Alpelisib-Piqray’s role

Alpelisib (Alpelisib)-Piqray is a phosphatidylinositol-3-kinase (PI3K) inhibitor that mainly has inhibitory activity against PI3Kα. In cancer cell lines, apelvis inhibits phosphorylation of PI3K downstream targets, including Akt, and shows activity in cell lines harboring PIK3CA mutations. In vivo, apelvis inhibits the PI3K/Akt signaling pathway and reduces tumor growth in xenograft models, including cancer models. In breast cancer cells, inhibition of PI3K by apelvis treatment induces an increase in estrogen receptor (ER) transcription. In a xenograft model derived from an ER-positive, PIK3CA-mutated cancer breast cancer cell line, the combination of apelvis and fulvestrant showed increased anti-tumor activity compared to treatment alone.