Publications by authors named "Yoganand Shanmugam"
Article Synopsis
- Newer HIV-1 maturation inhibitors, like VH3739937 (VH-937), have shown promise as effective antiretroviral treatments in clinical settings.
- VH-937 features a 4-cyanopyridyl ether design that is a step up from earlier inhibitors, leading to a better antiviral profile and effectiveness against the A364V mutation, a common resistance issue.
- Due to its improved pharmacokinetic properties, VH-937 has the potential for infrequent dosing, with initial human studies supporting the possibility of once-weekly administration.
GSK3532795 (formerly BMS-955176) is a second-generation HIV-1 maturation inhibitor that has shown broad spectrum antiviral activity and preclinical PK predictive of once-daily dosing in humans. Although efficacy was confirmed in clinical trials, the observation of gastrointestinal intolerability and the emergence of drug resistant virus in a Phase 2b clinical study led to the discontinuation of GSK3532795. As part of the effort to further map the maturation inhibitor pharmacophore and provide additional structural options, the evaluation of alternates to the C-3 phenyl substituent in this chemotype was pursued.
View Article and Find Full Text PDF