Drug updated on 12/11/2024
| Dosage Form | Tablet (oral; 50 mg, 150 mg, 200 mg) |
| Drug Class | Kinase inhibitors |
| Ongoing and Completed Studies | ClinicalTrials.gov |
Indication
- 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.
Latest News
Summary
- This summary is based on the review of three systematic review(s)/meta-analysis(es). [1-3]
- Effectiveness Outcomes: In a meta-analysis of randomized controlled trials, phosphatidylinositol 3-kinase (PI3K) inhibitors, specifically alpelisib, demonstrated significant benefits in the PIK3CA-mutated group, with improved objective response rate (OR), progression-free survival (PFS), and notably superior 6-month PFS compared to fulvestrant.
- Population and Treatment Recommendations: Alpelisib, in combination with endocrine therapy (ET), is recommended for postmenopausal and male patients with hormone receptor-positive (HR+), HER2-negative (HER2-), PIK3CA-mutated advanced breast cancer (ABC) or metastatic breast cancer (MBC) who have previously received ET, with or without a CDK 4/6 inhibitor.
- Comparative Effectiveness: Alpelisib was ranked first in 6-month PFS among PI3K inhibitors, surpassing other agents such as buparlisib, pictilisib, and taselisib, highlighting its potential for better outcomes in the specified patient population.
- Adverse Events: The use of alpelisib is associated with significant adverse events (AEs), including hyperglycemia (59%), diarrhea (56%), nausea (44%), and rash (38%), with grade 3/4 hyperglycemia and rash reported in 28% and 10% of patients, respectively; 18% of patients discontinued treatment due to toxicities.
- Safety Profile: Overall, PI3K inhibitors, including alpelisib, exhibited good safety profiles with few serious AEs, although specific safety outcomes were not detailed in the reviewed studies.
Product Monograph / Prescribing Information
| Document Title | Year | Source |
|---|---|---|
| Piqray (alpelisib) Prescribing Information. | 2024 | Novartis Pharmaceuticals Corporation, East Hanover, NJ |
Systematic Reviews / Meta-Analyses
| Document Title | Year | Source |
|---|---|---|
| Which Is the Most Appropriate PI3K Inhibitor for Breast Cancer Patients with or without PIK3CA Status Mutant? A Systematic Review and Network Meta-Analysis | 2020 | BioMed Research International |
| A systematic review and meta-analysis of selected toxicity endpoints of alpelisib | 2020 | Oncotarget |
| A Systematic Review of the Prevalence and Diagnostic Workup of PIK3CA Mutations in HR+/HER2- Metastatic Breast Cancer | 2020 | International Journal of Breast Cancer |
Clinical Practice Guidelines
| Document Title | Year | Source |
|---|---|---|
| Biomarkers for Systemic Therapy in Metastatic Breast Cancer: ASCO Guideline Update | 2022 | Oncology |
| Endocrine Treatment and Targeted Therapy for Hormone Receptor-Positive, Human Epidermal Growth Factor Receptor 2-Negative Metastatic Breast Cancer: ASCO Guideline Update | 2021 | Journal of Clinical Oncology |
| 5th ESO-ESMO international consensus guidelines for advanced breast cancer (ABC 5). | 2020 | Annals of Oncology |