Inibidor de integrase é uma classe de medicamentos para o tratamento da infecção pelo HIV.
Ação Eles atuam impedindo a replicação do vírus ao bloquear a atividade da enzima integrase, que tem a capacidade de inserir o DNA viral ao DNA humano.O primeiro medicamento desta classe foi o raltegravir, aprovado em 2007 pela FDA.
Ligações externas Cooper D, Gatell J, Rockstroh J, et al. Results of BENCHMRK-1, a phase III study evaluating the efficacy and safety of MK-0518, a novel HIV-1 integrase inhibitor, in patients with triple-class resistant virus. Abstract 105aLB, 14th CROI 2007, Los Angeles. DeJesus E, Berger D, Markowitz M, et al. Antiviral activity, pharmacokinetics, and dose response of the HIV-1 integrase inhibitor GS-9137 (JTK-303) in treatment-naive and treatment-experienced patients. J AIDS 2006, 43:1-5. PMID 16936557 Hazuda DJ, Felock P, Witmer M, et al. Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells. Science 2000, 287:646-50. PMID 10649997 Jones G, Ledford RM, yu F, et al. In vitro resistance profile of HIV-1 mutants selected by the HIV-1 integrase inhibitor, GS-9137 (JTK-303). Abstract 627, 14th CROI 2007, Los Angeles. Lataillade M, Kozal MJ. The hunt for HIV-1 integrase inhibitors. AIDS Patient Care and STDs 2006, 20:489-501. PMID 16839248 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 AIDS 2006, 43:509-515. PMID 17133211 Nair V. HIV integrase as a target for antiviral chemotherapy. Rev Med Virol 2002, 12:179-93. PMID 11987143 Pommier Y, Johnson AA, Marchand C. Integrase inhibitors to treat HIV/AIDS. Nat Rev Drug Discov 2005, 4:236-48. PMID 15729361 Reddy S, Min S, Borland J, et al. A double-blind, parallel, randomized, placebo-controlled, single and repeat dose-escalation study to investigate the safety, tolerability, and pharmacokinetics of the HIV integrase inhibitor GSK364735 in healthy subjects. Abstract 562, 14th CROI 2007, Los Angeles. Sato M, Motomura T, Aramaki H, et al. Novel HIV-1 integrase inhibitors derived from quinolone antibiotics. J Med Chem 2006, 49:1506-8. PMID 16509568 Steigbigel R, Kumar R, Eron J, et al. Results of BENCHMRK-2, a phase III study evaluating the efficacy and safety of MK-0518, a novel HIV-1 integrase inhibitor, in patients with triple-class resistant virus. Abstract 105bLB, 14th CROI 2007, Los Angeles. Zolopa A, Mullen M, Berger D, et al. The HIV integrase inhibitor GS9137 demonstrates potent ARV activity in treatment-experienced patients. Abstract 143 LB, 14th CROI 2007, Los Angeles.
Categoria:Inibidores de integrase