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Drug Evaluation

Darunavir (TMC114): a new HIV-1 protease inhibitor

, MD PhD & , PhD
Pages 1951-1964 | Published online: 14 Aug 2007

Bibliography

  • PALELLA FJ Jr, DELANEY KM, MOORMAN AC et al.: Declining morbidity and mortality among patients with advanced human immunodeficiency virus infection. N. Engl. J. Med. (1998) 338:853-860.
  • MOCROFT A, LEDERGERBER B, KATLAMA C et al.: Decline in the AIDS and death rates in the EuroSIDA study: an observational study. Lancet (2003) 362:22-29.
  • HAMERS FF, DOWNS AM: The changing face of the HIV epidemic in western Europe: what are the implications for public health policies? Lancet (2004) 364:83-94.
  • BACHELER L, JEFFREY S, HANNA G et al.: Genotypic correlates of phenotypic resistance to efavirenz in virus isolates from patients failing nonnucleoside reverse transcriptase inhibitor therapy. J. Virol. (2001) 75:4999-5008.
  • DELAUGERRE C, ROHBAN R, SIMON A et al.: Resistance profile and cross-resistance of HIV-1 among patients failing a non-nucleoside reverse transcriptase inhibitor-containing regimen. J. Med. Virol. (2001) 65:445-448.
  • MILLER V, LARDER BA: Mutational patterns in the HIV genome and cross-resistance following nucleoside and nucleotide analogue drug exposure. Antivir. Ther. (2001) 6(Suppl. 3):25-44.
  • CHARPENTIER C, DWYER DE, LECOSSIER D, CLAVEL F, HANCE AJ: Co-evolution and competition of viral populations with distinct resistance genotypes in patients failing treatment with protease inhibitors. Antivir. Ther. (2002) 7:S55 (Abstract 48).
  • TIBOTEC, INC.: PREZISTA™ (darunavir) Prescribing Information. June 2006. Tibotec. Inc. (2006).
  • KATLAMA C, ESPOSITO R, GATELL JM et al.: Efficacy and safety of TMC114/ritonavir in treatment-experienced HIV patients: 24-week results of POWER 1. AIDS (2007) 21:395-402.
  • HAUBRICH RH, BERGER D, CHILIADE P et al.: Week 24 efficacy and safety of TMC114/ritonavir in treatment-experienced HIV patients. AIDS (2007) 21:F11-F18.
  • KING NM, PRABU-JEYABALAN M, NALIVAIKA EA, WIGERINCK P, DE BETHUNE MP, SCHIFFER CA: Structural and thermodynamic basis for the binding of TMC114, a next-generation human immunodeficiency virus type 1 protease inhibitor. J. Virol. (2004) 78:12012-12021.
  • TIE Y, BOROSS PI, WANG YF et al.: High resolution crystal structures of HIV-1 protease with a potent non-peptide inhibitor (UIC-94017) active against multi-drug-resistant clinical strains. J. Mol. Biol. (2004) 338:341-352.
  • KOH Y, NAKATA H, MAEDA K et al.: Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro. Antimicrob. Agents Chemother. (2003) 47:3123-3129.
  • DE MEYER S, AZIJN H, SURLERAUX D et al.: TMC114, a novel human immunodeficiency virus type 1 protease inhibitor active against protease inhibitor-resistant viruses, including a broad range of clinical isolates. Antimicrob. Agents Chemother. (2005) 49:2314-2321.
  • SEKAR V, GUZMAN S, STEVENS T, DE PAEPE E, LEFEBVRE E, HOETELMANS R: Absolute bioavailability of TMC114, administered in the absence and presence of low-dose ritonavir. 7th International Workshop on Clinical Pharmacology of HIV Therapy. Lisbon, Portugal (20 – 22 April 2006) (Abstract and poster P86).
  • SEKAR V, KESTENS D, SPINOSA-GUZMAN S et al.: The effect of different meal types on the pharmacokinetics of darunavir (TMC114)/ritonavir in HIV-negative healthy volunteers. J. Clin. Pharmacol. (2007) 47:479-484.
  • SCHON A, DEL MAR INGARAMO M, FREIRE E: The binding of HIV-1 protease inhibitors to human serum proteins. Biophys. Chem. (2003) 105:221-230.
