Drug updated on 4/18/2024

Dosage FormTablet (oral; 50 mg, 150 mg, 200 mg)
Drug ClassKinase inhibitors
Ongoing and
Completed Studies


  • Indicated in combination with fulvestrant for the treatment of adults 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.

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  • Alpelisib (Piqray) is indicated in combination with fulvestrant for the treatment of adults with hormone receptor-positive, human epidermal growth factor receptor 2-negative, PIK3CA-mutated advanced or metastatic breast cancer. It has shown superior clinical efficacy as a second-line treatment compared to other PI3K/AKT/mTOR inhibitors.
  • The analysis was based on five systematic reviews/meta-analyses, providing an extensive evaluation based on their studies.
  • Compared to CDK4/6 inhibitors such as abemaciclib, ribociclib, and palbociclib, combined with fulvestrant, alpelisib maintains a credible safety margin similar to its counterparts while presenting superior clinical efficacy for HR-positive, HER2-negative metastatic breast cancer patients.
  • In considering specific populations and subgroups, particularly those with PIK3CA mutation epidemiology, combining alpelisib with endocrine therapy improves response rates and progression-free survival compared to endocrine therapy alone.
  • Adverse events associated with alpelisib include hyperglycemia, diarrhea, nausea, and rash. Despite these clinically relevant adverse events leading to an 18% discontinuation rate among patients under this drug regimen, no treatment-related deaths were reported, indicating its relative safety profile.
  • Alpelisib's beneficial impact is especially noted in patients exhibiting HR+/HER2-, PIK3CA-mutant metastatic breast cancer—a population subgroup that shows substantial clinical benefit from this targeted therapeutic approach.

Product Monograph / Prescribing Information

Document TitleYearSource
Piqray (alpelisib) Prescribing Information.2024Novartis Pharmaceuticals Corporation, East Hanover, NJ

Systematic Reviews / Meta-Analyses

Clinical Practice Guidelines