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Drug Evaluations

Raltegravir as antiretroviral therapy in HIV/AIDS

, MD FRCPC & , MSc MD FRCPC

Bibliography

  • HIV/AIDS. Fact sheet 360. Geneva, Switzerland; 2011. Available from: http://www.who.int/mediacentre/factsheets/fs360/en/index.html [Accessed 30 August 2013]
  • Consolidated guidelines on the use of antiretroviral drugs for treating and preventing HIV infection. Geneva, Switzerland; 2013. Available from: http://apps.who.int/iris/bitstream/10665/85321/1/9789241505727_eng.pdf [Accessed 30 August 2013]
  • European guidelines for treatment of HIV infected adults in europe. english version 7.1. Brussels, Belgium; 2013. Available from: http://www.eacsociety.org/Portals/0/Guidelines_Online_131014.pdf [Accessed 04 November 2013]
  • Recommendations on integrase inhibitor use in antiretroviral treatment-naïve HIV-infected individuals from the HHS panel on antiretroviral guidelines for adults and adolescents. Bethesda, Maryland; 2013. Available from: http://aidsinfo.nih.gov/news/1392/hhs-panel-on-antiretroviral-guidelines-for-adults-and-adolescents-updates-recommendations-on-insti-based-regimens-for-art-naive-individuals [Accessed 13 November 2013]
  • Richman DD, Morton SC, Wrin T, et al. The prevalence of antiretroviral drug resistance in the united states. AIDS 2004;18:1393-401
  • Drescher SM, von Wyl V, Yang WL, et al. Treatment-naive individuals are the major source of transmitted HIV-1 drug resistance in men who have sex with men in the swiss HIV cohort study. Clin Infect Dis 2013; [Epub ahead of print]
  • Viani RM, Peralta L, Aldrovandi G, et al. Prevalence of primary HIV-1 drug resistance among recently infected adolescents: a multicenter adolescent medicine trials network for HIV/AIDS interventions study. J Infect Dis 2006;194:1505-9
  • Torres TS, Cardoso SW, Velasque LS, et al. Incidence rate of modifying or discontinuing first combined antiretroviral therapy regimen due to toxicity during the first year of treatment stratified by age. Braz J Infect Dis 2013; [Epub ahead of print]
  • Cardoso SW, Grinsztejn B, Velasque L, et al. Incidence of modifying or discontinuing first HAART regimen and its determinants in a cohort of HIV-infected patients from Rio De Janeiro. Brazil. AIDS Res Hum Retroviruses 2010;26(8):865-74
  • Cicconi P, Cozzi-Lepri A, Castagna A, et al. Insights into reasons for discontinuation according to year of starting first regimen of highly active antiretroviral therapy in a cohort of antiretroviral-naïve patients. HIV Med 2010;11:104-13
  • Rodger AJ, Lodwick R, Schechter M, et al. Mortality in well controlled HIV in the continuous antiretroviral therapy arms of the SMART and ESPRIT trials compared with the general population. AIDS 2013;27:973-9
  • Bavinger C, Bendavid E, Niehaus K, et al. Risk of cardiovascular disease from antiretroviral therapy for HIV: a systematic review. PLoS One 2013;8:e59551
  • Assoumou L, Katlama C, Viard JP, et al. Changes in bone mineral density over a 2-year period in HIV-1-infected men under combined antiretroviral therapy with osteopenia. AIDS 2013;27:2425-30
  • Short CE, Shaw SG, Fisher MJ, et al. Prevalence of and risk factors for osteoporosis and fracture among a male HIV-infected population in the UK. Int J STD AIDS 2013; [Epub ahead of print]
  • Calza L. Renal toxicity associated with antiretroviral therapy. HIV Clin Trials 2012;13:189-211
  • Arribas JR, Eron J. Advances in antiretroviral therapy. Curr Opin HIV AIDS 2013;8:341-9
