Darunavir: An effective protease inhibitor for HIV-infected patients

Expert Review of Anti-Infective Therapy

Volumn 9, Issue 6, 2011, Pages 631-643

  Phung, Bao Chau ^a   Yeni, Patrick ^a  

^a BICHAT HOSPITAL   (France)

Author keywords

darunavir; protease inhibitor; resistance profile; ritonavir; tolerance

Indexed keywords

AMPRENAVIR; CLARITHROMYCIN; CYTOCHROME P450 2D6; CYTOCHROME P450 3A; CYTOCHROME P450 3A4; DARUNAVIR; EFAVIRENZ; EMTRICITABINE; ENFUVIRTIDE; ETRAVIRINE; FOSAMPRENAVIR PLUS RITONAVIR; HUMAN IMMUNODEFICIENCY VIRUS PROTEINASE; INDINAVIR; ITRACONAZOLE; KETOCONAZOLE; LOPINAVIR; LOPINAVIR PLUS RITONAVIR; MARAVIROC; NELFINAVIR; NONNUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITOR; OMEPRAZOLE; RALTEGRAVIR; RANITIDINE; RIFABUTIN; RITONAVIR; RNA DIRECTED DNA POLYMERASE INHIBITOR; SAQUINAVIR; TENOFOVIR; UNINDEXED DRUG; VIRUS RNA;

AGE; ALANINE AMINOTRANSFERASE BLOOD LEVEL; ANTIVIRAL ACTIVITY; ANTIVIRAL RESISTANCE; ARTICLE; ASPARTATE AMINOTRANSFERASE BLOOD LEVEL; BINDING AFFINITY; BODY WEIGHT; CD4 LYMPHOCYTE COUNT; CHOLESTEROL BLOOD LEVEL; COMBINATION CHEMOTHERAPY; CROSS RESISTANCE; DIARRHEA; DISTRIBUTION VOLUME; DOSAGE SCHEDULE COMPARISON; DRUG ABSORPTION; DRUG BINDING; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DOSE INCREASE; DRUG DOSE REGIMEN; DRUG EFFICACY; DRUG ELIMINATION; DRUG ERUPTION; DRUG HALF LIFE; DRUG INDUCED HEADACHE; DRUG METABOLISM; DRUG OXIDATION; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SAFETY; DRUG STRUCTURE; DRUG TOLERABILITY; DRUG WITHDRAWAL; FATIGUE; FOOD; FOOD DRUG INTERACTION; GAMMA GLUTAMYL TRANSFERASE BLOOD LEVEL; HEPATITIS B; HEPATITIS C; HERPES SIMPLEX; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; HYDROGEN BOND; HYPERGLYCEMIA; KIDNEY DYSFUNCTION; LIVER DYSFUNCTION; LIVER TOXICITY; LOW DRUG DOSE; MIXED INFECTION; MONOTHERAPY; MULTIDRUG RESISTANCE; NAUSEA; PREGNANCY; RECOMMENDED DRUG DOSE; RHINOPHARYNGITIS; SIDE EFFECT; SKIN MANIFESTATION; STEVENS JOHNSON SYNDROME; TOXIC EPIDERMAL NECROLYSIS; TOXIC HEPATITIS; TRIACYLGLYCEROL BLOOD LEVEL; UPPER RESPIRATORY TRACT INFECTION; VIREMIA; VIRUS LOAD; VIRUS MUTATION; VOMITING;

DRUG ADMINISTRATION ROUTES; DRUG ADMINISTRATION SCHEDULE; DRUG RESISTANCE, VIRAL; DRUG THERAPY, COMBINATION; HIV INFECTIONS; HIV PROTEASE INHIBITORS; HIV-1; HUMANS; LOPINAVIR; MULTICENTER STUDIES AS TOPIC; RANDOMIZED CONTROLLED TRIALS AS TOPIC; RITONAVIR; RNA, VIRAL; SULFONAMIDES; TREATMENT OUTCOME; VIRAL LOAD; VIRUS REPLICATION;

EID: 79959743059     PISSN: 14787210     EISSN: 17448336     Source Type: Journal    
DOI: 10.1586/eri.11.48     Document Type: Article

