Darunavir: an effective protease inhibitor for HIV-infected patients

References

• 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.338, 853–860 (1998).
   PubMed Web of Science ®Google Scholar
• Bartlett JA, DeMasi R, Quinn J et al. Overview of the effectiveness of triple combination therapy in antiretroviral-naive HIV-1 infected adults. AIDS15, 1369–1377 (2001).
   PubMed Web of Science ®Google Scholar
• Hertogs K, Bloor S, Kemp SD et al. Phenotypic and genotypic analysis of clinical HIV-1 isolates reveals extensive PI cross-resistance: a survey of over 6000 samples. AIDS14, 1203–1210 (2000).
   PubMed Web of Science ®Google Scholar
• Koh Y, Nakata H, Maeda K et al. Novel bis-tetrahydrofuranylurethane containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC 114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro. Antimicrob. Agents Chemother.47(10), 3123–3129 (2003).
   PubMed Web of Science ®Google Scholar
• King NM, Prabu-Jeyabalan M, Nalivaika EA et al. Structural and thermodynamic basis for the binding of TMC114, a next-generation human immunodeficiency virus type 1 protease TMC114: effect inhibitor. J. Virol.78(21), 12012–12021 (2004).
   PubMed Web of Science ®Google Scholar
• Surleraux DL, de Kock HA, Verschueren WG et al. Design of HIV-1 protease inhibitors active on multidrug-resistant virus. Med. Chem.48, 1965–1973 (2005).
   Web of Science ®Google Scholar
• Dierynck I, De Wit M, Gustin E et al. Binding kinetics of darunavir to human immunodeficiency virus type 1 protease explain the potent antiviral activity and high genetic barrier. J. Virol.81(24), 13845–13851 (2007).
   PubMed Web of Science ®Google Scholar
• Tie Y, Boross PI, Wang YF et al. High-resolution crystal structure of HIV-1 protease with a potent non-peptide inhibitor (UIC-94017) active against multi-drug-resistant clinical strains. J. Mol. Biol.338, 341–352 (2004).
   PubMed Web of Science ®Google Scholar
• Surleraux DL, Tahri A, Verschueren WG et al. Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor. Med. Chem.48, 1813–1822 (2005).
   Web of Science ®Google Scholar
• 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.49(6), 2314–2321 (2005).
   PubMed Web of Science ®Google Scholar
• 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.47(4), 479–484 (2007).
   PubMed Web of Science ®Google Scholar
• Sekar VJ, Lefebvre E, De Paepe E et al. Pharmacokinetic interaction between darunavir boosted with ritonavir and omeprazole or ranitidine in human immunodeficiency virus negative healthy volunteers. Antimicrob. Agents Chemother.51(3), 958–961 (2007).
   PubMed Web of Science ®Google Scholar
• Back D, Sekar V, Hoetelmans RM. Darunavir: pharmacokinetics and drug interactions. Antivir. Ther.13(1), 1–13 (2008).
   PubMed Web of Science ®Google Scholar
• Hoetelmans RMW, Marien K, De Pauw M et al. Pharmacokinetic interaction between TMC114/ritonavir and tenofovir disoproxil fumarate in healthy volunteers. Br. J. Clin. Pharmacol.64(5), 655–661 (2007).
   PubMed Web of Science ®Google Scholar
• Sekar VJ, Lefebvre E, Marien K et al. Pharmacokinetic interaction between darunavir and saquinavir in HIV-negative volunteers. Ther. Drug Monit.29(6), 795–801 (2007).
   PubMed Web of Science ®Google Scholar
• Sekar VJ, De Pauw M, Marien K et al. Pharmacokinetic interaction between TMC114/r and efavirenz in healthy volunteers. Antivir. Ther.12(4), 509–514 (2007).
   PubMed Web of Science ®Google Scholar
• Sekar VJ, Lefebvre E, Guzman SS et al. Pharmacokinetic interaction between ethinyl estradiol, norethindrone and darunavir with low-dose ritonavir in healthy women. Antivir. Ther.13(4), 563–569 (2008).
   PubMed Web of Science ®Google Scholar
• Sekar V, Lefebvre E, De Marez T et al. Effect of repeated doses of darunavir plus low-dose ritonavir on the pharmacokinetics of sildenafil in healthy male subjects: Phase I randomized, open-label, two-way crossover study. Clin. Drug Investig.28(8), 479–485 (2008).
   PubMed Web of Science ®Google Scholar
• Sekar VJ, Spinosa-Guzman S, De Paepe E et al. Darunavir/ritonavir pharmacokinetics following coadministration with clarithromycin in healthy volunteers. J. Clin. Pharmacol.48(1), 60–65 (2008).
