PQR620

PQR620 is a potent, highly selective, and orally bioavailable small molecule inhibitor of both mTORC1 and mTORC2 (TORC1/2). Developed by PIQUR Therapeutics, it is a second-generation mTOR inhibitor that targets the ATP-binding site of the mTOR kinase domain. Unlike first-generation rapalogs, which primarily inhibit mTORC1, PQR620 provides a more comprehensive blockade of the PI3K/Akt/mTOR signaling pathway by preventing the feedback activation of Akt associated with mTORC2. Preclinical studies have demonstrated its efficacy as a single agent and in combination with the BCL2 inhibitor venetoclax across a broad range of lymphoid malignancies, including diffuse large B-cell lymphoma (DLBCL) and mantle cell lymphoma (MCL). Additionally, its ability to cross the blood-brain barrier suggests potential applications in treating primary central nervous system lymphoma and various neurological disorders.

Other names

5-[4,6-bis(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine