alpelisib + sacituzumab govitecan

**Alpelisib + sacituzumab govitecan** is an investigational combination therapy used in the treatment of metastatic or locally recurrent HER2-negative breast cancer, including triple-negative breast cancer (TNBC). Alpelisib is a *phosphatidylinositol 3-kinase alpha (PI3Kα) inhibitor* that targets the PI3K pathway, particularly in cancers with PIK3CA mutations, resulting in inhibition of cell growth and survival. Sacituzumab govitecan is an *antibody–drug conjugate (ADC)* composed of a humanized anti-Trop-2 monoclonal antibody conjugated to SN-38, the active metabolite of irinotecan, via a hydrolysable linker. The ADC binds to Trop-2 on tumor cells, delivering SN-38 directly, causing DNA damage and cell death primarily through inhibition of topoisomerase 1. The combination is under clinical investigation based on rational hypotheses of targeting both PI3K signaling and direct cytotoxic delivery to Trop-2-expressing tumor cells in HER2-negative breast cancer[1][3][4][5][7][8].

Brand names

Piqray + Trodelvy