References (53)

1. 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 (Pubitemid 28135961)
2. Bartlett JA, DeMasi R, Quinn J et al. Overview of the effectiveness of triple combination therapy in antiretroviral-naive HIV-1 infected adults. AIDS 15, 1369-1377 (2001 (Pubitemid 32663904)
3. 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. AIDS 14, 1203-1210 (2000 (Pubitemid 30420664)
4. 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 (Pubitemid 37229567)
5. 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 (Pubitemid 39390785)
6. 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 (Pubitemid 40403065)
7. 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 (Pubitemid 350247878)
8. 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 (Pubitemid 38447090)
9. 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 (Pubitemid 40396314)
10. 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 (Pubitemid 40734460)
11. 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 (Pubitemid 46465961)
12. 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 (Pubitemid 46355280)
13. Back D, Sekar V, Hoetelmans RM. Darunavir: pharmacokinetics and drug interactions. Antivir. Ther. 13(1), 1-13 (2008 (Pubitemid 351541670)
14. 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 (Pubitemid 47568821)
15. 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 (Pubitemid 350190857)
16. 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 (Pubitemid 47041149)
17. 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 (Pubitemid 352016719)
18. 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 (Pubitemid 351948050)
19. 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 (Pubitemid 350292277)
20. 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
21. 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 (Pubitemid 47235493)
22. Sekar VJ, Lefebvre E, De Marez T et al. Pharmacokinetics of darunavir (TMC114) and atazanavir during coadministration in HIV-negative, healthy volunteers. Drugs R D 8(4), 241-248 (2007 (Pubitemid 47026341)
23. 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 (Pubitemid 46355280)
24. 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. Trials 8(4), 213-220 (2007 (Pubitemid 47327458)
25. 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. AIDS 23, 1923-1930 (2009
26. Sued O, Lattner J, Gun A et al. Use of darunavir and enfuvirtide in a pregnant woman. Int. J. STD AIDS 19, 866-867 (2008
27. Furco A, Gosrani B, Nicholas S et al. Successful use of darunavir, etravirine, enfuvirtide and tenofovir/emtricitabine in pregnant woman with multiclass HIV resistance. AIDS 23, 434-435 (2009
28. Ripamonti D, Cattaneo D, Cortinovis M et al. Transplacental passage of ritonavir-boosted darunavir in two pregnant women. Int. J. STD AIDS 20, 215-216 (2009
29. Blanche S, Bologna R, Cahn P et al. Pharmacokinetics, safety and efficacy of darunavir/ritonavir in treatment-experienced children and adolescents. AIDS 23(15), 2005-2013 (2009
30. 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. AIDS 21, 395-402 (2007
31. 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. AIDS 21(6), F11-F18 (2007 (Pubitemid 46568621)
32. D'Aquila RT, Schapiro JM, Brun-Vezinet F et al. Drug resistance mutations in HIV-1 (IAS-USATop. HIV Med. 11, 92-96 (2003
33. 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
34. 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
35. 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 369(9568), 1169-1178 (2007 (Pubitemid 46541620)
36. 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.
37. 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 (Pubitemid 47514614)
38. 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.
39. 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
40. 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. Lancet 370(9581), 49-58 (2007 (Pubitemid 47023100)
41. 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.
42. 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. AIDS 22(12), 1389-1397 (2008
43. 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. AIDS 23, 1679-1688 (2009
44. 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. AIDS 24, 223-230 (2010
45. 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. AIDS 24, 2365-2374 (2010
46. 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.
47. 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. Retroviruses 24(3), 379-388 (2008 (Pubitemid 351457745)
48. 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 AnalysisJ. Acquir. Immune Defic. Syndr. 46(3), 373-375 (2007 (Pubitemid 350287370)
49. 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
50. Lefebvre E, Schiffer C. Resilience to resistance of HIV-1 protease inhibitors: profile of darunavir. AIDS Rev. 10, 131-142 (2008
51. 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
52. 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
53. Thompson MA, Aberg JA, Cahn P et al. Antiretroviral treatment of adult HIV infection: 2010 recommendations of the International AIDS Society-USA panel. JAMA 304, 321-333 (2010