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Drug Evaluations

Raltegravir: a review of its pharmacokinetics, pharmacology and clinical studies

, PharmD PhD
Pages 1151-1160 | Published online: 12 Aug 2010

Bibliography

  • FDA. Isentress; Prescribing Information. Available from: http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/022145s014lbl.pdf. Version date: 26 March 2010
  • Hazuda D, Iwamoto M, Wenning L. Emerging pharmacology: inhibitors of human immunodeficiency virus integration. Annu Rev Pharmacol Toxicol 2009;49:377-94
  • Croxtall JD, Lyseng-Williamson KA, Perry CM. Raltegravir. Drugs 2008;68:131-8
  • Markowitz M, Morales-Ramirez JO, Nguyen BY, 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
  • Lei HP, Ji W, Lin J, Effects of Ginkgo biloba extract on the pharmacokinetics of bupropion in healthy volunteers. Br J Clin Pharmacol 2009;68:201-6
  • Iwamoto M, Wenning LA, Petry AS, Safety, tolerability, and pharmacokinetics of raltegravir after single and multiple doses in healthy subjects. Clin Pharmacol Ther 2008;83:293-9
  • Molto J, Valle M, Mothe B, Pharmacokinetics and safety of once-daily raltegravir (800mg) plus atazanavir (400 mg) in HIV-infected patients [abstract O_13]. 10th International workshop on clinical pharmacology of HIV therapy; 15 – 17 April 2009; Amsterdam, the Netherlands
  • Yilmaz A, Gisslen M, Spudich S, Raltegravir cerebrospinal fluid concentrations in HIV-1 infection. PLoS One 2009;4:e6877
  • Calcagno A, Bonora S, Bertucci R, Raltegravir penetration in the cerebrospinal fluid of HIV-positive patients. AIDS 2010;24:931-2
  • Bonora S, D'Avolio A, Simele M, Steady-state raltegravir penetration in seminal plasma of healthy volunteers [abstract # 609]. 17th Conference on Retroviruses and Opportunistic Infections; 16 – 19 February 2010; San Francisco, CA
  • Clavel C, Mandelbrot L, Marcelin AG, Raltegravir concentrations in the cervico-vaginal compartment in HIV-1 infected women treated with raltegravir: DIVA 01 study [abstract # 608]. 17th Conference on Retroviruses and Opportunistic Infections; 16 – 19 February 2010; San Francisco, CA
  • Molto J, Valle M, Back D, Pharmacokinetics of once-daily raltegravir (800 mg) in plasma and PBMCs in HIV-infected patients [abstract #LB-01]. 11th International Workshop on Clinical Pharmacology of HIV Therapy; 7 – 9 April 2010; Sorrento, Italy
  • Kassahun K, McIntosh I, Cui D, Metabolism and disposition in humans of raltegravir (MK-0518), an anti-AIDS drug targeting the HIV-1 integrase enzyme. Drug Metab Dispos 2007;35:1657-63
  • Wenning LA, Petry AS, Kost JT, Pharmacokinetics of raltegravir in individuals with UGT1A1 polymorphisms. Clin Pharmacol Ther 2009;85:623-7
  • Iwamoto M, Hanley WD, Petry AS, Lack of a clinically important effect of moderate hepatic insufficiency and severe renal insufficiency on raltegravir pharmacokinetics. Antimicrob Agents Chemother 2009;53:1747-52
  • Tommassi C, Nicastri E, Gallo AL, Raltegravir and darunavir plasma pharmacokinetic in HIV-1-infeced patients with advanced liver disease [abstract #10]. 11th International Workshop on Clinical Pharmacology of HIV Therapy; 7 – 9 April 2010; Sorrento, Italy
  • Molto J, Sanz-Moreno J, Valle M, Effect of hemodialysis on raltegravir clearance in HIV-infected patients with end stage renal disease [abstract #7]. 11th International Workshop on Clinical Pharmacology of HIV Therapy; 7 – 9 April 2010; Sorrento, Italy
  • Wiznia A, Samson P, Acosta E, ; IMPAACT P1066. Safety and efficacy of rlategravir in pediatric HIV infection: preliminary analysis from the international maternal pediatric adolescent AIDs clinical trial group, P1066 [abstract 881]. 16th Conference on Retroviruses and Opportunistic Infections; 8 – 11 February 2009; Montreal, Canada
  • Nachman S, Acosta E, Samson P, ; the P1066 team. Interim results from IMPAACT P1066: raltegravir oral chewable tablet formulation in children 6 to 11 years [abstract # 161LB]. 17th Conference on Retroviruses and Opportunistic Infections; 16 – 19 February 2010; San Francisco, CA
