-
1
-
-
0034723439
-
Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells
-
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.
-
(2000)
Science
, vol.287
, pp. 646-650
-
-
Hazuda, D.J.1
Felock, P.2
Witmer, M.3
-
2
-
-
63649143775
-
-
Isentress raltegravir, package insert, Whitehouse Station, NJ: Merck, 2007
-
Isentress (raltegravir) [package insert]. Whitehouse Station, NJ: Merck, 2007.
-
-
-
-
3
-
-
0030812190
-
Differential divalent cation requirements uncouple the assembly and catalytic reactions of human immunodeficiency virus type 1 integrase
-
Hazuda DJ, Felock PJ, Hastings JC, Pramanik B, Wolfe AL. Differential divalent cation requirements uncouple the assembly and catalytic reactions of human immunodeficiency virus type 1 integrase. J Virol 1997;71:7005-11.
-
(1997)
J Virol
, vol.71
, pp. 7005-7011
-
-
Hazuda, D.J.1
Felock, P.J.2
Hastings, J.C.3
Pramanik, B.4
Wolfe, A.L.5
-
4
-
-
0034468560
-
Repair of gaps in retroviral DNA integration intermediates
-
Yoder KE, Bushman FD. Repair of gaps in retroviral DNA integration intermediates. J Virol 2000;74:11191-200.
-
(2000)
J Virol
, vol.74
, pp. 11191-11200
-
-
Yoder, K.E.1
Bushman, F.D.2
-
5
-
-
2342541832
-
Requirement for integrase during reverse transcription of human immunodeficiency virus type-1 and the effect of cysteine mutations of integrase on its interactions with reverse transcriptase
-
Zhu K, Dobard C, Chow SA. Requirement for integrase during reverse transcription of human immunodeficiency virus type-1 and the effect of cysteine mutations of integrase on its interactions with reverse transcriptase. J Virol 2004; 78:5045-55.
-
(2004)
J Virol
, vol.78
, pp. 5045-5055
-
-
Zhu, K.1
Dobard, C.2
Chow, S.A.3
-
7
-
-
63649161204
-
-
Petry AS, Wenning LA, Laethem M, et al. Safety, tolerabililty, and pharmacokinetics after single and multiple doses of MK-0518 inhealthy subjects [abstract A-376]. In: Program and abstracts of 46th Intersci- ence Conference on Antimicrobial Agents and Chemotherapy (San Francisco). Washington, DC: American Society for Microbiology, 2006.
-
Petry AS, Wenning LA, Laethem M, et al. Safety, tolerabililty, and pharmacokinetics after single and multiple doses of MK-0518 inhealthy subjects [abstract A-376]. In: Program and abstracts of 46th Intersci- ence Conference on Antimicrobial Agents and Chemotherapy (San Francisco). Washington, DC: American Society for Microbiology, 2006.
-
-
-
-
8
-
-
33845366857
-
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
-
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 Dene Syndr 2006;43:509-15.
-
(2006)
J Acquir Immune Dene Syndr
, vol.43
, pp. 509-515
-
-
Markowitz, M.1
Morales-Ramirez, J.O.2
Nguyen, B.Y.3
-
9
-
-
63649123250
-
-
Kassahun K, Mcintosh I, Hreniuk D, et al. Absorption, metabolism, and excretion of MK-0518, a potent HIV-1 integrase inhibitor, in healthy male volunteers [abstract A-372]. In: Program and abstracts of 46th Interscience Conference on Antimicrobial Agents and Chemotherapy (San Francisco). Washington, DC: American Society for Microbiology, 2006.
-
Kassahun K, Mcintosh I, Hreniuk D, et al. Absorption, metabolism, and excretion of MK-0518, a potent HIV-1 integrase inhibitor, in healthy male volunteers [abstract A-372]. In: Program and abstracts of 46th Interscience Conference on Antimicrobial Agents and Chemotherapy (San Francisco). Washington, DC: American Society for Microbiology, 2006.
-
-
-
-
10
-
-
38349182976
-
Lack of pharmacokinetic effect of raltegravir on midazolam: In vitro/in vivo correlation
-
Iwamoto M, Kassahan K, Matthew D, et al. Lack of pharmacokinetic effect of raltegravir on midazolam: in vitro/in vivo correlation. J Clin Pharmacol 2008;48:209-14.
