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Drug Evaluation

Lopinavir/ritonavir: a protease inhibitor for HIV-1 treatment

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Pages 2363-2375 | Published online: 19 Aug 2008

Bibliography

  • Jaffe HW, Bregman DJ, Selik RM. Acquired immune deficiency syndrome in the United States: the first 1,000 cases. J Infect Dis 1983;148(2):339-45
  • Centers for Disease Control (CDC). Updated on acquired immune deficiency syndrome (AIDS)-United States. MMWR Morb Mortal Wkly Rep 1982;31(37):507-8, 513-4
  • Report on the Global AIDS Epidemic 2007. UNAIDS; 2007
  • Palella FJ, Delaney KM, Moorman AC, et al. Declining morbidity and mortality among patients with advanced human immunodeficiency virus infection. N Engl J Med 1998;338(13):853-60
  • Guidelines for the use of antiretroviral agents in HIV-1 infected adults and adolescents (DHHS); 2008
  • European AIDS Clinical Society Guidelines (EACS). Guidelines for the Clinical Management and Treatment of HIV infected adults in Europe; 2007
  • ARTEMIS. Darunavir/ritonavir noninferior to lopinavir/ritonavir as first-line PI in antiretroviral-naïve HIV-infected patients at 48 weeks [abstract H-718b]. 47th Interscience Conference on Antimicrobial Agents and Chemotherapy. 17 – 20 September 2007. Chicago, Illinois
  • Valdez J, Berger D, McMurchie, et al. Efficacy and safety of darunavir/ritonavir compared with lopinavir/ritonavir: a 48-week HIV-1 infected treatment experienced patients. The TITAN study. Lancet 2007;370:49-58
  • Sham HK, Kempf DJ, Molla A, et al. ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob Agents Chemother 1998;42(12):3218-24
  • Gatell JM, Mensa J, Zamora L. Lopinavir/ritonavir, la primera asociación a dosis fija con ritonavir. Barcelona: Antares; 2003
  • Awni W, Chiu YL, Braun N, et al. Significantly reduced food effect and pharmacokinetic variability with a novel lopinavir/ritonavir tablet formulation [abstract WeOa0206]. 3rd International AIDS Society Conference on HIV Pathogenesis and Treatment; 2005; Rio de Janeiro
  • Molla A, Korneyeva M, Gao Q, et al. Ordered accumulation of mutations in HIV protease confers resistance to ritonavir. Nat Med 1996;2:760-6
  • Cvetkovic RS, Goa KL. Lopinavir/ritonavir a review if its use in the management of HIV-infection. Drugs 2003;63(8):769-802
  • Molla A, Vasavanonda S, Kumar G, et al. Human serum attenuates the activity of protease-inhibitors toward wild-type and mutant human immunodeficiency virus. Virology 1998;250:255-62
  • Acosta EP, Kakuda TN, Brundage RC, et al. Pharmacodynamics of human immunodeficiency virus type 1 protease inhibitors. Clin Infect Dis 2000;30:151-9
  • Murphy RL, da Silva BA, Hicks CB, et al. Seven-year efficacy of lopinavir–ritonavir-based regimen in antiretroviral-naïve HIV-1 infected patients. HIV Clin Trials 2008
  • Solas C, Lafeuillade A, Halfon P, et al. Discrepancies between protease inhibitor concentrations and viral load in reservoirs and sanctuary sites in human immunodeficiency virus infected patients. Antimicrob Agents Chemother 2003;47(1):238-43
  • Capparelli EV, Holland D, Okamoto C, et al. Lopinavir concentrations in cerebrospinal fluid exceed the 50% inhibitory concentration for HIV. AIDS 2005;19:949-52
  • Van den Brande G, Marquie-Beck J, Capparelli E, et al. Kaletra independently reduces HIV replication in cerebrospinal fluid [abstract 403]. 12th Conference on Retroviruses and Opportunistic Infections. 22 – 25 February 2005. Boston, Massachusetts