   PubMed Web of Science ®Google Scholar
• Sekar VJ, Lefebvre E, De Pauw M et al. Pharmacokinetics of darunavir/ritonavir and ketoconazole following co-administration in HIV-healthy volunteers. Br. J. Clin. Pharmacol.66(2), 215–221 (2008).
   PubMed Web of Science ®Google Scholar
• Scholler-Gyure M, Kakuda TN, Sekar V et al. Pharmacokinetics of darunavir/ritonavir and TMC125 alone and coadministered in HIV-negative volunteers. Antivir. Ther.12(5), 789–796 (2007).
   PubMed Web of Science ®Google Scholar
• Sekar VJ, Lefebvre E, De Marez T et al. Pharmacokinetics of darunavir (TMC114) and atazanavir during coadministration in HIV-negative, healthy volunteers. Drugs R D8(4), 241–248 (2007).
   PubMedGoogle Scholar
• Sekar VJ, Lefebvre E, De Paepe E et al. Pharmacokinetic interaction between darunavir boosted with ritonavir and omeprazole or ranitidine in human immunodeficiency virus-negative healthy volunteers. Antimicrob. Agents Chemother.51(3), 958–961 (2007).
   PubMed Web of Science ®Google Scholar
• Rachlis A, Clotet B, Baxter J et al. Safety, tolerability, and efficacy of darunavir (TMC114) with low-dose ritonavir in treatment-experienced, hepatitis B or C co-infected patients in POWER 1 and 3. HIV Clin. Trials8(4), 213–220 (2007).
   PubMed Web of Science ®Google Scholar
• Pacanowski J, Bollens D, Poirier JM et al. Efficacy of darunavir despite low plasma trough levels during late pregnancy in an HIV-hepatitis C virus infected patient. AIDS23, 1923–1930 (2009).
   PubMed Web of Science ®Google Scholar
• Sued O, Lattner J, Gun A et al. Use of darunavir and enfuvirtide in a pregnant woman. Int. J. STD AIDS19, 866–867 (2008).
   PubMed Web of Science ®Google Scholar
• Furco A, Gosrani B, Nicholas S et al. Successful use of darunavir, etravirine, enfuvirtide and tenofovir/emtricitabine in pregnant woman with multiclass HIV resistance. AIDS23, 434–435 (2009).
   PubMed Web of Science ®Google Scholar
• Ripamonti D, Cattaneo D, Cortinovis M et al. Transplacental passage of ritonavir-boosted darunavir in two pregnant women. Int. J. STD AIDS20, 215–216 (2009).
   PubMed Web of Science ®Google Scholar
• Blanche S, Bologna R, Cahn P et al. Pharmacokinetics, safety and efficacy of darunavir/ritonavir in treatment-experienced children and adolescents. AIDS23(15), 2005–2013 (2009).
   PubMed Web of Science ®Google Scholar
• Katlama C, Esposito R, Gatell JM et al. for the POWER 1 Study Group. Efficacy and safety of TMC114/ritonavir in treatment-experienced HIV patients: 24-week results of POWER 1. AIDS21, 395–402 (2007).
   PubMed Web of Science ®Google Scholar
• Haubrich R, Berger D, Chiliade P et al.; for the POWER 2 Study group. Week 24 efficacy and safety of TMC114/ritonavir in treatment-experienced HIV patients. AIDS21(6), F11–F18 (2007).
   PubMed Web of Science ®Google Scholar
• D’Aquila RT, Schapiro JM, Brun-Vezinet F et al. Drug resistance mutations in HIV-1 (IAS-USA). Top. HIV Med.11, 92–96 (2003).
   PubMedGoogle Scholar
• Johnson VA, Brun-Vezinet F, Clotet B et al. Update of the drug resistance mutations in HIV-1 (IAS-USA): 2004. Top. HIV Med.12, 119–124 (2004).
   PubMedGoogle Scholar
• Johnson VA, Brun-Vezinet F, Clotet B et al. Update of the drug resistance mutations in HIV-1 (IAS-USA): 2005. Top. HIV Med.13, 125–131 (2005).
   PubMedGoogle Scholar
• 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. Lancet369(9568), 1169–1178 (2007).
   PubMed Web of Science ®Google Scholar
• Katlama C, Bellos N, Grinsztejn B et al. POWER 1 and 2: combined final 144-week efficacy and safety results for darunavir/ritonavir (DRV/r) 600/100 mg bid in treatmentexperienced HIV patients. Presented at: 9th International Congress on Drug Therapy in HIV Infection. Glasgow, UK, 9–13 November 2008.
   Google Scholar
• 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. Acquir. Immune Defic. Syndr.46(1), 24–31 (2007).
