Shifting paradigms: The resistance profile of etravirine

Journal of Antimicrobial Chemotherapy

Volumn 62, Issue 4, 2008, Pages 643-647

  Geretti, Anna Maria ^a  

^a ROYAL FREE AND UNIVERSITY COLLEGE MEDICAL SCHOOL   (United Kingdom)

Author keywords

Genotype; Mutations; Non nucleoside reverse transcriptase inhibitors

Indexed keywords

DARUNAVIR; EFAVIRENZ; ENFUVIRTIDE; ETRAVIRINE; LOPINAVIR PLUS RITONAVIR; NEVIRAPINE; PLACEBO; PROTEINASE INHIBITOR; RITONAVIR; RNA DIRECTED DNA POLYMERASE; RNA DIRECTED DNA POLYMERASE INHIBITOR;

ANTIVIRAL ACTIVITY; ANTIVIRAL RESISTANCE; ANTIVIRAL SUSCEPTIBILITY; ARTICLE; CLINICAL PRACTICE; CLINICAL TRIAL; CROSS RESISTANCE; DRUG DOSE COMPARISON; DRUG TREATMENT FAILURE; GENE MUTATION; GENOTYPE PHENOTYPE CORRELATION; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; OUTCOME ASSESSMENT; PREDICTION; TREATMENT DURATION; TREATMENT OUTCOME; VIRUS LOAD;

DRUG RESISTANCE, VIRAL; HIV INFECTIONS; HUMANS; PYRIDAZINES; REVERSE TRANSCRIPTASE INHIBITORS;

EID: 50849108264     PISSN: 03057453     EISSN: 14602091     Source Type: Journal    
DOI: 10.1093/jac/dkn248     Document Type: Article

References (24)