  • Sax PE, DeJesus E, Mills A, et al. Co-formulated elvitegravir, cobicistat, emtricitabine, and tenofovir versus co-formulated efavirenz, emtricitabine, and tenofovir for initial treatment of HIV-1 infection: a randomised, double-blind, phase 3 trial, analysis of results after 48 weeks. Lancet 2012;379:2439-48
  • DeJesus E, Rockstroh JK, Henry K, et al. Co-formulated elvitegravir, cobicistat, emtricitabine, and tenofovir disoproxil fumarate versus ritonavir-boosted atazanavir plus co-formulated emtricitabine and tenofovir disoproxil fumarate for initial treatment of HIV-1 infection: A randomised, double-blind, phase 3, non-inferiority trial. Lancet 2012;379:2429-38
  • Cahn P, Pozniak AL, Mingrone H, et al. Dolutegravir versus raltegravir in antiretroviral-experienced, integrase-inhibitor-naive adults with HIV: week 48 results from the randomised, double-blind, non-inferiority SAILING study. Lancet 2013;382:700-8
  • Raffi F, Rachlis A, Stellbrink HJ, et al. Once-daily dolutegravir versus raltegravir in antiretroviral-naive adults with HIV-1 infection: 48 week results from the randomised, double-blind, non-inferiority SPRING-2 study. Lancet 2013;381:735-43
  • Isentress (raltegravir). FDA highlights of prescribing information. Washington, DC; 2013. Available from: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022145s029lbl.pdf [Accessed 04 November 2013]
  • Isentress (raltegravir). London, UK; 2013. Available from: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Summary_for_the_public/human/000860/WC500037406.pdf [Accessed 04 November 2013]
  • Van Maele B, Debyser Z. HIV-1 integration: an interplay between HIV-1 integrase, cellular and viral proteins. AIDS Rev 2005;7:26-43
  • 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
  • Lataillade M, Kozal MJ. The hunt for HIV-1 integrase inhibitors. AIDS Patient Care STDS 2006 Jul;20:489-501
  • Cocohoba J, Dong BJ. Raltegravir: the first HIV integrase inhibitor. Clin Ther 2008;30:1747-65
  • Summa V, Petrocchi A, Bonelli F, et al. Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection. J Med Chem 2008;51:5843-55
  • Evering TH, Markowitz M. Raltegravir: an integrase inhibitor for HIV-1. Expert Opin Investig Drugs 2008;14:413-22
  • Iwamoto M, Wenning LA, Petry AS, et al. Safety, tolerability, and pharmacokinetics of raltegravir after single and multiple doses in healthy subjects. Clin Pharmacol Ther 2008;83:293-9
  • 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
  • Rizk ML, Hang Y, Luo WL, et al. Pharmacokinetics and pharmacodynamics of once-daily versus twice-daily raltegravir in treatment-naive HIV-infected patients. Antimicrob Agents Chemother 2012;56:3101-6
  • Wohl DA, Dumond JB, Blevins S, et al. Raltegravir pharmacokinetics in treatment-naive patients is not influenced by race: results from the raltegravir early therapy in african-americans living with HIV (REAL) study. Antimicrob Agents Chemother 2013;57:784-8
  • Brainard DM, Friedman EJ, Jin B, et al. Effect of low-, moderate-, and high-fat meals on raltegravir pharmacokinetics. J Clin Pharmacol 2011;51:422-7
  • Kassahun K, McIntosh I, Cui D, et al. Metabolism and disposition in humans of raltegravir (MK-0518), an anti-AIDS drug targeting the human immunodeficiency virus 1 integrase enzyme. Drug Metab Dispos 2007;35:1657-63
  • Iwamoto M, Hanley WD, Petry AS, et al. Lack of a clinically important effect of moderate hepatic insufficiency and severe renal insufficiency on raltegravir pharmacokinetics. Antimicrob Agents Chemother 2009;53:1747-52
  • Barau C, Furlan V, Yazdanpanah Y, et al. Characterization of binding of raltegravir to plasma proteins. Antimicrob Agents Chemother 2013;57:5147-50
