO (Children 6–<18 yr): 50 mg once daily until disease progression or unacceptable toxicity. After 24 wk, may ↑ to 125 mg once daily to optimize clinical/radiological response; continue until disease progression or unacceptable toxicity. Once patient becomes 18 yr old, gradually ↑ to 250 mg once daily.
• PO (Children 2–<6 yr): 50 mg once daily until disease progression or unacceptable toxicity.

Piqray, Vijoice

• Acts as an inhibitor of phosphatidylinositol 3–kinase (PI3K). Mutations in the gene encoding the catalytic α-subunit of PI3K (PI3KCA) lead to activation of PI3Kα and Akt-signaling, cellular transformation, and tumor generation. Alpelisib inhibits phosphorylation of PI3K downstream targets (including Akt) and demonstrated activity in cell lines harboring a PIK3CA mutation. Activating mutations in PIK3CA may induce overgrowths and malformations in PROS.

• Decreased progression of breast cancer.
• Reduction in lesion volume in PIK3CA-related overgrowth spectrum.

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors

Absorption: Well absorbed following oral administration.

Distribution: Widely distributed to tissues.

Metabolism/Excretion: Primarily metabolized via hydrolysis; also metabolized to a lesser extent by CYP3A4. Excreted in feces (36% as unchanged drug; 32% as metabolites) and urine (2% as unchanged drug; 7% as metabolites).

Half-life: 8–9 hr.

(plasma concentrations)

• Instruct patient to take alpelisib as directed. Take missed doses with food within 9 hr of time usually taken. If >9 hr, omit dose and take next dose next day at usual time. If patient vomits after dose, skip dose and take next dose next day. Advise patient to read Patient Information before starting and with each Rx refill in case of changes.
• Advise patients to notify health care professional of the signs and symptoms of hypersensitivity reactions, skin reactions, hyperglycemia (e.g., excessive thirst, urinating more often than usual or higher amount of urine than usual, or increased appetite with weight loss), and lung problems occur. Advise patients to immediately report new or worsening respiratory symptoms.
• If diarrhea occurs, advise patient to start antidiarrheal treatment, increase oral fluids, and notify health care professional.
• Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking any new medications.
• Rep: May cause fetal harm. Advise females of reproductive potential and males with female partners of reproductive potential to use effective contraception during and for 1 wk after last dose. Advise patient to avoid breast feeding during and for 1 wk after last dose. May impair fertility in male and female patients.

AL-pe-LISib

NDC Code^*

• 0078- Novartis Pharmaceuticals Corporation
  • 0078-0701- PIQRAY
    • 0078-0701-84- 1 BLISTER PACK in 1 CARTON (0078-0701-84) > 28 TABLET in 1 BLISTER PACK (0078-0701-51)

• 0078- Novartis Pharmaceuticals Corporation
  • 0078-0708- PIQRAY
    • 0078-0708-02- 2 BLISTER PACK in 1 CARTON (0078-0708-02) > 28 TABLET in 1 BLISTER PACK (0078-0708-51)

• 0078- Novartis Pharmaceuticals Corporation
  • 0078-0708- PIQRAY
    • 0078-0708-91- 1 BLISTER PACK in 1 CARTON (0078-0708-91) > 28 TABLET in 1 BLISTER PACK (0078-0708-90)

• 0078- Novartis Pharmaceuticals Corporation
  • 0078-0715- PIQRAY
    • 0078-0715-02- 2 KIT in 1 CARTON (0078-0715-02) > 1 KIT in 1 KIT (0078-0715-61) * 14 TABLET in 1 BLISTER PACK * 14 TABLET in 1 BLISTER PACK

• 0078- Novartis Pharmaceuticals Corporation
  • 0078-0715- PIQRAY
    • 0078-0715-91- 1 KIT in 1 CARTON (0078-0715-91) > 1 KIT in 1 KIT (0078-0715-94) * 14 TABLET in 1 BLISTER PACK * 14 TABLET in 1 BLISTER PACK