Title
TMC310911, a Novel Human Immunodeficiency Virus Type 1 Protease Inhibitor, Shows In Vitro an Improved Resistance Profile and Higher Genetic Barrier to Resistance Compared with Current Protease Inhibitors
UMMS Affiliation
Department of Biochemistry and Molecular Pharmacology
Date
12-8-2011
Document Type
Article
Medical Subject Headings
Drug Resistance, Viral; HIV Antigens; HIV Protease Inhibitors; HIV-1; Humans; Virus Replication; gag Gene Products, Human Immunodeficiency Virus
Abstract
TMC310911 is a novel human immunodeficiency virus type 1 (HIV-1) protease inhibitor (PI) structurally closely related to darunavir (DRV) but with improved virological characteristics. TMC310911 has potent activity against wild-type (WT) HIV-1 (median 50% effective concentration [EC(50)], 14 nM) and a wide spectrum of recombinant HIV-1 clinical isolates, including multiple-PI-resistant strains with decreased susceptibility to currently approved PIs (fold change [FC] in EC(50), >10). For a panel of 2,011 recombinant clinical isolates with decreased susceptibility to at least one of the currently approved PIs, the FC in TMC310911 EC(50) was
Rights and Permissions
Citation: Antimicrob Agents Chemother. 2011 Dec;55(12):5723-31. Epub 2011 Sep 6. Link to article on publisher's site