-
(2008)
J Clin Pharmacol
, vol.48
, pp. 209-214
-
-
Iwamoto, M.1
Kassahan, K.2
Matthew, D.3
-
11
-
-
46249087089
-
Atazanavir modestly increases plasma levels of raltegravir in healthy adults
-
Iwamoto M, Wenning L, Mistry GC, et al. Atazanavir modestly increases plasma levels of raltegravir in healthy adults. Clin Infect Dis 2008;47:137-40.
-
(2008)
Clin Infect Dis
, vol.47
, pp. 137-140
-
-
Iwamoto, M.1
Wenning, L.2
Mistry, G.C.3
-
12
-
-
63649108083
-
-
Wenning L, Friedman K, Kost J, et al. Lack of a significant drug interaction between MK-0518 and tenotbvir disoproxil fumarate [abstract A-0375]. In: Program and abstracts of 46th Interscience Conference on Antimicrobial Agents and Chemotherapy (San Francisco). Washington, DC: American Society for Microbiology, 2006.
-
Wenning L, Friedman K, Kost J, et al. Lack of a significant drug interaction between MK-0518 and tenotbvir disoproxil fumarate [abstract A-0375]. In: Program and abstracts of 46th Interscience Conference on Antimicrobial Agents and Chemotherapy (San Francisco). Washington, DC: American Society for Microbiology, 2006.
-
-
-
-
13
-
-
63649104573
-
-
Iwamoto M. Wenning L, Petry A, et al. Minimal effect of ritonavir and efavirenz on the pharmacokinetics of MK-0518 [abstract A-0373]. In: Program and abstracts of 46th Interscience Conference on Antimicrobial Agents and Chemotherapy (San Francisco). Washington, DC: American Society for Microbiology, 2006.
-
Iwamoto M. Wenning L, Petry A, et al. Minimal effect of ritonavir and efavirenz on the pharmacokinetics of MK-0518 [abstract A-0373]. In: Program and abstracts of 46th Interscience Conference on Antimicrobial Agents and Chemotherapy (San Francisco). Washington, DC: American Society for Microbiology, 2006.
-
-
-
-
14
-
-
63649103710
-
-
Anderson M, Kakuda T, Miller J, et al. Pharmacokinetic evaluation of non-nucleoside reverse transcriptase inhibitor (NNRTI) TMC125 and integrase inhibitor (InSTI) raltegravir (RAL) in healthy subjects [abstract TuPDB02[. In: Program and abstracts of the 4th International AIDS Society Conference on HIV Pathogenesis, Treatment, and Prevention (Sydney, Australia). 2007.
-
Anderson M, Kakuda T, Miller J, et al. Pharmacokinetic evaluation of non-nucleoside reverse transcriptase inhibitor (NNRTI) TMC125 and integrase inhibitor (InSTI) raltegravir (RAL) in healthy subjects [abstract TuPDB02[. In: Program and abstracts of the 4th International AIDS Society Conference on HIV Pathogenesis, Treatment, and Prevention (Sydney, Australia). 2007.
-
-
-
-
15
-
-
63649138981
-
-
Wenning L, Hanley H, Stone J, et al. Effect of tipranavir + ritonavir on pharmacokinetics of MK-0518 [abstract A-0374]. In: Program and abstracts of 46th Interscience Conference on Antimicrobial Agents and Chemotherapy (San Francisco). Washington, DC: American Society for Microbiology, 2006.
-
Wenning L, Hanley H, Stone J, et al. Effect of tipranavir + ritonavir on pharmacokinetics of MK-0518 [abstract A-0374]. In: Program and abstracts of 46th Interscience Conference on Antimicrobial Agents and Chemotherapy (San Francisco). Washington, DC: American Society for Microbiology, 2006.
-
-
-
-
16
-
-
63649126616
-
-
Khanlou H, Allavena C, Billaud E, McKellar M, Reliquet V. Development of hepatic cytolysis after switching from enfuvirtide to raltegravir in virologically suppressed patients treated with tipranvir/rito- navir [abstract TuPE0087|. In: Program and abstracts of the XVII International AIDS Conference (Mexico City). 2008.
-
Khanlou H, Allavena C, Billaud E, McKellar M, Reliquet V. Development of hepatic cytolysis after switching from enfuvirtide to raltegravir in virologically suppressed patients treated with tipranvir/rito- navir [abstract TuPE0087|. In: Program and abstracts of the XVII International AIDS Conference (Mexico City). 2008.
