Abstract
Phosphatidylinositol-3-kinase (PI3K)/AKT/mammalian target of rapamycin (MTOR) pathway hyperactivation is seen in a multitude of malignancies. Due to the importance of this pathway in numerous critical cellular functions, preclinical and clinical investigations have aimed to target this pathway as an anti-cancer therapeutic strategy. This has led to the development of PI3K, AKT, and MTOR inhibitors for use in cancer patients, leading to multiple FDA approvals over the past decade. In this review, we outline therapeutic targets in PI3K/AKT/MTOR signaling in solid tumors, the current state of using inhibitors of this pathway to treat patients whose cancers possess activating mutations in PIK3CA, AKT1/2, or MTOR, and exciting new inhibitors that are entering clinical trials.