  • Letendre SL, van den Brande G, Hermes A, et al. Lopinavir with ritonavir reduces the HIV RNA level in cerebrospinal fluid. Clin Infect Dis. 2007;45(11) [Epub ahead of print]
  • Min SS, Corbett AH, Rezk N, et al. Differential penetration of protease inhibitors and non-nucleoside reverse transcriptase inhibitors into the female genital tract [abstract WePeB5966]. 14th International AIDS Conference. 7 – 12 July 2002. Barcelona, Spain
  • Launay O, Tod M, Louchahi K, et al. Differential diffusion of indinavir and lopinavir in genital secretions of HIV-infected women [abstract H-1712]. 42nd Interscience Conference on Antimicrobial Agents and Chemotherapy. 27 – 30 September 2002. San Diego, CA
  • Vergara TCR, Schechter M, Suarez-Kurtz G, et al. Poor penetration of lopinavir in the genital tract of men receiving HAART in Brazil [abstract B 12171]. 15th International AIDS Conference. 11 – 16 July 2004. Bangkok, Thailand
  • Ghosn J, Chaix ML, Peytavin G et al. Absence of HIV-1 shedding in male genital tract after 1 year of first-line lopinavir/ritonavir alone or in combination with zidovudine/lamivudine. J Antimicrob Chemother 2008;61(6):1344-7
  • Yeh RF, Hammill HA, Fiscus SA, et al. Single agent therapy with lopinavir/ritonavir controls HIV-1 viral replication in the female genital tract [poster 7.7/02]. 11th European AIDS Conference. 24 – 27 October 2007 Madrid, Spain
  • Hurst M, Faulds D. Lopinavir. Drugs 2000;60(6):1371-9
  • Qazi NA, Morlese JF, Pozniak AL. Lopinavir/ritonavir (ABT-378/r). Expert Opin Pharmacother 2002;3(3):315-27
  • Gustavson L, Lam W, Bertz R, et al. Assessment of the bioequivalence and food effects for liquid and soft elastic capsule coformulations of ABT-378/ritonavir in healthy subjects. 40th Interscience Conference on Antimicrobial Agents and Chemotherapy. 17 – 20 September 2000 Toronto, Canada
  • Bertz R, Lam W, Brun S, et al. Multiple-dose pharmacokinetics of ABT-378/ritonavir in HIV + subjects. 39th Interscience Conference on Antimicrobial Agents and Chemotherapy. 26 – 29 September 1999 San Francisco, CA
  • Kaletra®. European summary of product characteristics. Abbot Laboratories, Maidenhead; 2001
  • Zhu T, Chiu Y, Doan T, et al. New tablet formulation of lopinavir/ritonavir is bioequivalent to the capsule at a dose of 800/200 mg [poster H-1894]. 45th Interscience Conference on Antimicrobial Agents and Chemotherapy. 16 – 19 December 2005 Washington, DC
  • Johnson M, Gathe J, Podzamczer D, et al. A once-daily lopinavir/ritonavir-based regimen provides noninferior antiviral activity compared with a twice-daily regimen. J AIDS 2006;43(2):153-60
  • Mildvan D, Tierney C, Gross R, et al. Randomized comparison in treatment-naive patients of once-daily vs twice daily lopinavir/ritonavir-based ART and comparison of once-daily self administered vs directly observed therapy. ACTG A5073 Study Team [abstract 138]. 14th Conference on Retroviruses and Opportunistic Infections. 25 – 28 February 2007. Los Angeles, CA
  • Gathe J, da Silva B, Loutfy M, et al. Study M05-730 primary efficacy results at week 48: phase 3, randomized, open-label study of lopinavir/ritonavir tablets once daily vs twice daily, coadministered with tenofovir plus emtricitabine in ARV-naive HIV-1- infected subjects [abstract 775]. 15th Conference on Retroviruses and Opportunistic Infections. 3 – 6 February 2008. Boston, Massachusetts
  • US Food and Drug Administration. Department of Health and Human Services. HIV and AIDS therapies. Approved therapies and treatment guidelines. Available from: http://www.fda.gov [Accessed 29 June 2008]