-
-
-
-
17
-
-
34748860363
-
Rapid and durable an- tiretroviral effect of the HIV-1 integrase inhibitor raltegravir as part of combination therapy in treatment-naive patients with HIV-1 infection: Results of a 48-week controlled study
-
Markowitz M, Nguyen BY, Gotuzzo E, et al. Rapid and durable an- tiretroviral effect of the HIV-1 integrase inhibitor raltegravir as part of combination therapy in treatment-naive patients with HIV-1 infection: results of a 48-week controlled study. J Acquir Immune Dene Syndr 2007;46:125-33.
-
(2007)
J Acquir Immune Dene Syndr
, vol.46
, pp. 125-133
-
-
Markowitz, M.1
Nguyen, B.Y.2
Gotuzzo, E.3
-
18
-
-
63649102403
-
-
Markowitz M, Nguyen B-Y, Gotuzzo E, et al. Sustained antiretroviral efficacy of raltegravir as part of combination ART in treatment-naive HIV-1-infected patients: 96-week data [abstract TuAB0102J. In: Program and abstracts of the XVII International AIDS Conference (Mexico City). 2008.
-
Markowitz M, Nguyen B-Y, Gotuzzo E, et al. Sustained antiretroviral efficacy of raltegravir as part of combination ART in treatment-naive HIV-1-infected patients: 96-week data [abstract TuAB0102J. In: Program and abstracts of the XVII International AIDS Conference (Mexico City). 2008.
-
-
-
-
19
-
-
63649133604
-
-
Lennox J, Dejesus E, Lazzarin A, et al. STARTMRK, a phase III study of the safety & efficacy of raltegravir (RAL)-based vs efavirenz (EFV)- based combination therapy in treatment-naive HIV-infected patients [abstract H-896a[. In: Program and abstracts of the 48th Interscience Conference on Antimicrobial Agents and Chemotherapy (Washington, DC). Washington, DC: American Society for Microbiology, 2008.
-
Lennox J, Dejesus E, Lazzarin A, et al. STARTMRK, a phase III study of the safety & efficacy of raltegravir (RAL)-based vs efavirenz (EFV)- based combination therapy in treatment-naive HIV-infected patients [abstract H-896a[. In: Program and abstracts of the 48th Interscience Conference on Antimicrobial Agents and Chemotherapy (Washington, DC). Washington, DC: American Society for Microbiology, 2008.
-
-
-
-
20
-
-
34147136222
-
Safety and efficacy of the HIV-1 integrase inhibitor raltegravir (MK-0518) in treatment-experienced patients with multidrug-resistant virus: A phase II randomised controlled trial
-
Grinsztejn B, Nguyen BY, Katlama C, et al. Safety and efficacy of the HIV-1 integrase inhibitor raltegravir (MK-0518) in treatment-experienced patients with multidrug-resistant virus: a phase II randomised controlled trial. Lancet 2007;369:1261-9.
-
(2007)
Lancet
, vol.369
, pp. 1261-1269
-
-
Grinsztejn, B.1
Nguyen, B.Y.2
Katlama, C.3
-
21
-
-
63649156971
-
-
Grinsztejn B, Nguyen B, Katlama C, et al. 48-Week efficacy and safety of MK-0518, a novel HIV-1 integrase inhibitor, in patients with triple- class resistant virus [abstract H-713], In: Program and abstracts of 47th Interscience Conference on Antimicrobial Agents and Chemotherapy (Chicago). Washington, DC: American Society for Microbiology, 2007.
-
Grinsztejn B, Nguyen B, Katlama C, et al. 48-Week efficacy and safety of MK-0518, a novel HIV-1 integrase inhibitor, in patients with triple- class resistant virus [abstract H-713], In: Program and abstracts of 47th Interscience Conference on Antimicrobial Agents and Chemotherapy (Chicago). Washington, DC: American Society for Microbiology, 2007.
-
-
-
-
22
-
-
47949120697
-
Raltegravir with optimized background therapy for resistant HIV-1 infection
-
Steigbigel R, Cooper D, Kumar P, et al. Raltegravir with optimized background therapy for resistant HIV-1 infection. N Engl J Med 2008;359:339-54.
-
(2008)
N Engl J Med
, vol.359
, pp. 339-354
-
-
Steigbigel, R.1
Cooper, D.2
Kumar, P.3
-
23
-
-
47949114939
-
Subgroup and resistance analyses of raltegravir for resistant HIV-1 infection
-
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.
