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  • PI3K inhibition with PIQRAY has been shown to induce an increase in estrogen receptor (ER) transcription in breast cancer cells1

  • PIQRAY inhibits the alpha isoform of PI3K 50 times more potently than other PI3K isoforms (β, γ, δ)2

 

PIQRAY is a nonchemotherapeutic α-selective PI3K inhibitor that works synergistically with fulvestrant across both the PI3K and ER pathways, respectively1
PIQRAY mechanism of action

Based on in vitro/in vivo studies. Preclinical activity does not necessarily correlate with clinical outcomes.
PI3Kα, α isoform of phosphatidylinositol-3-kinase.

PIK3CA is a common driver mutation in HR+/HER2- aBC with effects that may be addressed with a targeted approach1,5

 

Important Safety Information

PIQRAY is contraindicated in patients with severe hypersensitivity to it or any of its components.

Severe Hypersensitivity: Severe hypersensitivity reactions, including anaphylaxis and anaphylactic shock, can occur in patients treated with PIQRAY. Severe hypersensitivity reactions were manifested by symptoms, including, but not limited to, dyspnea, flushing, rash, fever, or tachycardia...

Indication

PIQRAY® (alpelisib) tablets is 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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References: 1. Piqray. Prescribing information. Novartis Pharmaceuticals Corp. 2. Data on file. Novartis Pharmaceuticals Corp; 2021. 3. Chalhoub C, Baker SJ. PTEN and the PI3-kinase pathway in cancer. Annu Rev Pathol. 2009;4:127-150. 4. Faslodex [prescribing information]. Wilmington, DE: AstraZeneca Pharmaceuticals LP. 5. The Cancer Genome Atlas Network. Comprehensive molecular portraits of human breast tumours. Nature. 2012;490(7418):61-70.