  • Tan D, Walmsday S. Lopinavir plus ritonavir: a novel protease inhibitor combination for HIV infections. Expert Rev Anti Infect Ther 2007;5(1);13-28
  • Walmsley S, Bernstein B, King M, et al. Lopinavir–ritonavir versus nelfinavir for the initial treatment of HIV infection. The M98-863 Study Team. N Engl J Med 2002;346(26):2039-46
  • Eron Jr J, Yeni P, Gathe J, et al. The KLEAN study of fosamprenavir–ritonavir versus lopinavir–ritonavir, each in combination with abacavir–lamivudine, for initial treatment of HIV infection over 48 weeks: a randomized non-inferiority trial. Lancet 2006;368(9534):476-82
  • King M, Fredrick L, da Silva B, et al. Once-daily and twice-daily lopinavir/ritonavir based-regimens provide similar virologic response through 48 weeks: results of a meta-analysis. British HIV Association 2008 [poster abstract No. 17]. HIV Med 2008;9(Suppl 1):10-50
  • Molina JM, Andrade-Villanueva J, Echevarría J, et al. Efficacy and safety of once- daily atazanavir/ritonavir compared to twice-daily lopinavir/ritonavir, each in combination with tenofovir and emtricitabine in ARV-naive HIV-1 infected subjects: the CASTLE Study, 48-week results [abstract 37]. 15th Conference on Retroviruses and Opportunistic Infections. 3 – 6 February 2008. Boston, Massachusetts
  • Walmsley S, et al.; The Gemini Study. Saquinavir/r (SQV/r) vs lopinavir/r (LPV/r) plus emtricitabine/tenofovir (FTC/TDF) as initial therapy in HIV-1 infected patients [abstract PS1/4]. 11th European AIDS Conference. 24 – 27 October 2007. Madrid, Spain
  • Riddler S, Haubrich R, DiRienzo G, et al. A prospective, randomized, Phase III trial of NRTI-, PI- and NNRTI-sparing regimens for initial treatment of HIV-1 infection- ACTG 5142 [abstract THLB0204]. 16th International AIDS Conference. 13 – 18 August 2006. Toronto, Canada
  • Benson CA, Deeks SG, Brun SC, et al. Safety and antiviral activity at 48 weeks of lopinavir/ritonavir plus nevirapine and 2 nucleoside reverse-transcriptase inhibitors in human immunodeficiency virus type 1-infected protease inhibitor experienced patients. J Infect Dis 2002;185:599-607
  • Pollard RB, Thompson M, Hicks C, et al. Phase 3 comparison of lopinavir/ritonavir vs investigator-selected protease inhibitor in single PI-experienced, NNRTI-naive patients: 48 week results of study M 98-888 [poster PL.3.2]. 7th International Congress on Drug Therapy in HIV Infection. 14 – 18 November 2004. Glasgow, UK
  • Johnson M, Grinsztejn B, Rodriguez C, et al. 96 week comparison of once-daily atazanavir/ritonavir and twice-daily lopinavir/ritonavir in patients with multiple virological failures. AIDS 2006;20(5):711-8
  • Hill A. Atazanavir/ritonavir versus lopinavir/ritonavir: equivalent or different efficacy profiles? AIDS 2005:19(17):2054-5
  • Hicks C, Cahn P, Cooper D, et al. Durable efficacy of tipranavir/ritonavir in combination with an optimised background regimen of antiretroviral drugs for treatment-experienced HIV-1-infected patients at 48 weeks in the Randomized Evaluation of Strategic Intervention in multi-drug reSistant patients with Tipranavir (RESIST) studies: an analysis of combined data from two randomised open-label trials. Lancet 2006;368:466-75
  • Dragsted UB, Gerstoft J, Youle M, et al. A randomized trial to evaluate lopinavir/ritonavir versus saquinavir/ritonavir in HIV-1 infected patients: the MaxCmin2 trial. Antivir Ther 2005;10(6):735-43
  • Elston RC, Yates P, Tisdale M, et al. GW433908(908)/ritonavir: 48 week results in PI-experienced subjects: a retrospective analysis of virological response based on baseline genotype and phenotype [abstract MoOrB1055]. 15th International AIDS Conference. 11 – 16 July 2004. Bangkok, Thailand