-
(2008)
N Engl J Med
, vol.359
, pp. 355-365
-
-
Cooper, D.A.1
Steigbigel, R.T.2
Gatell, J.M.3
-
24
-
-
37349120701
-
Antiretroviral therapy with the integrase inhibitor raltegravir alters decay kinetics of HIV, significantly reducing the second phase
-
Murray JM, Emery S, Kelleher AD, et al. Antiretroviral therapy with the integrase inhibitor raltegravir alters decay kinetics of HIV, significantly reducing the second phase. AIDS 2007;21:2315-21.
-
(2007)
AIDS
, vol.21
, pp. 2315-2321
-
-
Murray, J.M.1
Emery, S.2
Kelleher, A.D.3
-
25
-
-
50949112147
-
Outcomes of multidrug-resistant patients switched from enfuvirtide to raltegravir within a virologically suppressive regimen
-
Harris M, Larsen G, Montaner J. Outcomes of multidrug-resistant patients switched from enfuvirtide to raltegravir within a virologically suppressive regimen. AIDS 2008;22:1224-6.
-
(2008)
AIDS
, vol.22
, pp. 1224-1226
-
-
Harris, M.1
Larsen, G.2
Montaner, J.3
-
26
-
-
63649148924
-
-
Towner W, Klein D, Follansbee S, et al. Pilot study of switching enfuvirtide to raltegravir in HIV-1 positive patients well controlled on an enfuvirtide-based regimen [abstract TuPE0115[. In: Program and abstracts of the XVII International AIDS Conference (Mexico City), 2008.
-
Towner W, Klein D, Follansbee S, et al. Pilot study of switching enfuvirtide to raltegravir in HIV-1 positive patients well controlled on an enfuvirtide-based regimen [abstract TuPE0115[. In: Program and abstracts of the XVII International AIDS Conference (Mexico City), 2008.
-
-
-
-
27
-
-
63649084263
-
-
Talbot A, Machouf N, Thomas R, et al. Retrospective analysis of a switch from enfuvirtide to raltegravir in patients with undetectable viral load: efficacy and safety at 12 weeks in a Montreal cohort [abstract TuPEOl 12]. In: Program and abstracts of the XVII International AIDS Conference (Mexico City). 2008.
-
Talbot A, Machouf N, Thomas R, et al. Retrospective analysis of a switch from enfuvirtide to raltegravir in patients with undetectable viral load: efficacy and safety at 12 weeks in a Montreal cohort [abstract TuPEOl 12]. In: Program and abstracts of the XVII International AIDS Conference (Mexico City). 2008.
-
-
-
-
28
-
-
63649136444
-
-
Merck Research Laboratories. Briefing Document-FDA Antiviral Drugs Advisory Committee Meeting. Isentress (raltegravir) 400 mg for treatment of HIV (NDA 22-145). 5 September 2007. Available at http: //www.fda.gov/ohrms/ dockets/ac/07/briefing/2007-4314bl-01-Merck.pdf. Accessed 10 February 2009.
-
Merck Research Laboratories. Briefing Document-FDA Antiviral Drugs Advisory Committee Meeting. Isentress (raltegravir) 400 mg for treatment of HIV (NDA 22-145). 5 September 2007. Available at http: //www.fda.gov/ohrms/ dockets/ac/07/briefing/2007-4314bl-01-Merck.pdf. Accessed 10 February 2009.
-
-
-
-
29
-
-
49849103584
-
Severe rhabdomyol- ysis associated with raltegravir use
-
Zembower T, Gerzenshten L, Colemen K, Palella F. Severe rhabdomyol- ysis associated with raltegravir use. AIDS 2008;22:1382-4.
-
(2008)
AIDS
, vol.22
, pp. 1382-1384
-
-
Zembower, T.1
Gerzenshten, L.2
Colemen, K.3
Palella, F.4
-
30
-
-
63649139412
-
Exacerbation of depression associated with starting raltegravir: A report of four cases
-
Harris M, Larsen G, Montaner J. Exacerbation of depression associated with starting raltegravir: a report of four cases. AIDS 2008;22:1890-2.
-
(2008)
AIDS
, vol.22
, pp. 1890-1892
-
-
Harris, M.1
Larsen, G.2
Montaner, J.3
-
31
-
-
12944270496
-
HIV-1 integrase inhibitors that compete with the target DNA substrate define a unique strand transfer conformation for integrase
-
Elspeth A, Felock P, Wolfe A, et al. HIV-1 integrase inhibitors that compete with the target DNA substrate define a unique strand transfer conformation for integrase. Proc Natl Acad Sci 2000;97:11244-9.
