amcenestrant + alpelisib

Amcenestrant + alpelisib is an investigational combination therapy developed for estrogen receptor (ER)-positive, HER2-negative advanced or metastatic breast cancer, especially in postmenopausal women. - Amcenestrant is an oral selective estrogen receptor degrader (SERD) that binds to and degrades the estrogen receptor, antagonizing estrogen-driven tumor growth[3][5][7]. - Alpelisib is a small molecule, oral, selective inhibitor of the phosphatidylinositol 3-kinase alpha (PI3Kα) isoform, targeting the PI3K/AKT signaling pathway, particularly beneficial in tumors with PIK3CA mutations[9]. The combination is studied to overcome endocrine resistance in hormone-receptor positive, HER2-negative breast cancer by simultaneously blocking estrogen signaling and PI3K pathway signaling[1][5]. Clinical trials (e.g., AMEERA-1) have investigated safety, dosing, and preliminary efficacy of this combination[1][5][7].