1. Andries K, Azijn H, Thielemans T et al. TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriplase inhibitor-resistant human immunodeficiency virus typie 1. Antimicrob Agents Chemother 2004; 48: 4680-6.
2. Vingerhoets J, Azijn H, Fransen E et al. TMC125 displays a high genetic barrier to the development of resistance: Evidence from in vitro selection experiments. J Virol 2005; 79: 12773-82.
3. Das K, Clark AD Jr, Lewi PJ et al. Roles of conformational and positional adaptability in structure-based design of TMC125-R165335 (etravirine) and related non-nucleoside reverse transcriptase inhibitors that are highly potent and effective against wild-type and drug-resistant HIV-1 variants. J Med Chem 2004; 47: 2550-60.
4. Gazzard BG, Pozniak AL, Rosenbaum W et al. An open-label assessment of TMC 125 - a new, next-generation NNHTI, for 7 days in HIV-1 infected individuals with NNRTI resistance. Acquir Immune Defic Syndr 2003; 17: F49-54.
5. Gruzdev B, Rakhmanova A, Doubovskaya E et al. A randomized, double-blind, placebo-controlled trial of TMC125 as 7-day monotherapy in antiretroviral naive, HIV-1 infected subjects. Acquir Immune Defic Syndr 2003; 17: 2487-94.
6. Woodfall B, Vingerhoets J, Pesters M et al. Impact of NNRTI and NRTI resistance on the response to the regimen of TMC125 plus two NRTIs in study TMC125-C227. In: Abstracts of the Eighth International Congress on Drug Therapy in HIV infection, Glasgow, 2006. Abstract PL5.6.
7. Nadler JP, Berger DS, Blick G et al. Efficacy and safety of etravirine (TMC125) in patients with highly resistant HIV-1: Primary 24-week analysis. Acquir Immune Defic Syndr 2007; 21: F1-10.
8. Cohen C, Steinhart C, Ward D et al. 48-week durable efficacy and safety results of TMC125 in HIV patients with NNRTI and PI resistance-study TMC125-C223. In: Abstracts of the Twelfth British HIV Association Annual Spring Conference, Brighton, 2006. Abstract P2.
9. Vingerhoets J, Peeters M, Corbett C et al. Impact of baseline resistance on the virologic response to a novel NNRTI, TMC125, in patients with extensive NNRTI and PI resistance: Analysis of study TMC125-C223. In: Abstracts of the Thirteenth Conference on Retroviruses and Opportunistic Infections, Denver, 2006. Abstract 154.
10. Cohen C, Steinhart C, Ward D et al. Efficacy and safety results at 48 weeks with the novel NNRTI, TMC125, and impact of baseline resistance on the virologic response in study TMC125-C223. In: Abstracts of the Sixteenth International AIDS Conference, Toronto, 2006. Abstract TuPE0061.
11. Vingerhoets J, Janssen K, Welkenhuysen-Gybets J et al. Impact of baseline K103N or Y181C on the virological response to the NNRTI TMC125: analysis of study TMC125-C223. In: Abstracts of the Fifteenth International HIV Drug Resistance Workshop. Antivir Ther 2006; 11: S22.
12. Madruga JV, Cahn P, Grinsztejn B et al. Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-1: 24-week results from a randomised, double-blind, placebo-controlled trial. Lancet 2007; 370: 29-38.
13. Lazzarin A, Campbell T, Clotet B et al. Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-2: 24-week results from a randomised, double-blind, placebo-controlled trial. Lancet 2007; 370: 39-48.
14. Cahn P, Haubrich R, Leider J et al. Pooled 24-week results of DUET-1 and -2: TMC125 (etravirine; ETR) vs placebo in 1203 treatment-experienced HIV-1-infected patients. In: Abstracts of the Forty-seventh Interscience Conference on Antimicrobial Agents and Chemotherapy, Chicago, 2007. Abstract H-717.
15. Haubrich R, Cahn P, Grinsztejn B et al. DUET-1: Week-48 results of a Phase III randomised double-blind trial to evaluate the efficacy and safety of TMC125 vs placebo in 612 treatment-experienced HIV-1 infected patients. In: Abstracts of the Fifteenth Conference on Retroviruses and Opportunistic Infections, Boston, 2008. Abstract 790.
16. Johnson M, Campbell T, Clotet B et al. DUET-2: Week-48 results of a Phase III randomised doublle-blind trial to evaluate the efficacy and safety of TMC125 vs placebo in 612 treatment-experienced HIV-1 infected patients. In: Abstracts of the Fifteenth Conference on Retroviruses and Opportunistic Infections, Boston, 2008. Abstract 791.
17. Schapiro JM, Vingerhoets J, Nijs S et al. Combined PI and NNRTI resistance analysis of the pooled DUET trial: Towards a regimen-based resistance interpretation. In: Abstracts of the Sixth European HIV Drug Resistance Workshop, Budapest, 2008. Abstract 46.
18. Vingerhoets J, Buelens A, Peeters M et al. Impact of baseline mutations on the virological response to TMC125 in the phase III clinical trials DUET-1 and DUET-2. In: Abstracts of the Sixteenth International HIV Drug Resistance Workshop, Barbados, 2007. Antivir Ther 2007; 12: S34.
19. Su G, Li Y, Paul A et al. In vitro selection and characterization of viruses resistant to R1206, a novel non-nucleoside reverse transcriptase inhibitor. In: Abstracts of the Sixteenth International HIV Drug Resistance Workshop, Barbados, 2007. Antivir Ther 2007; 12: S35.
20. Brillant J, Klumpp K, Swallow S et al. In vitro resistance development for a second-generation NNRTI: TMC125. In: Abstracts of the Thirteenth International HIV Drug Resistance Workshop. Antivir Ther 2004; 9: S20.
21. Tambuyzer L, Vingerhoets J, Azijn H et al. Emerging mutations in patients with virological failure on etravirine (ETR; TMC125) in the DUET-1 and DUET-2 clinical trials. In: Abstracts of the Sixth European HIV Drug Resistance Workshop, Budapest, 2008. Abstract 47.
22. Winters B, Villacian J, Van Craenenbroeck E et al. Development of Virco TYPE HIV-1 resistance analysis, including clinical cut-offs for TMC125, a new NNRTI. In: Abstracts of the Fifteenth Conference on Retroviruses and Opportunistic Infections, Boston, 2008. Abstract 873.
23. Picchio G, Vingerhoets J, Staes M et al. Prevalence of TMC125 resistance-associated mutations in a large panel of clinical isolates. In: Abstracts of the Fifteenth Conference on Retroviruses and Opportunistic Infections, Boston, 2008. Abstract 866.
24. Sungkanuparph S, Manosuthi W, Kiertiburanakul S et al. Evaluating the role of etravirine in the second-line ART after failing initial NNRTI-based regimens in a resource-limited setting. In: Abstracts of the Fifteenth Conference on Retroviruses and Opportunistic Infections, Boston, 2008. Abstract 865.