  • SEKAR V, SPINOSA-GUZMAN S, LEFEBVRE E, HOETELMANS R: Clinical pharmacology of TMC114 – a new HIV protease inhibitor. 16th International AIDS Conference. Toronto, Canada (13 – 18 August 2006) (Abstract and poster TUPE0083).
  • SEKAR VJ, SPINOSA-GUZMAN S, LASURE A et al.: Mass-balance study of 14C-labelled darunavir (TMC114) in HIV-negative healthy volunteers. 8th International Workshop on Clinical Pharmacology of HIV Therapy. Budapest, Hungary (16 – 18 April 2007) (Poster 80).
  • SEKAR VJ, LEFEBVRE E, DE PE et al.: Pharmacokinetic interaction between TMC114/r and omeprazole or ranitidine in HIV-negative healthy volunteers. Antimicrob. Agents. Chemother. (2007) 51:958-961.
  • BACK D, SEKAR V, LEFEBVRE E et al.: Use of darunavir (TMC114) in combination with other drugs: guidance from pharmacokinetic studies. 8th International Congress on Drug Therapy in HIV Infection, Glasgow, UK (12 – 16 November 2006) (Abstract and poster PL5.1).
  • HOETELMANS R, LASURE A, KOESTER A et al.: The effect on TMC114, a potent next-generation HIV protease inhibitor, with low-dose ritonavir on atorvastatin pharmacokinetics. 44th Interscience Conference on Antimicrobial Agents and Chemotherapy. Washington, DC, USA (30 October – 2 November 2004) (Abstract and poster H-865).
  • SEKAR V, LEFEBVRE E, DE MAREZ T et al.: Pharmacokinetic interaction between TMC114, a new protease inhibitor and sildenafil. 46th Interscience Conference on Antimicrobial Agents and Chemotherapy, San Francisco, CA, USA (27 – 30 September 2006) (Abstract and poster A-0369).
  • SEKAR VJ, SPINOSA-GUZMAN S, MARIEN K et al.: Pharmacokinetic drug-drug interaction between the new HIV protease inhibitor darunavir (TMC114) and the lipid-lowering agent pravastatin. 8th International Workshop on Clinical Pharmacology of HIV Therapy, Budapest, Hungary (16 – 18 April 2007). (Abstract and poster 54).
  • ABEL S, RIIDGWAY C, HAMLIN J, DAVIS J, MACK R, SEKAR V: An open, randomised, 2-way crossover study to investigate the effects of darunavir/ritonavir on the pharmacokinetics of maraviroc in healthy subjects. 8th International Workshop on Clinical Pharmacology of HIV Therapy, Budapest, Hungary (16 – 18 April 2007) (Abstract and poster 55).
  • SEKAR V, DE MEYER S, VANGENEUGDEN T et al.: Pharmacokinetic/pharmacodynamic (PK/PD) analyses of TMC114 in the POWER 1 and POWER 2 trials in treatment-experienced HIV-infected patients. 13th Conference on Retroviruses and Opportunistic Infections Denver, CO, USA (5 – 9 February 2006) (Abstract and poster J-121).
  • ARASTEH K, CLUMECK N, POZNIAK A et al.: TMC114/ritonavir substitution for protease inhibitor(s) in a non-suppressive antiretroviral regimen: a 14-day proof-of-principle trial. AIDS (2005) 190:943-947.
  • PEETERS M, VAN BAELEN B, DE MEYER S et al.: TMC114/RTV activity in multiple PI-experienced patients: correlation of baseline genotype, phenotype, PK, and IQ with antiviral activity at Day 14. 11th Conference on Retroviruses and Opportunistic Infections, San Francisco, CA, USA (February 2004) (Abstract and poster 533).
  • D'AQUILA RT, SCHAPIRO JM, BRUN-VEZINET F et al.: Drug resistance mutations in HIV-1. Top. HIV Med. (2003) 11:92-96.
  • CLOTET B, BELLOS N, MOLINA JM et al.: Efficacy and safety of darunavir-ritonavir at week 48 in treatment-experienced patients with HIV-1 infection in POWER 1 and 2: a pooled subgroup analysis of data from two randomised trials. Lancet (2007) 369:1169-1178.
