Voxtalisib (XL765, SAR245409) is a potent inhibitor of the PI3K (phosphoinositide 3-kinase) pathway, which plays a critical role in cell growth, survival, and metabolism. It has been primarily investigated for its antitumor activity in various cancers due to its ability to block signaling pathways that promote tumor progression. It has shown promise in preclinical and clinical studies for treating solid tumors and hematologic malignancies, including glioblastoma, breast cancer, and non-Hodgkin’s lymphoma. By inhibiting multiple isoforms of PI3K as well as mTOR, voxtalisib disrupts key survival mechanisms in cancer cells, leading to reduced proliferation and increased apoptosis. Its dual inhibition profile makes it a candidate for overcoming resistance seen with selective PI3K inhibitors. Research has also explored its use in combination therapies with other anticancer agents to enhance efficacy and target multiple pathways simultaneously.