  • La Porte CJ, Back DJ, Blaschke T, Updated guideline to perform therapeutic drug monitoring for antiretroviral agents. Rev Antivir Ther 2006;3:4-14
  • Grinsztejn B, Nguyen BY, Katlama C, 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
  • Wenning LA, Hwang E, Nguyen B-Y, Pharmacokinetic/pharmacodynamic (PK/PD) analyses for raltegravir (RAL) in phase III studies in treatment experienced HIV-infected patients following 48 weeks of treatment [abstract H-4054]. 48th Annual ICAAC/46th IDSA Meeting; 25 – 28 October 2008; Washington DC
  • McSharry J, Weng Q, Kulaway R, Drusano G. Dose range and dose fractionation studies for raltegravir pharmacodynamics in an in vitro hollow fiber infection model system [abstract O-09]. 10th International workshop on clinical pharmacology of HIV therapy; 15 – 17 April 2009; Amsterdam, the Netherlands
  • Burger DM, Colbers EPH, Van Luin M, Koopmans PP. AUC0-3h of raltegravir is correlated to AUC0-12h: a novel approach for therapeutic drug monitoring of raltegravir [abstract #41]. 11th International Workshop on Clinical Pharmacology of HIV Therapy; 7 – 9 April 2010; Sorrento, Italy
  • Iwamoto M, Kassahun K, Troyer MD, Lack of a pharmacokinetic effect of raltegravir on midazolam: in vitro/in vivo correlation. J Clin Pharmacol 2008;48:209-14
  • Van Luin M, Colbers A, Verwey-Van Wissen CP, The effect of raltegravir on the glucuronidation of lamotrigine. J Clin Pharmacol 2009;49:1220-7
  • Anderson MS, Wenning LA, Moreau A, Effect of raltegravir on the pharmacokinetics of oral contraceptives [abstract H-1758]. 47th Interscience Conference on Antimicrobial Agents and Chemconf-procapy; 17 – 20 September 2007; Chicago, USA
  • Fulco PP, Hynicka L, Rackley D. Raltegravir-based HAART regimen in a patient with large B-cell lymphoma. Ann Pharmacother 2010;44:377-82
  • Van Luin M, Colbers A, van Ewijk-Beneken-Kolmer EWJ, Drug-drug interactions between raltegravir and pravastatin in healthy volunteers [abstract #29]. 11th International Workshop on Clinical Pharmacology of HIV Therapy; 7 – 9 April 2010; Sorrento, Italy
  • Burger DM, Magis-Escurra C, van den Berk GE, Gelinck LB. Pharmacokinetics of double-dose raltegravir in two patients with HIV infection and tuberculosis. AIDS 2010;24:328-30
  • Moreno A, Quereda C, Fortun J, Safe co-administration of raltegravir, pegylated-interferon and, ribavirin in HIV individuals with hepatitis C virus-related liver damage. AIDS 2010;24:1231-3
  • Bickel M, Anadol E, Vogel M, Daily dosing of tacrolimus in patients treated with HIV-1 therapy containing a ritonavir-boosted protease inhibitor or raltegravir. J Antimicrob Chemother 2010;65:999-1004
  • Di BA, Rosso R, Siccardi M, Lack of interaction between raltegravir and cyclosporin in an HIV-infected liver transplant recipient. J Antimicrob Chemother 2009;64:874-5
  • Tricot L, Teicher E, Peytavin G, Safety and efficacy of raltegravir in HIV-infected transplant patients cotreated with immunosuppressive drugs. Am J Transplant 2009;9:1946-52
  • Lennox JL, DeJesus E, Lazzarin A, 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
  • Steigbigel RT, Cooper DA, Teppler H, Long-term efficacy and safety of Raltegravir combined with optimized background therapy in treatment-experienced patients with drug-resistant HIV infection: week 96 results of the BENCHMRK 1 and 2 phase iii trials. Clin Infect Dis 2010;50:605-12
  • Eron JJ, Young B, Cooper DA, 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
  • De Castro N, Braun J, Charreau I, Switch from enfuvirtide to raltegravir in virologically suppressed multidrug-resistant HIV-1-infected patients: a randomized open-label trial. Clin Infect Dis 2009;49:1259-67
  • Papendorp SG, van den Berk GE. Preoperative use of raltegravir-containing regimen as induction therapy: very rapid decline of HIV-1 viral load. AIDS 2009;23:739
