1 research outputs found
Identification and Optimization of Pteridinone Toll-like Receptor 7 (TLR7) Agonists for the Oral Treatment of Viral Hepatitis
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