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
Department of Biochemistry and Molecular Pharmacology
Medical Subject Headings
Drug Resistance, Viral; HIV Antigens; HIV Protease Inhibitors; HIV-1; Humans; Virus Replication; gag Gene Products, Human Immunodeficiency Virus
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
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Citation: Antimicrob Agents Chemother. 2011 Dec;55(12):5723-31. Epub 2011 Sep 6. Link to article on publisher's site
Dierynck, Inge; Van Marck, Herwig; Van Ginderen, Marcia; Jonckers, Tim H. M.; Nalam, Madhavi N. L.; Schiffer, Celia A.; Raoof, Araz; Kraus, Guenter; and Picchio, Gaston, "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" (2011). Biochemistry and Molecular Pharmacology Publications and Presentations. Paper 131.