  • Working Group of the office of AIDS Research Advisory Council (OARAC). Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents, version December 1, 2010. Available from: http://aidsinfo.nih.gov/contentfiles/AdultandAdolescentGL.pdf. [Last accessed 7 July 2010]
  • Yazdanpanah Y, Fagard C, Descamps D, 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
  • Cooper DA, Steigbigel RT, Lennox JL, Review of cancer incidence in raltegravir (RAL) clinical trials [abstract 559]. 16th Conference on Retroviruses and Opportunistic Infections; 8 – 11 February 2009; Montreal, Canada
  • Vispo E, Mena A, Maida I, Hepatic safety profile of raltegravir in HIV-infected patients with chronic hepatitis C. J Antimicrob Chemother 2010;65:543-7
  • Rockstroh J, Teppler H, Zhao J, Hepatic safety & efficacy of raltegravir in patients co-infected with HIV and hepatitisB and/or C virus [abstract 662]. 17th Conference on Retroviruses and Opportunistic Infections; 16 – 19 February 2010; San Francisco, CA
  • Zembower TR, Gerzenshtein L, Coleman K, Palella FJ Jr. Severe rhabdomyolysis associated with raltegravir use. AIDS 2008;22:1382-4
  • Dori L, Buonomini AR, Viscione M, A case of rhabdomiolysis associated with raltegravir use. AIDS 2010;24:473-5
  • Martinez E, Larrousse M, Llibre JM, Substitution of raltegravir for ritonavir-boosted protease inhibitors in HIV-infected patients: the SPIRAL study. AIDS 2010;24:1697-707
  • Wenning LA, Friedman EJ, Kost JT, Lack of a significant drug interaction between raltegravir and tenofovir. Antimicrob Agents Chemother 2008;52:3253-8
  • Iwamoto M, Wenning LA, Petry AS, Minimal effects of ritonavir and efavirenz on the pharmacokinetics of raltegravir. Antimicrob Agents Chemother 2008;52:4338-43
  • Anderson MS, Kakuda TN, Hanley W, Minimal pharmacokinetic interaction between the human immunodeficiency virus nonnucleoside reverse transcriptase inhibitor etravirine and the integrase inhibitor raltegravir in healthy subjects. Antimicrob Agents Chemother 2008;52:4228-32
  • Hanley WD, Wenning LA, Moreau A, Effect of tipranavir-ritonavir on pharmacokinetics of raltegravir. Antimicrob Agents Chemother 2009;53:2752-5
  • Iwamoto M, Wenning LA, Mistry GC, Atazanavir modestly increases plasma levels of raltegravir in healthy subjects. Clin Infect Dis 2008;47:137-40
  • Zhu L, Mahnke L, Butterton J, Pharmacokinetics and safety of twice daily atazanavir 300 mg and raltegravir 400 mg in healthy subjects [abstract 696]. 16th Conference on Retroviruses and Opportunistic Infections; 8 – 11 February 2009; Montreal, Canada
  • Anderson MS, Sekar V, Tomaka F, Pharmacokinetic evaluation of darunavir/ritonavir and raltegravir in healthy subjects [abstract A-962]. 48th Annual ICAAC/46th IDSA Meeting; 25 – 28 October 2008; Washington DC
  • Rhame F, Long M, Acosta E. RAL-KAL: pharmacokinetics of coadminsitered raltegravir and lopinavir/ritonavir in healthy subjects [abstract TuPe0075]. 17th International AIDS Conference; 3 – 8 August 2008; Mexico City, Mexico
  • Luber A, Slowinski PD, Acosta E, Steady-state pharmacokinetics (PK) of fosamprenavir (FPV) and raltegravir (RAL) alone and combined with unboosted and ritonavir-boosted FPV [abstract A1-1297]. 49th Interscience Conference on Antimicrobial Agents and Chemotherapy; 12 – 15 September 2009; San Francisco, CA
  • Andrews E, Glue P, Fang J, Assessment of the pharmacokinetics of co-administered maraviroc and raltegravir. Br J Clin Pharmacol 2010;69:51-7
  • Brainard DM, Petry A, Fang L, Lack of a clinically important effect of rifabutin (RFB) on raltegravir (RAL) pharmacokinetics [abstract A1-1296]. 49th Interscience Conference on Antimicrobial Agents and Chemotherapy; 12 – 15 September 2009; San Francisco, CA
  • Wenning LA, Hanley WD, Brainard DM, 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, Effects of omeprazole on plasma levels of raltegravir. Clin Infect Dis 2009;48:489-92
  • Markowitz M, Nguyen BY, Gotuzzo E, 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
  • Markowitz M, Nguyen BY, Gotuzzo E, 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

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