  • HILL A, MOYLE G: Relative antiviral efficacy of TMC114/r and tipranavir/r versus control PI in the POWER and RESIST trials. HIV Med. (2007) 8(4):259-264.
  • MOLINA JM, COHEN C, KATLAMA C et al.: Safety and efficacy of darunavir (TMC114) with low-dose ritonavir in treatment-experienced patients: 24-week results of POWER 3. J. Acquire. Immune. Defic. Syndromes. (2007). In press
  • JOHNSON VA, BRUN-VEZINET F, CLOTET B et al.: Update of the drug resistance mutations in HIV-1: 2005. Top. HIV Med. (2005) 13:51-57.
  • HILL A, MONTANER J, SMITH C: Prediction of clinical benefits of darunavir/r from treatment effects on CD4 counts and HIV RNA. HIV Med. (2007) 8(4):234-240.
  • HILL A and GEBO K: Predicted effect of TMC114/r on costs of care in two US cohorts of HIV-infected patients. 46th Interscience Conference on Antimicrobial Agents and Chemotherapy, San Francisco, CA, USA (27 – 30 September 2006) (Poster O-1468).
  • OLSEN CH, GATELL J, LEDERGERBER B et al.: Risk of AIDS and death at given HIV-RNA and CD4 cell count, in relation to specific antiretroviral drugs in the regimen. AIDS (2005) 19:319-330.
  • JOHNSON VA, BRUN-VEZINET F, CLOTET B et al.: Update of the drug resistance mutations in HIV-1: Fall 2005. Top. HIV Med. (2005) 13:125-131.
  • DE MEYER S, VANGENEUGDEN T, LEFEBVRE E et al.: Phenotypic and genotypic determinants of TMC114 (darunavir) resistance: POWER 1, 2 and 3 pooled analysis. 8th International Congress on Drug Therapy in HIV Infection, Glasgow, UK (2 – 16 November 2006) (Abstract and poster P196).
  • DE MEYER S, VANGENEUGDEN T, LEFEBVRE E et al.: Phenotypic and genotypic determinants of resistance to TMC114: pooled analysis of POWER 1, 2 and 3. 15th International HIV Drug Resistance Workshop, Sitges, Spain (13 – 17 June 2006) (Abstract and poster P73).
  • RINEHART A, LECOCQ P, MCKENNA P, PATTERY T, WASILKOWSKI B, BACHELER LT: Predicted phenotypic resistance in routine clinical samples between 1998 and 2003. Antivir. Ther. (2004) 9:S90 (Abstract).
  • COHEN C, FALCON R, RINEHART A, LEFEBVRE E: Factors influencing TMC114/r efficacy in treatment-experienced HIV patients: POWER 1, 2 and 3 pooled 24-Week analysis. 44th Annual Meeting of the Infectious Diseases Society of America, Toronto, Ontario, Canada (12 – 15 October 2006) (Abstract 688).
  • VANGENEUGDEN T, WINTERS B, BACHELER L et al.: Impact of optimised background regimen on virological response to TMC114 with low-dose ritonavir in POWER 1, 2 and 3, as measured by the phenotypic susceptibility score. Antivir. Ther. (2006) 11:S36.
  • Tibotec BVBA, Mechelen, Belgium. Data on file.
  • GERETTI AM: Epidemiology of antiretroviral drug resistance in drug-naive persons. Curr. Opin. Infect. Dis. (2007) 20:22-32.
  • LEFEBVRE E, DE MEYER S, DE PAEPE E, HILL A: Darunavir (TMC114)/r provides greater efficacy benefits versus control protease inhibitor(s), regardless of the protease inhibitor or sensitivity to the protease inhibitor: POWER 1 and 2 trials. 8th International Congress on Drug Therapy in HIV Infection. Glasgow, UK (12 – 16 November 2006) (Abstract and poster P29).
  • COLLIER AC, GOFFARD JC, KATNER H, ROZENBAUM W, VANGENEUGDEN T, LEFEBVRE E: Safety and efficacy of TMC114/r (darunavir/ritonavir) by gender, age and race: combined 24-week analysis of POWER 1, 2 and 3. 46th Interscience Conference on Antimicrobial Agents and Chemotherapy, San Francisco, CA, USA (27 – 30 September 2006) (Abstract and poster H-1396).
