alpelisib (Piqray)

Indications

• treatment or postmenopausal women & men, with ER & PR-positive, HER2-negative, PIK3CA-mutated, advanced or metastatic breast cancer

* used in combination with fulvestran

Monitor

• serum glucose, hemoglobin A1c

Adverse effects

• hyperglycemia, increase in serum creatinine, hypocalcemia
• lymphopenia, anemia, prolonged aPTT prolonged
• elevated liver enzymes, increase in serum lipase
• diarrhea, nausea/vomiting, decreased appetite, stomatitis
• pneumonitis/interstitial lung disease
• weight loss, fatigue
• rash, hair loss
• potentially severe skin reactions
  • Stevens-Johnson Syndrome, erythema multiforme, toxic epidermal necrolysis

Laboratory

• used in combination with approved the companion diagnostic test, therascreen PIK3CA RGQ PCR Kit*

* detects the PIK3CA mutation in a tissue &/or a liquid biopsy

* patients who are negative by the therascreen test using a liquid biopsy should undergo tumor biopsy for PIK3CA mutation testing.

Mechanism of action

• PIK3 inhibitor

More general terms

• small inhibitory antineoplastic agent (ib drug)

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=56649450