  • Yilmaz A, Gisslen M, Spudich S, et al. Raltegravir cerebrospinal fluid concentrations in HIV-1 infection. PLoS One 2009;4:e6877
  • Antoniou T, Hasan S, Loutfy MR, et al. Pharmacokinetics of maraviroc, raltegravir, darunavir, and etravirine in the semen of HIV-infected men. J Acquir Immune Defic Syndr 2013;62:e58-60
  • Miller M, Witmer M, Stillmock K, et al. Biochemical and antiviral activity of MK-0518, a potent HIV integrase inhibitor [abstract THAA0302]. 16th International AIDS Conference; 13 – 18 August 2006
  • Nicastri E, Tommasi C, Abbate I, et al. Effect of raltegravir on the total and unintegrated proviral HIV DNA during raltegravir-based HAART. Antivir Ther 2011;16:797-803
  • Andrade A, Rosenkranz SL, Cillo AR, et al. Three distinct phases of HIV-1 RNA decay in treatment-naive patients receiving raltegravir-based antiretroviral therapy: ACTG A5248. J Infect Dis 2013;208:884-91
  • Lennox JL, DeJesus E, Lazzarin A, et al. Safety and efficacy of raltegravir-based versus efavirenz-based combination therapy in treatment-naive patients with HIV-1 infection: a multicentre, double-blind randomised controlled trial. Lancet 2009;374:796-806
  • Peterson K, Ruelle J, Vekemans M, et al. The role of raltegravir in the treatment of HIV-2 infections: evidence from a case series. Antivir Ther 2012;17:1097-100
  • Molto J, Valle M, Back D, et al. Plasma and intracellular (peripheral blood mononuclear cells) pharmacokinetics of once-daily raltegravir (800 milligrams) in HIV-infected patients. Antimicrob Agents Chemother 2011;55:72-5
  • Markowitz M, Nguyen BY, Gotuzzo E, et al. Sustained antiretroviral effect of raltegravir after 96 weeks of combination therapy in treatment-naive patients with HIV-1 infection. J Acquir Immune Defic Syndr 2009;52:350-6
  • 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
  • Eron JJ Jr, Rockstroh JK, Reynes J, et al. Raltegravir once daily or twice daily in previously untreated patients with HIV-1: a randomised, active-controlled, phase 3 non-inferiority trial. Lancet Infect Dis 2011;11:907-15
  • Krishna R, Rizk ML, Schulz V, et al. A single dose food effect study of raltegravir (RAL) formulations. PE10/17. 14th European AIDS Conference; 16 – 19 October 2013
  • Wenning LA, Hanley WD, Brainard DM, et al. Effect of rifampin, a potent inducer of drug-metabolizing enzymes, on the pharmacokinetics of raltegravir. Antimicrob Agents Chemother 2009;53:2852-6
  • Iwamoto M, Wenning LA, Nguyen BY, et al. Effects of omeprazole on plasma levels of raltegravir. Clin Infect Dis 2009;48:489-92
  • Markowitz M, Nguyen BY, Gotuzzo E, et al. Rapid and durable antiretroviral 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 Defic Syndr 2007;46:125-33
  • 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
  • Yazdanpanah Y, Fagard C, Descamps D, et al. High rate of virologic suppression with raltegravir plus etravirine and darunavir/ritonavir among treatment-experienced patients infected with multidrug-resistant HIV: results of the ANRS 139 TRIO trial. Clin Infect Dis 2009;49:1441-9
  • Taiwo B, Zheng L, Gallien S, et al. Efficacy of a nucleoside-sparing regimen of darunavir/ritonavir plus raltegravir in treatment-naive HIV-1-infected patients (ACTG A5262). AIDS 2011;25:2113-22
  • Bedimo R, Drechsler H, Cutrell J, et al. RADAR study: Week 48 safety and efficacy of raltegravir combined with boosted darunavir compared to tenofovir/emtricitabine combined with boosted darunavir in antiretroviral-naive patients: Impact on bone health [abstract WEPE5]. 127th IAS Conference on HIV Pathogenesis, Treatment and Prevention; 30 June – 3 July 2013
