Category/Class

Oral targeted therapy, phosphatidylinositol 3 kinase inhibitor (predominantly alpha) (PI3K alpha)       

Indication

Used in combination with fulvestrant for the treatment of men and postmenopausal women with hormone receptor-positive, 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.

Dosing

300 mg, dispensed as two 150 mg tablets   

Administration

Take orally once daily with food at approximately the same time each day. Do not crush or cut. Missed doses may be taken within nine hours; after nine hours, do not take the missed dose and resume therapy the next day at the usual dose time.            

Adverse Reactions

The most frequent adverse reactions to alpelisib when taken with fulvestrant were hyperglycemia, rash, elevated creatinine, elevated lipase, elevated liver function tests (e.g, GGT, ALT), diarrhea, decreased lymphocytes and hemoglobin, nausea, decreased appetite, stomatitis, hair loss, and fatigue. Occasional and rare side effects included severe pneumonitis, severe hypersensitivity reactions, and severe cutaneous reactions.

Nursing Considerations

Test fasting plasma glucose and HbA1c and optimize blood glucose prior to starting alpelisib. Monitor blood glucose throughout therapy, and more frequently in patients with prediabetes or diabetes. Educate patients on symptoms of hyperglycemia. Consider monitoring fasting glucose in patients at high risk for diabetes. Initiate or optimize antihyperglycemic medications as indicated.

Advise patients about the signs of severe cutaneous adverse reactions, including progressive skin rash or mucosal lesions, and flu-like syndrome. Severe diarrhea may lead to dehydration and acute kidney injury, and the drug may need to be interrupted, dose reduced, or discontinued. Instruct patients to use antidiarrheals and oral hydration and notify their healthcare team if diarrhea occurs.

Monitor patients' laboratory values, including complete blood counts, glucose, and renal and liver function. Monitor clinical symptoms or radiologic changes for pneumonitis and interstitial lung disease. Discontinue alpelisib if severe pneumonitis occurs.

Advise female patients and male patients with female partners of reproductive potential about the risk to a fetus and to use effective contraception during treatment and for one week after the last dose.

Drug-Drug Interactions

Coadministration with a strong CYP3A4 inducer may decrease the concentration and potential effectiveness of alpelisib. BCRP inhibitors may increase the concentration of alpelisib. If unable to use alternative drugs, closely monitor for increased adverse reactions. Alpelisib may decrease the concentration and efficacy of CYP2C9 substrates.

Patient Education

Instruct patients on the potential for hyperglycemia, allergic reactions, and severe skin reactions. Educate patients about risk of diarrhea, at-home management, and antidiarrheal medications. Advise patients to use effective contraception because of the risk of embryo-fetal toxicity. Avoid pregnancy and breastfeeding while taking alpelisib and for at least one week after the last dose.

Gero-Oncology Considerations

Patients aged 65 and older had a higher incidence of high-grade hyperglycemia. Older patients may be more sensitive to side effects and should be carefully monitored for incidence and clinical impact.      

Safe Handling

Alpelisib can cause fetal harm.         

Patient Assistance

Information about the Novartis Oncology Universal Copay Program is available.