  • Podzamczer D, King M, Klein C, et al. High-dose lopinavir/ritonavir in highly treatment-experienced HIV-1 patients: efficacy, safety, and predictors of response. HIV Clin Trials 2007;8(4):193-204
  • Bertz R, Li J, King M et al. Lopinavir Inhibitory Quotient Predicts Virologic Response in Highly Antiretroviral-experienced Patients Receiving High-dose Lopinavir/Ritonavir. 11th Conference on Retrovirus and Opportunistic Infections 8 – 11 February 2004, San Francisco, CA
  • Negredo E, Molto J, Burger D, et al. Lopinavir/ritonavir plus nevirapine as a nucleoside sparing approach in antiretroviral-experienced patients (NEKA Study). J Acquir Immune Defic Syndr 2005;38:47-52
  • Gathe Jr J, Yeh RF, Mayberry C, et al. Single agent therapy with lopinavir/ritonavir suppresses plasma HIV-1 viral replication in HIV-1 naïve subjects: IMANI-2 48 weeks results. 4th International AIDS Society Conference on HIV Pathogenesis, Treatment and Prevention. 22 – 25 July 2007. Sydney, Australia
  • Delfraissy JF, Flandre P, Delaugerre C, et al. Lopinavir/ritonavir monotherapy or plus zidovudine and lamivudine in antiretroviral-naive HIV-infected patients. AIDS 2008;22(3):385-93
  • Arribas J, Pulido F, Delgado R, et al. Lopinavir/ritonavir as single drug therapy for maintenance of HIV-1 viral suppression: 48-week results of a randomized, controlled, open-label, proof-of-concept pilot clinical trial (OK study). J Acquir Immune Defic Syndr 2005;40:280-7
  • Arribas J, Pulido F, Delgado R, et al. Lopinavir/ritonavir monotherapy versus lopinavir/ritonavir and two nucleosides for maintenance therapy of HIV. Ninety-six week results of a randomized, controlled, open-label clinical trial (OK04 Study) [oral presentation PS3/1]. 11th European AIDS Conference. 24 – 27 October 2007. Madrid, Spain
  • Cameron W, da Silva B, Arribas J, et al. A two-year randomized controlled clinical trial in antiretroviral-naïve subjects using lopinavir/ritonavir (LPV/r) monotherapy after initial induction treatment compared to an efavirenz (EFV) 3-drug regimen (Study M03-613) [abstract THLB0201]. 16th International AIDS Conference. 13 – 18 August 2006. Toronto, Canada
  • Hicks C, da Silva B, King M, et al. Extensive resistance testing during 5 years of lopinavir/ritonavir treatment in antiretroviral naive HIV-infected patients: results from Study 720. XV 15th International AIDS Conference. 11 – 16 July 2004. Bangkok, Thailand
  • Kempf J, King M, Bernstein B, et al. Incidence of resistance in a double-blind study comparing lopinavir/ritonavir plus stavudine and lamivudine to nelfinavir plus stavudine and lamivudine. J Infect Dis 2004;189:51-60
  • Molina JM, Gathe J, Lim PL, et al. Comprehensive resistance testing in antiretroviral-naive patients treated with once daily lopinavir/ritonavir plus tenofovir DF and emtricitabine: 48 week results from study 418 [poster WePeB5701]. 15th International AIDS Conference. 11 – 16 July 2004. Bangkok, Thailand
  • Delaugerre C, Flandre P, Chaix ML et al. Protease Gene Mutations in a Trial Comparing First Line LPV/r Monotherapy to LPV/r + AZT/3TC (MONARK Trial). XVI International HIV Drug Resistance Workshop: Poster n. 75. 12 – 16 June 2007. Barbados, West Indies
  • Arribas J, Pulido F, Delgado R, et al. Drug resistance outcomes at 48 weeks in the OK04 Trial: a comparative trial of single-drug maintenance therapy with lopinavir/ritonavir vs triple therapy with lopinavir/ritonavir [poster 638]. 14th Conference on Retroviruses and Opportunistic Infections. 25 – 28 February 2007. Los Angeles, CA
