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
Dierynck, Inge Van Marck, Herwig Van Ginderen, Marcia Jonckers, Tim H. M. Nalam, Madhavi N. L. Schiffer, Celia A. Raoof, Araz Kraus, Guenter Picchio, Gaston
Citations
Student Authors
Faculty Advisor
Academic Program
UMass Chan Affiliations
Document Type
Publication Date
Subject Area
Embargo Expiration Date
Link to Full Text
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
Source
Antimicrob Agents Chemother. 2011 Dec;55(12):5723-31. Epub 2011 Sep 6. Link to article on publisher's site