Raltegravir has no residual antiviral activity in vivo against HIV-1 with resistance-associated mutations to this drug

Journal of Antimicrobial Chemotherapy

Volumn 64, Issue 5, 2009, Pages

  Wirden, Marc ^a   Simon, Anne ^a   Schneider, Luminita ^a   Tubiana, Roland ^a   Malet, Isabelle ^a   Ait Mohand, Hocine ^a   Peytavin, Gilles ^b   Katlama, Christine ^a   Calvez, Vincent ^a   Marcelin, Anne Genevieve ^a  

^a PITIÉ SALPÊTRIÈRE HOSPITAL   (France)

^b BICHAT HOSPITAL   (France)

Author keywords

Integrase inhibitor; N155H; Q148H; Residual activity

Indexed keywords

ABACAVIR; ATAZANAVIR; DARUNAVIR PLUS RITONAVIR; EMTRICITABINE; ETRAVIRINE; INTEGRASE; LAMIVUDINE; RALTEGRAVIR; TENOFOVIR; ZIDOVUDINE; 2 PYRROLIDONE DERIVATIVE; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT;

ANTIVIRAL ACTIVITY; ANTIVIRAL RESISTANCE; ARTICLE; CD4 LYMPHOCYTE COUNT; CLINICAL ARTICLE; COST BENEFIT ANALYSIS; DRUG BLOOD LEVEL; GENOTYPE; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1 INFECTION; RISK BENEFIT ANALYSIS; SALVAGE THERAPY; VIRUS LOAD; VIRUS MUTATION; DRUG EFFECT; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; MISSENSE MUTATION; RETROSPECTIVE STUDY; VIROLOGY;

ANTI-HIV AGENTS; DRUG RESISTANCE, VIRAL; HIV INFECTIONS; HIV-1; HUMANS; MUTATION, MISSENSE; PYRROLIDINONES; RETROSPECTIVE STUDIES; VIRAL LOAD;

EID: 73949084442     PISSN: 03057453     EISSN: 14602091     Source Type: Journal    
DOI: 10.1093/jac/dkp310     Document Type: Article

References (11)

1. Steigbigel RT, Cooper DA, Kumar PN et al. Raltegravir with optimized background therapy for resistant HIV-1 infection. N Engl J Med 2008; 359: 339-54.
2. Cooper DA, Steigbigel RT, Gatell JM et al. Subgroup and resistance analyses of raltegravir for resistant HIV-1 infection. N Engl J Med 2008; 359: 355-65.
3. Malet I, Delelis O, Valantin MA et al. Mutations associated with failure of raltegravir treatment affect integrase sensitivity to the inhibitor in vitro. Antimicrob Agents Chemother 2008; 52: 1351-8.
4. Miller MD, Danovich RM, Ke Y et al. Longitudinal analysis of resistance to the HIV-1 integrase inhibitor raltegravir: results from P005 a Phase II study in treatment-experienced patients. In: Abstracts of the Seventeeth International HIV Drug Resistance Workshop: Basic Principles & Clinical Implications, Sitges, Spain, 2008. Abstract 6. Antivir Ther 2008; 13 Suppl 3: A8.
5. Canducci F, Sampaolo M, Marinozzi MC et al. Dynamic patterns of human immunodeficiency virus type 1 integrase gene evolution in patients failing raltegravir-based salvage therapies. AIDS 2009; 23: 455-60.
6. Malet I, Delelis O, Soulie C et al. Quasispecies variant dynamics during emergence of resistance to raltegravir in HIV-1-infected patients. J Antimicrob Chemother 2009; 63: 795-804.
7. Wirden M, Simon A, Schneider L et al. Interruption of nonnucleoside reverse transcriptase inhibitor (NNRTI) therapy for 2 months has no effect on levels of human immunodeficiency virus type 1 in plasma of patients harboring viruses with mutations associated with resistance to NNRTIs. J Clin Microbiol 2003; 41: 2713-5.
8. Delelis O, Malet I, Na L et al. The G140S mutation in HIV integrases from raltegravir-resistant patients rescues catalytic defect due to the resistance Q148H mutation. Nucleic Acids Res 2009; 37: 1193-201.
9. Markowitz M, Morales-Ramirez JO, Nguyen BY et al. Antiretroviral activity, pharmacokinetics, and tolerability of MK-0518, a novel inhibitor of HIV-1 integrase, dosed as monotherapy for 10 days in treatment-naive HIV-1-infected individuals. J Acquir Immune Defic Syndr 2006; 43: 509-15.
10. Hatano H, Lampiris H, Gupta S et al. Long-term evolution of integrase resistance during failure of integrase inhibitor-based ART. In: Abstracts of the Sixteenth Conference on Retroviruses and Opportunistic Infections, Montréal, Canada, 2009. Abstract 621. Foundation for Retrovirology and Human Health, Alexandria, VA, USA. http://www.retroconference.org/AbstractSearch/Default.aspx?Conf=18 (23 July 2009, date last accessed).
11. Deeks SG, Martin JN. Partial treatment interruptions. Curr Opin HIV AIDS 2007; 2: 46-55.