1228587-59-4Relevant articles and documents
Identification and optimization of pteridinone toll-like receptor 7 (TLR7) agonists for the oral treatment of viral hepatitis
Roethle, Paul A.,McFadden, Ryan M.,Yang, Hong,Hrvatin, Paul,Hui, Hon,Graupe, Michael,Gallagher, Brian,Chao, Jessica,Hesselgesser, Joseph,Duatschek, Paul,Zheng, Jim,Lu, Bing,Tumas, Daniel B.,Perry, Jason,Halcomb, Randall L.
supporting information, p. 7324 - 7333 (2013/10/21)
Pteridinone-based Toll-like receptor 7 (TLR7) agonists were identified as potent and selective alternatives to the previously reported adenine-based agonists, leading to the discovery of GS-9620. Analogues were optimized for the immunomodulatory activity and selectivity versus other TLRs, based on differential induction of key cytokines including interferon α (IFN-α) and tumor necrosis factor α (TNF-α). In addition, physicochemical properties were adjusted to achieve desirable in vivo pharmacokinetic and pharmacodynamic properties. GS-9620 is currently in clinical evaluation for the treatment of chronic hepatitis B (HBV) infection.