Pivikto

Alpelisib

Postmenopausal women, & men, w/ hormone receptor +ve, HER2 -ve, advanced breast cancer w/ a PIK3CA mutation in combination w/ fulvestrant after disease progression following an endocrine-based regimen.

300 mg (2 x 150 mg) once daily on a continuous basis. Max daily dose: 300 mg. Co-administered w/ fulvestrant 500 mg IM on days 1, 15 & 29, & once mthly thereafter.

Should be taken with food: Take at approx same time each day. Swallow whole, do not chew/crush/split.

Hypersensitivity.

Hypersensitivity reactions (including anaphylactic reaction & shock). Permanently discontinue & should not be reintroduced in patients w/ serious hypersensitivity reactions. Do not initiate in patients w/ a history of severe cutaneous reactions; permanently discontinue if severe cutaneous reactions is confirmed. Patients w/ type 1 & uncontrolled type 2 diabetes. Hyperglycemia w/ rapid onset after starting treatment; frequently self-monitor in the 1st 4 wk & especially w/in the 1st 2 wk of treatment, as clinically indicated. May require dose interruption, reduction or discontinuation based on severity of hyperglycaemia. Permanently discontinue in all patients w/ confirmed pneumonitis. Do not initiate in patients w/ ongoing osteonecrosis of the jaw from previous or concurrent treatment w/ bisphosphonates/denosumab. Patients w/ severe renal impairment. Minor influence on the ability to drive & use machines. Not recommended during pregnancy & in women of childbearing potential not using contraception. Women should not breast-feed during treatment & for at least 4 days after the last dose. Elderly ≥75 yr. Childn 0-18 yr.

Anemia; diarrhea, nausea, stomatitis, vomiting, abdominal pain, dyspepsia; fatigue, mucosal inflammation, peripheral edema, pyrexia, mucosal dryness; UTI; decreased wt, increased blood creatinine; hyperglycemia, decreased appetite; headache, dysgeusia; rash, alopecia, pruritus, dry skin. Lymphopenia, thrombocytopenia; blurred vision, dry eye; toothache, gingivitis, cheilitis, gingival pain; edema; hypersensitivity; increased γ-glutamyltransferase, ALT, lipase, glycosylated Hb; hypokalemia, hypocalcemia, dehydration; muscle spasm, myalgia, osteonecrosis of jaw; insomnia; acute kidney injury; pneumonitis; erythema, dermatitis, palmar-plantar erythrodysesthesia syndrome, erythema multiforme; HTN, lymphedema.

Increase in systemic exposure w/ BCRP inhibitor (eg, eltrombopag, lapatinib, pantoprazole). May increase & decreased systemic exposure of CYP3A4 substrates (eg, rifampicin, ribociclib, encorafenib). May reduce clinical activity of CYP2B6 sensitive substrates w/ narrow therapeutic index eg, bupropion. Increased AUC w/ food.

Targeted Cancer Therapy

L01EM03 - alpelisib ; Belongs to the class of phosphatidylinositol-3-kinase (Pi3K) inhibitors. Used in the treatment of cancer.

Rx