  • Study of darunavir/r + tenofovir/emtricitabine vs. darunavir/r + raltegravir in HIV-infected antiretroviral naïve subjects (ANRS 143-NEAT001). Nantes, France; 2013. Available from: http://clinicaltrials.gov/show/NCT01066962
  • Messiaen P, Wensing AM, Fun A, et al. Clinical use of HIV integrase inhibitors: a systematic review and meta-analysis. PLoS One 2013;8:e52562
  • 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
  • Eron JJ, Cooper DA, Steigbigel RT, et al. Efficacy and safety of raltegravir for treatment of HIV for 5 years in the BENCHMRK studies: final results of two randomised, placebo-controlled trials. Lancet Infect Dis 2013;13:587-96
  • Elion R, Molina JM, Ramon Arribas Lopez J, et al. A randomized phase 3 study comparing once-daily elvitegravir with twice-daily raltegravir in treatment-experienced subjects with HIV-1 infection: 96-week results. J Acquir Immune Defic Syndr 2013; 1;63:494-7
  • SECOND-LINE Study Group. Boyd MA, Kumarasamy N, Moore CL, et al. Ritonavir-boosted lopinavir plus nucleoside or nucleotide reverse transcriptase inhibitors versus ritonavir-boosted lopinavir plus raltegravir for treatment of HIV-1 infection in adults with virological failure of a standard first-line ART regimen (SECOND-LINE): a randomised, open-label, non-inferiority study. Lancet 2013;381:2091-9
  • Paton N, Kityo C, Hoppe A, et al. A pragmatic randomised controlled strategy trial of three second-line treatment options for use in public health rollout programme settings: The europe-africa research network for evaluation of second-line therapy (EARNEST) trial [abstract WELBB02]. 7th International AIDS Society Conference on HIV Pathogenesis, Treatment and Prevention; 30 June – 3 July 2013
  • Lennox JL, Dejesus E, Berger D, et al. Raltegravir versus efavirenz regimens in treatment-naive HIV-1-infected patients: 96-week efficacy, durability, subgroup, safety, and metabolic analyses. J Acquir Immune Defic Syndr 2010;55:39-48
  • Rockstroh JK, DeJesus E, Lennox JL, et al. Durable efficacy and safety of raltegravir versus efavirenz when combined with tenofovir/emtricitabine in treatment-naïve HIV-infected patients: final five-year results from STARTMRK. J Acquir Immune Defic Syndr 2013;6:77-85
  • Reynes J, Trinh R, Pulido F, et al. Lopinavir/ritonavir combined with raltegravir or tenofovir/emtricitabine in antiretroviral-naive subjects: 96-week results of the PROGRESS study. AIDS Res Hum Retroviruses 2013;29:256-65
  • Kozal MJ, Lupo S, DeJesus E, et al. A nucleoside- and ritonavir-sparing regimen containing atazanavir plus raltegravir in antiretroviral treatment-naive HIV-infected patients: SPARTAN study results. HIV Clin Trials 2012;13:119-30
  • Eron JJ, Young B, Cooper DA, et al. Switch to a raltegravir-based regimen versus continuation of a lopinavir-ritonavir-based regimen in stable HIV-infected patients with suppressed viraemia (SWITCHMRK 1 and 2): two multicentre, double-blind, randomised controlled trials. Lancet 2010;375:396-407
  • Martinez E, Larrousse M, Llibre JM, et al. Substitution of raltegravir for ritonavir-boosted protease inhibitors in HIV-infected patients: the SPIRAL study. AIDS 2010;24:1697-707
  • Katlama C, Assoumou L, Valantin MA, et al. Maraviroc plus raltegravir dual therapy in aviremic HIV infected patients with lipodystrophy: results from the ROCnRAL ANRS 157 study. 20th Conference on Retroviruses and Opportunistic Infections; 2013
  • Nishijima T, Gatanaga H, Shimbo T, et al. Switching tenofovir/emtricitabine plus lopinavir/r to raltegravir plus darunavir/r in patients with suppressed viral load did not result in improvement of renal function but could sustain viral suppression: a randomized multicenter trial. PLoS One 2013;8:e73639