  • Norton M, Young T, Parkin N, et al. Prevalence, mutational patterns, and phenotypic correlates of the L76V protease mutation in relation to LPV-associated mutations [poster 854]. 15th Conference on Retroviruses and Opportunistic Infections. 3 – 6 February 2008. Boston, Massachusetts
  • Kempf DJ, Isaacson JD, King MS, et al. Identification of genotypic changes in human immunodeficiency virus protease that correlate with reduced susceptibility to the protease inhibitor lopinavir among viral isolates from protease inhibitor- experienced patients. J Virol 75(16):7462-9
  • De Mendoza C, Valer L, Bacheler L, et al. Prevalence of the HIV-1 protease mutation I47A in clinical practice and association with lopinavir resistance. AIDS 2006;20:1071-4
  • Martínez E, Domingo P, Galindo M, et al. Risk of metabolic abnormalities in patients infected with HIV receiving antiretroviral therapy that contains lopinavir–ritonavir. Clin Infect Dis 2004;38:1017-23
  • Haubrich R, Riddler S, Di Rienzo G, et al. Metabolic outcomes of ACTG 5142: a prospective, randomized, Phase III trial of NRTI-, PI-, and NNRTI-sparing Regimens for initial treatment of HIV-1. 14th Conference on Retroviruses and Opportunistic Infections. 25 – 28 February 2007. Los Angeles, CA.
  • Cameron DW, da Silva B, Arribas J, et al. Significant sparing of peripheral lipoatrophy by HIV treatment with LPV/r plus ZDV/3TC induction followed by LPV/r monotherapy compared with EFV plus ZDV/3TC [oral abstract 44]. 14th Conference on Retroviruses and Opportunistic Infections. 25 – 28 February 2007. Los Angeles, CA
  • Sulkowsky MS, Mehta SH, Chaisson RE, et al. Hepatotoxicity associated with protease inhibitor-based antiretroviral regimens with or without concurrent ritonavir. AIDS 2004;18(17):2277-84
  • Da Silva B, King M, Cernohous P, et al. Lopinavir/ritonavir safety, tolerability and efficacy in HIV patients co-infected with hepatitis C and/or hepatitis B: review of clinical trials [abstract MoPeB3285]. 15th International AIDS Conference. 11 – 16 July 2004. Bangkok, Thailand
  • Pinto JFC, Eyer-Silva WA, Morais-de-Sa, et al. Recurrent edema associated with the co-formulation of lopinavir and ritonavir. Rev Soc Bras Med Trop 2004;357-8
  • Colebunders R, De Schacht C, Vanwolleghem T, et al. Lopinavir/ritonavir- and indinavir-induced thrombocytopenia in a patient with HIV-infection. Int J Infect Dis 2004;8:315-6
  • Doco-Lecompte T, Garrec A, Thomas L, et al. Lopinavir/ritonavir and lithiasis: seven cases. AIDS 2004;18:705-6
  • Bongiovanni M, Chiesa E, Monforte A, et al. Hair loss in an HIV-1 infected woman receiving lopinavir plus ritonavir therapy as first line HAART. Dermatol Online J 2003;9:28
  • Stek A, Mirochnick N, Capparelli E, et al. Reduced lopinavir exposure during pregnancy. AIDS 2006;20:1931-9
  • Cassard B, Rouault A, Damond F, et al. Therapeutic drug monitoring of lopinavir/ritonavir containing regimen in pregnant HIV infected women [poster WePe3.2c09]. 3rd International AIDS Society Conference on HIV Pathogenesis, Treatment and Prevention. 24 – 27 July 2005. Río de Janeiro, Brazil.
  • Best B, Stek A, Hu C, et al. High-dose lopinavir and standard-dose emtricitabine pharmacokinetics during pregnancy and postpartum [poster 629]. 15th Conference on Retroviruses and Opportunistic Infections. 3 – 6 February 2008. Boston, Massachusetts
  • Guía de interacciones farmacológicas en HIV. Available from: http://www.interaccioneshiv.com [Accessed 28 June 2008]

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