   PubMed Web of Science ®Google Scholar
• Pozniak A, Arasteh K, Molina JM et al. POWER 3 analysis: 144-week efficacy and safety results for darunavir/ritonavir 600/100mg bid in treatment-experienced HIV patients. Presented at: 9th International Congress on Drug Therapy in HIV Infection. Glasgow, UK, 9–13 November 2008.
   Google Scholar
• 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.49, 1441–1449 (2009).
   PubMed Web of Science ®Google Scholar
• Madruga JV, Berger D, McMurchie M et al. Efficacy and safety of darunavir-ritonavir compared with that of lopinavir-ritonavir at 48 weeks in treatment-experienced, HIV-infected patients in TITAN: a randomised controlled Phase III trial. Lancet370(9581), 49–58 (2007).
   PubMed Web of Science ®Google Scholar
• Arribas J, Arathoon E, Gonsalez CR et al. Effects of once-daily (qd) versus twice-daily (bid) darunavir/ritonavir (DRV/r) on lipid parameters at week 48 in treatment-experienced, HIV-1-infected patients with no DRV resistance-associated mutations (RAMs) in the ODIN study. Presented at: 18th International Aids Conference. Vienna, Austria, 18–23 July 2010.
   Google Scholar
• Ortiz R, Dejesus E, Khanlou H et al. Efficacy and safety of once-daily darunavir/ritonavir versus lopinavir/ritonavir in treatment-naive HIV-1-infected patients at week 48. AIDS22(12), 1389–1397 (2008).
   PubMed Web of Science ®Google Scholar
• Mills A, Nelson M, Jayaweera D et al. ARTEMIS: efficacy and safety of darunavir/ritonavir 800/100mg once-daily vs lopinavir/ritonavir in treatment-naive, HIV-1-infected patients at 96 week analysis. AIDS23, 1679–1688 (2009).
   PubMed Web of Science ®Google Scholar
• Arribas J, Horban A, Gerstoft J et al. The MONET trial: darunavir/ritonavir with or without nucleoside analogues, for patients with HIV RNA below 50 copies/ml. AIDS24, 223–230 (2010).
   PubMed Web of Science ®Google Scholar
• Katlama C, Valantin MA, Algarte M et al. Efficacy of darunavir/ritonavir maintenance monotherapy in patients with HIV-1 viral suppression: a randomized open-label, noninferiority trial, MONOI-ANRS 136. AIDS24, 2365–2374 (2010).
   PubMed Web of Science ®Google Scholar
• Banhegyi D, Katlama C, Da Cunha C et al. Phase III TITAN week 96 final analysis: efficacy/safety of darunavir/r (DRV/r) vs. loprinavir/r (LPV/r) in LPV-naive, treatmentexperienced patients. Presented at: 9th International Congress on Drug Therapy in HIV Infection. Glasgow, UK, 9–13 November 2008.
   Google Scholar
• De Meyer S, Vangeneugden T, van Baelen B et al. Resistance profile of darunavir: combined 24-week results from the POWER trials. AIDS Res. Hum. Retroviruses24(3), 379–388 (2008).
   PubMed Web of Science ®Google Scholar
• Rusconi S, Gianotti N, Adorni F et al. Determinants of HIV-1 genotypic resistance to darunavir (TMC114) in a large Italian resistance database (Antiretroviral Resistance Cohort Analysis). J. Acquir. Immune Defic. Syndr.46(3), 373–375 (2007).
   PubMed Web of Science ®Google Scholar
• Poveda E, Anta L, Blanco JL et al. Drug resistance mutations in HIV-infected patients in the Spanish drug resistance database failing tipranavir and darunavir therapy. Antimicrob. Agents Chemother.54(7), 3018–3020 (2010).
   PubMed Web of Science ®Google Scholar
• Lefebvre E, Schiffer C. Resilience to resistance of HIV-1 protease inhibitors: profile of darunavir. AIDS Rev.10, 131–142 (2008).
   PubMed Web of Science ®Google Scholar
• Spagnuolo V, Gianotti N, Seminari E et al. Changes in darunavir/r resistance score after previous failure to tipranavir/r in HIV-1-infected multidrug-resistant patients. J. Acquir. Immune Defic. Syndr.50, 192–195 (2009).
   PubMed Web of Science ®Google Scholar
• Nelson M, Girard PM, DeMasi R et al. Suboptimal adherence to darunavir/ritonavir has minimal effect on efficacy compared with lopinavir/ritonavir in treatment-naive, HIV-infected patients: 96 week ARTEMIS data. J. Antimicrob. Chemother.65, 1505–1509 (2010).
   PubMed Web of Science ®Google Scholar
• Thompson MA, Aberg JA, Cahn P et al. Antiretroviral treatment of adult HIV infection: 2010 recommendations of the International AIDS Society-USA panel. JAMA304, 321–333 (2010).
   PubMed Web of Science ®Google Scholar