1228586-24-0Relevant 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.
, 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.
