Caly Chien

TL;DR: These results provide the first clinical validation of an inhibitor of HCV NS5A, a protein with no known enzymatic function, as an approach to the suppression of virus replication that offers potential as part of a therapeutic regimen based on combinations ofHCV inhibitors.

TL;DR: Administration of BMS-663068 for 8 days with or without ritonavir resulted in substantial declines in plasma HIV-1 RNA levels and was generally well tolerated, suggesting long-term clinical trials of the prodrug as part of combination antiretroviral therapy are warranted.

TL;DR: A methoxy moiety at the C6 position of this isoquinoline ring system proved to be optimal with respect to potency and PK, thus providing the clinical compound 35, which demonstrated antiviral activity in HCV-infected patients.

TL;DR: In this paper, the authors used compartmental absorption modeling to predict the potential feasibility of extended-release (ER) delivery to achieve target Cmax :Cmin ratios, and further refined the model with respect to colonic absorption, following delivery of BMS-626529 to upper and lower GI sites.

TL;DR: The data showed that prodrug 4 had excellent potential to significantly reduce dissolution rate-limited absorption following oral dosing in humans, and provided guidance for further efforts to obtain an effective HIV-1 attachment inhibitor.