  • VALDEZ-MADRUGA J, LAFEUILLADE A, BEATTY G, SPINOSA GUZMAN S, EL MALT M, LEFEBVRE E: TMC114/r is well tolerated by treatment-experienced patients in POWER 1, 2 and 3: integrated clinical safety analysis. Presented at the 16th International AIDS Conference, Toronto, Canada (13 – 18 August 2006) (Abstract and poster TUPE0062).
  • VANGENEUGDEN T, VAN BAELEN B, DE PAEPE E et al.: TMC114/r in treatment-experienced patients in POWER 1, 2 and 3: integrated analysis of laboratory parameters. 16th International AIDS Conference, Toronto, Canada (13 – 18 August 2006) (Abstract and poster TUPE0063).
  • RACHLIS A, CLOTET B, BAXTER J, LEFEBVRE E: TMC114/r tolerability in treatment-experienced, hepatitis B or C (HBV/HCV) co-infected patients in POWER 1 and 3. 44th Annual Meeting of the Infectious Diseases Society of America, Toronto, Ontario, Canada (12 – 15 October 2006) (Abstract and poster 961).
  • JEMSEK JG, ARATHOON E, ARLOTTI M et al.: Body fat and other metabolic effects of atazanavir and efavirenz, each administered in combination with zidovudine plus lamivudine, in antiretroviral-naive HIV-infected patients. Clin. Infect. Dis. (2006) 42:273-280.
  • TOMAKA F, LEFEBVRE E, SEKAR V et al.: Similar changes in metabolic parameters of darunavir (TMC114) and atazanavir, each coadministered with low-dose ritonavir in healthy volunteers. Frontiers in Drug Development for Antiretroviral Therapies, Cancun, Mexico (10 – 14 December 2006) (Abstract and poster 85).
  • JOHNSON M, HILL A, SMITH C: Analysis of treatment costs for HIV RNA reductions, full virological suppression, and CD4 increases for treatment-experienced, HIV-infected patients. 12th Annual Conference of the British HIV Association (BHIVA), Brighton, UK (29 March – 1 April 2006) (Abstract and poster P29).
  • MAUSKOPF J, BROGAN A, SMETS E, NUYTS G, MARTIN S: Cost-effectiveness of darunavir (TMC114)/ritonavir compared with currently available protease inhibitors in treatment-experienced HIV patients. 8th International Congress on Drug Therapy in HIV Infection, Glasgow, UK (12 – 16 November 2006) (Abstract and poster P51).
  • BROGAN A, MAUSKOPF J, MARTIN JN, SMETS E: Cost effectiveness analysis of darunavir/r for HIV infection in treatment-experienced adults in the US: understanding the uncertainty in the estimates. International Society for Pharmacoeconomics and Outcomes Research (2007). (Abstract).
  • GARBER AM, PHELPS CE: Economic foundations of cost-effectiveness analysis. J. Health Econ. (1997) 16:1-31.
  • HILL AM, SMITH C: Analysis of cost of full virologic suppression for treatment-experienced, HIV-infected patients. 16th International AIDS Conference, Toronto, Canada (13 – 18 August 2006) (Abstract and poster MOPE0679).
  • HILL A, GEBO K: Predicted effect of TMC114/r on costs of care in two US cohorts of HIV-infected patients. 46th Interscience Conference on Antimicrobial Agents and Chemotherapy (San Francisco, CA, USA (27 – 30 September 2006) (Abstract O-1468).
  • DUBOIS D, SMETS E, VANGENEUGDEN T et al.: Improved quality of life in treatment-experienced HIV patients treated with TMC114/r versus control protease inhibitors: results of POWER 1 and 2 Functional Assessment of HIV Infection (FAHI). International AIDS Conference, Toronto, Canada (13 – 18 August 2006) (Abstract and poster TUPE0069).
  • HAMMER SM, SAAG M, SCHECHTER M et al.: Treatment for adult HIV infection. 2006 recommendations of the International AIDS Society – USA Panel. JAMA (2006) 296:827-843.

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