  • da Silva D, Van Wesenbeeck L, Breilh D, et al. HIV-1 resistance patterns to integrase inhibitors in antiretroviral-experienced patients with virological failure on raltegravir-containing regimens. J Antimicrob Chemother 2010;65:1262-9
  • Canducci F, Marinozzi MC, Sampaolo M, et al. Genotypic/phenotypic patterns of HIV-1 integrase resistance to raltegravir. J Antimicrob Chemother 2010;65:425-33
  • Parczewski M, Bander D, Urbanska A, et al. HIV-1 integrase resistance among antiretroviral treatment naive and experienced patients from northwestern Poland. BMC Infect Dis 2012;12:368
  • Eron JJ, Clotet B, Durant J, et al. Safety and efficacy of dolutegravir in treatment-experienced subjects with raltegravir-resistant HIV type 1 infection: 24-week results of the VIKING study. J Infect Dis 2013;207:740-8
  • 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
  • Raffi F, Jaeger H, Quiros-Roldan E, et al. Once-daily dolutegravir versus twice-daily raltegravir in antiretroviral-naïve adults with HIV-1 infection (SPRING-2 study): 96 week results from a randomised, double-blind, non-inferiority trial. Lancet Infect Dis 2013;13:927-35
  • Madeddu G, Menzaghi B, Ricci E, et al. Raltegravir central nervous system tolerability in clinical practice: results from a multicenter observational study. AIDS 2012;26:2412-15
  • Perry ME, Almaani N, Desai N, et al. Raltegravir-induced drug reaction with eosinophilia and systemic symptoms (DRESS) syndrome - implications for clinical practice and patient safety. Int J STD AIDS 2013;24:639-42
  • Lee FJ, Carr A. Tolerability of HIV integrase inhibitors. Curr Opin HIV AIDS 2012;7:422-8
  • Tsai WJ, Lee SS, Tsai HC, et al. Rapid onset of rhabdomyolysis after switching to a raltegravir-based antiretroviral regimen. J Microbiol Immunol Infect 2013; [Epub ahead of print]
  • Lee FJ, Amin J, Bloch M, et al. Skeletal muscle toxicity associated with raltegravir-based combination antiretroviral therapy in HIV-infected adults. J Acquir Immune Defic Syndr 2013;62:525-33
  • Monteiro P, Perez I, Pich J, et al. Creatine kinase elevation in HIV-1-infected patients receiving raltegravir-containing antiretroviral therapy: a cohort study. J Antimicrob Chemother 2013;68:404-8
  • Hegazi A, Mc Keown D, Doerholt K, et al. Raltegravir in the prevention of mother-to-child transmission of HIV-1: effective transplacental transfer and delayed plasma clearance observed in preterm neonates. AIDS 2012;26:2421-3
  • Nobrega I, Travassos AG, Haguihara T, et al. Short communication: use of raltegravir in late-presenting HIV-infected pregnant women. AIDS Res Hum Retroviruses 2013;29:1451-4
  • Pinnetti C, Baroncelli S, Villani P, et al. Rapid HIV-RNA decline following addition of raltegravir and tenofovir to ongoing highly active antiretroviral therapy in a woman presenting with high-level HIV viraemia at week 38 of pregnancy. J Antimicrob Chemother 2010;65:2050-2
  • Taylor N, Touzeau V, Geit M, et al. Raltegravir in pregnancy: a case series presentation. Int J STD AIDS 2011;22:358-60
  • Tricot L, Teicher E, Peytavin G, et al. Safety and efficacy of raltegravir in HIV-infected transplant patients cotreated with immunosuppressive drugs. Am J Transplant 2009;9:1946-52
  • Martinez E, D'Albuquerque PM, Llibre JM, et al. Changes in cardiovascular biomarkers in HIV-infected patients switching from ritonavir-boosted protease inhibitors to raltegravir. AIDS 2012;26:2315-26

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