The discovery of PIK3CA mutations has led to the development of targeted therapies. PI3K inhibitors, such as alpelisib (Piqray), have shown efficacy in treating cancers with PIK3CA mutations. Alpelisib is specifically approved for use in combination with fulvestrant for the treatment of hormone receptor-positive, HER2-negative breast cancer with PIK3CA mutations in postmenopausal women and men.