Mechanism of Action | PIQRAY® (alpelisib) tablets

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

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 approach^1,5

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.

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

Important Safety Information

Indication

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

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