sapanisertib

Sapanisertib is a potent, orally available small molecule that acts as an ATP-competitive dual inhibitor of the mammalian target of rapamycin complexes 1 and 2 (mTORC1/2). By binding to and inhibiting both TORC1 and TORC2 complexes of mTOR, sapanisertib disrupts the PI3K/Akt/mTOR signaling pathway—a pathway frequently dysregulated in human cancers—leading to decreased tumor cell proliferation and increased apoptosis. Sapanisertib is considered a second-generation mTOR inhibitor with activity against tumors resistant to first-generation rapalogs. It has been investigated primarily for various advanced solid tumors including endometrial cancer, ovarian cancer, glioblastoma, neuroendocrine tumors (including pancreatic), soft tissue sarcoma, bladder cancer, thyroid cancer as well as other malignancies. Additionally, preclinical studies have shown its potential as a multistage antimalarial agent by inhibiting Plasmodium kinases such as phosphatidylinositol 4-kinase type III beta (PI4Kβ) and cGMP-dependent protein kinase (PKG).

Other names

sapanisertib