PIQRAY® (alpelisib) | PIK3CA-mutated advanced breast cancer | PIK3CA mutations

For Healthcare Professionals Outside the US

Patients with a PIK3CA mutation face a poor prognosis1

Patients with a PIK3CA mutation can have:
PIK3CA mutations have been identified in patients with endocrine resistance. A more aggressive disease can lead to shorter mPFS or death. ~40% of patients with HR+/HER2- aBC have a PIK3CA mutation PIK3CA mutations have been identified in patients with endocrine resistance. A more aggressive disease can lead to shorter mPFS or death. ~40% of patients with HR+/HER2- aBC have a PIK3CA mutation

PIK3CA is the most commonly mutated gene in HR+/HER2- aBC5

PIQRAY directly targets the PI3K pathway, which may help overcome endocrine resistance6

  • PI3K inhibition with PIQRAY has been shown to induce an increase in estrogen receptor transcription in breast cancer cells6
  • PIQRAY inhibits the alpha isoform of PI3K 50 times more potently than other PI3K isophorms (β, γ, δ)2

PIQRAY is a nonchemotherapeutic α-selective PI3K inhibitor that works synergistically with fulvestrant across both the PI3K and ER pathways, respectively6

PIQRAY and fulvestrant mechanism of action graphic PIQRAY and fulvestrant mechanism of action graphic Based on in vitro/in vivo studies. Preclinical activity does not necessarily correlate with clinical outcomes.

PIK3CA is a common mutation in HR+/HER2- aBC with effects that may be addressed with a targeted approach5,6

AKT, protein kinase B; HER2, human epidermal growth factor receptor 2; HR, hormone receptor; mPFS, median progression-free survival; mTOR, mechanistic target of rapamycin; PI3Kα, α isoform of phosphatidylinositol-3-kinase.
PIQRAY mechanism of action video with Dr Fabrice André
Watch how PIQRAY
addresses the effects
of the PIK3CA mutation
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MOA video image

Test patients for PIK3CA mutations at HR+/HER2- MBC diagnosis to be ready to treat at progression9*

  • Why to test: patients face a poor prognosis

    ~40% of HR+/HER2- aBC patients have a PIK3CA mutation, and can have endocrine resistance and/or shorter mPFS2-5

  • When to test: test at MBC diagnosis

    Test at initial MBC diagnosis9:

    Test for PIK3CA mutations at initial MBC diagnosis if tumor is HR+/HER2-

  • How to test: using tissue or plasma samples

    PIK3CA mutations can be detected in tissue (using archival specimens and recent or new biopsies) or plasma. If mutation is not detected in plasma, test tumor tissue2

Test up front knowing that PIK3CA mutations are generally stable in archival tissue samples2
  • In SOLAR-1, 315 of the 341 (92.5%) patients used archival tumor tissue and tested positive for a PIK3CA mutation2
References: 1. Mosele F, Stefanovska B, Lusque A, et al. Outcome and molecular landscape of patients with PIK3CA-mutated metastatic breast cancer. Ann Oncol. 2020;31(3):377-386. 2. Data on file. Novartis Pharmaceuticals Corp; 2018. 3. André F, Ciruelos E, Rubovszky G, et al. Alpelisib for PIK3CA-mutated, hormone receptor-positive advanced breast cancer. N Engl J Med. 2019;380(20):1929-1940. 4. Mollon LE, Anderson EJ, Dean JL, et al. A systematic literature review of the prognostic and predictive value of PIK3CA mutations in HR+/HER2- metastatic breast cancer. Clin Breast Cancer. 2020;20(3):e232-e243. 5. The Cancer Genome Atlas Network. Comprehensive molecular portraits of human breast tumours. Nature. 2012;490(7418):61-70. 6. Piqray® (alpelisib) EU Summary of Product Characteristics. Novartis; 2022. 7. Chalhoub C, Baker SJ. PTEN and the PI3-kinase pathway in cancer. Annu Rev Pathol. 2009;4:127-150. 8. Falsodex EU Summary of Product Characteristics. AstraZeneca; 2020. 9. Gennari A, André F, Barrios CH, et al. ESMO Clinical Practice Guideline for the diagnosis, staging and treatment of patients with metastatic breast cancer. Ann Oncol. 2021;32(12):1475-1495.