-
(2000)
Proc Natl Acad Sci
, vol.97
, pp. 11244-11249
-
-
Elspeth, A.1
Felock, P.2
Wolfe, A.3
-
32
-
-
37249065868
-
Resistance to the HIV- integrase inhibitor raltegravir: Analysis of protocol 005, a phase II study in patients with triple-class resistant HIV-1 infection
-
Hazuda DJ, Miller MD, Nguyen BY, Zhao J. Resistance to the HIV- integrase inhibitor raltegravir: analysis of protocol 005, a phase II study in patients with triple-class resistant HIV-1 infection. Antiviral Therapy 2007; 12;S10.
-
(2007)
Antiviral Therapy
, vol.12
-
-
Hazuda, D.J.1
Miller, M.D.2
Nguyen, B.Y.3
Zhao, J.4
-
33
-
-
42049119625
-
Mutations associated with failure of raltegravir treatment affect integrase sensitivity to the inhibitor in vitro
-
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;51:1351-8.
-
(2008)
Antimicrob Agents Chemother
, vol.51
, pp. 1351-1358
-
-
Malet, I.1
Delelis, O.2
Valantin, M.A.3
-
34
-
-
63649132054
-
-
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]. In: Program and abstracts of the 14th Conference on Retroviruses and Opportunistic Infections (Los Angeles). Washington, DC: American Society for Microbiology, 2007.
-
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]. In: Program and abstracts of the 14th Conference on Retroviruses and Opportunistic Infections (Los Angeles). Washington, DC: American Society for Microbiology, 2007.
-
-
-
-
35
-
-
63649099135
-
-
DeJesus E, Cohen C, Elion R, et al. First report of raltegravir (RAL, MK-0518) use after virologic rebound on elvitegravir (EVT, GS 9137) [abstract TuPEB032]. In: Program and abstracts of the 4th International AIDS Society Conference on HIV Pathogenesis, Treatment, and Prevention (Sydney, Australia). 2007.
-
DeJesus E, Cohen C, Elion R, et al. First report of raltegravir (RAL, MK-0518) use after virologic rebound on elvitegravir (EVT, GS 9137) [abstract TuPEB032]. In: Program and abstracts of the 4th International AIDS Society Conference on HIV Pathogenesis, Treatment, and Prevention (Sydney, Australia). 2007.
-
-
-
-
36
-
-
40549125135
-
Resistance and cross-resistance to first generation integrase inhibitors: Insights from a phase II study of elvitegravir (GS-9137)
-
McColl DJ, Fransen S, Gupta S, et al. Resistance and cross-resistance to first generation integrase inhibitors: insights from a phase II study of elvitegravir (GS-9137). Antiviral Therapy 2007;12;S11.
-
(2007)
Antiviral Therapy
, vol.12
-
-
McColl, D.J.1
Fransen, S.2
Gupta, S.3
-
37
-
-
67649538485
-
-
Panel on Antiretroviral Guidelines tor Adults and Adolescents, Available at, Accessed 3 November 2008
-
Panel on Antiretroviral Guidelines tor Adults and Adolescents. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents. Department of Health and Human Services. 2008:1-128. Available at http://www.aidsinfo.nih.gov/Content Files/AdultandAdolescentGL.pdf. Accessed 3 November 2008.
-
(2008)
Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents
, pp. 1-128
-
-
-
38
-
-
63649100891
-
-
Eron J, Andrade J, Zajdenverg R, et al. Switching from stable lopinavir/ ritonavir-based to raltegravir-based combination ART resulted in a superior lipid profile at week 12 but did not demonstrate non-inferior virologic efficacy at week 24 [ abstract 70aLB ]. In: Program and abstracts of the 16th Conference on Retroviruses and Opportunistic Agents (Montreal). 2009.
-
Eron J, Andrade J, Zajdenverg R, et al. Switching from stable lopinavir/ ritonavir-based to raltegravir-based combination ART resulted in a superior lipid profile at week 12 but did not demonstrate non-inferior virologic efficacy at week 24 [ abstract 70aLB ]. In: Program and abstracts of the 16th Conference on Retroviruses and Opportunistic Agents (Montreal). 2009.
-
-
-
|