Andrew Mulato, Eric Lansdon, Ron Aoyama, Johannes Voigt, Michael Lee, Albert Liclican, Gary Lee, Eric Singer, Brian Stafford, Ruoyu Gong, Bernard Murray, Julie Chan, Johnny Lee, Yili Xu, Shekeba Ahmadyar, Ana Gonzalez, Aesop Cho, George J Stepan, Uli Schmitz, Brian Schultz, Bruno Marchand, Boris Brumshtein, Ruth Wang, Helen Yu, Tomas Cihlar, Lianhong Xu, Stephen R Yant
Protease inhibitors (PIs) remain an important component of antiretroviral therapy for the treatment of HIV-1 infection due to their high genetic barrier to resistance development. Nevertheless, the two most commonly prescribed HIV PIs, atazanavir and darunavir, still require co-administration with a pharmacokinetic boosting agent to maintain sufficient drug plasma levels which can lead to undesirable drug-drug interactions. Herein, we describe GS-9770, a novel investigational non-peptidomimetic HIV PI with unboosted once-daily oral dosing potential due to improvements in its metabolic stability and its pharmacokinetic properties in preclinical animal species...
February 21, 2024: Antimicrobial Agents and Chemotherapy