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Darunavir/cobicistat once daily for the treatment of HIV

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References

  • Maltêz F, Doroana M, Branco T, Valente C. Recent advances in antiretroviral treatment and prevention in HIV-infected patients. Curr Opin HIV AIDS 2011;6(Suppl 1):S21-30
  • Mathis S, Khanlari B, Pulido F, et al. Effectiveness of protease inhibitor monotherapy versus combination antiretroviral maintenance therapy: a meta-analysis. PLoS One 2011;6:e22003
  • Llibre JM, Arribas JR, Domingo P, et al. Clinical implications of fixed-dose coformulations of antiretrovirals on the outcome of HIV-1 therapy. AIDS 2011;25(14):1683-90
  • Günthard HF, Aberg JA, Eron JJ, et al. Antiretroviral treatment of adult HIV infection: 2014 Recommendations of the International Antiviral Society–USA Panel. JAMA 2014;312(4):410-25
  • DHHS guidelines: Panel on antiretroviral guidelines for adults and adolescents. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents. Department of Health and Human Services. Available from: www.aidsinfo.nih.gov/ContentFiles/AdultandAdolescentGL.pdf [Last accessed January 9, 2015]
  • EACS European Guidelines for treatment of HIV infected adults in Europe. Version 7.1. Updated November 2014. Available from: www.eacsociety.org/files/guidelines_english_71_141204.pdf [Last accessed 9 Jan 2015]
  • BHIVA. British HIV Association guidelines for the treatment of HIV-1-positive adults with antiretroviral therapy 2012 (Updated November 2013). HIV Med 2014;15(Suppl 1):1-85
  • 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 2008;22(12):1389-97
  • Mills AM, Nelson M, Jayaweera D, et al. Once-daily darunavir/ritonavir vs. lopinavir/ritonavir in treatment-naive, HIV-1-infected patients: 96-week analysis. AIDS 2009;23(13):1679-88
  • Cahn P, Fourie J, Grinsztejn B, et al. Week 48 analysis of once-daily vs. twice-daily darunavir/ritonavir in treatment-experienced HIV-1-infected patients. AIDS 2011;25(7):929-39
  • Orkin C, DeJesus E, Khanlou H, et al. Final 192-week efficacy and safety of once-daily darunavir/ritonavir compared with lopinavir/ritonavir in HIV-1-infected treatment-naive patients in the ARTEMIS trial. HIV Med 2013;14(1):49-59
  • Kakuda TN, Brochot A, van de Casteele T, et al. Establishing darunavir dosing recommendations in treatment-naive and treatment-experienced pediatric patients. In: abstracts of the Fourteenth International Workshop on Clinical Pharmacology in HIV. Amsterdam, The Netherlands. O_13 2013
  • 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(9568):1169-78
  • 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 Syndr 2007;46(1):24-31
  • Bánhegyi D, Katlama C, da Cunha CA, et al. Week 96 efficacy, virology and safety of darunavir/r versus lopinavir/r in treatment-experienced patients in TITAN. Curr HIV Res 2012;10(2):171-81
  • Hull MW, Montaner JS. Ritonavir-boosted protease inhibitors in HIV therapy. Ann Med 2011;43(5):375-88
  • Merry C, Barry MG, Mulcahy F, et al. Saquinavir pharmacokinetics alone and in combination with ritonavir in HIV-infected patients. AIDS 1997;11(4):F29-33
  • Zeldin RK, Petruschke RA. Pharmacological and therapeutic properties of ritonavir-boosted protease inhibitor therapy in HIV-infected patients. J Antimicrob Chemother 2004;53(1):4-9
  • Palella FJJr, Delaney KM, Moorman AC, et al. Declining morbidity and mortality among patients with advanced human immunodeficiency virus infection. HIV Outpatient Study Investigators. N Engl J Med 1998;338(13):853-60
  • Samaras K, Richardson R, Carr A. Postprandial lipid effects of low-dose ritonavir vs. raltegravir in HIV-uninfected patients. AIDS 2010;24(11):1727-31
  • Xu L, Lu H, Murray BP, et al. Cobicistat (GS-9350): a potent and selective inhibitor of human CYP3A as a novel pharmacoenhancer. ACS Med Chem Lett 2010;1(5):209-13
  • Xu L, Liu H, Hong A, et al. Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers. Part II: P2/P3 region and discovery of cobicistat (GS-9350). Bioorg Med Chem Lett 2014;24(3):995-9
  • Mathias AA, German P, Murray BP, et al. Pharmacokinetics and pharmacodynamics of GS-9350: a novel pharmacokinetic enhancer without anti-HIV activity. Clin Pharmacol Ther 2010;87(3):322-9
  • German P, Warren D, West S, et al. Pharmacokinetics and bioavailability of an integrase and novel pharmacoenhancer-containing single-tablet fixed-dose combination regimen for the treatment of HIV. J Acquir Immune Defic Syndr 2010;55(3):323-9
  • Ramanathan S, Warren D, Wei L, Kearney BP. Pharmacokinetic boosting of atazanavir with the pharmacoenhancer GS-9350 versus ritonavir. 49th Interscience Conference on Antimicrobial Agents and Chemotherapy; San Francisco, CA, USA. A1-1301 2009
  • Gallant JE, Koenig E, Andrade-Villanueva J, et al. Cobicistat versus ritonavir as a pharmacoenhancer of atazanavir plus emtricitabine/tenofovir disoproxil fumarate in treatment-naive HIV type 1-infected patients: week 48 results. J Infect Dis 2013;208(1):32-9
  • Elion R, Cohen C, Gathe J, et al. Phase 2 study of cobicistat versus ritonavir each with once-daily atazanavir and fixed-dose emtricitabine/tenofovir DF in the initial treatment of HIV infection. AIDS 2011;25(15):1881-6
  • Shah BM, Schafer JJ, Priano J, Squires KE. Cobicistat: a new boost for the treatment of human immunodeficiency virus infection. Pharmacotherapy 2013;33(10):1107-16
  • Zolopa A, Sax PE, DeJesus E, et al. A randomized double-blind comparison of coformulated elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate versus efavirenz/emtricitabine/tenofovir disoproxil fumarate for initial treatment of HIV-1 infection: analysis of week 96 results. J Acquir Immune Defic Syndr 2013;63(1):96-100
  • Rockstroh JK, DeJesus E, Henry K, et al. A randomized, double-blind comparison of coformulated elvitegravir/cobicistat/emtricitabine/tenofovir DF vs ritonavir-boosted atazanavir plus coformulated emtricitabine and tenofovir DF for initial treatment of HIV-1 infection: analysis of week 96 results. J Acquir Immune Defic Syndr 2013;62(5):483-6
  • 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(6):2314-21
  • 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(10):3123-9
  • Back D, Sekar V, Hoetelmans RM. Darunavir: pharmacokinetics and drug interactions. Antivir Ther 2008;13(1):1-13
  • Kakuda TN, Brochot A, Tomaka F, et al. Pharmacokinetics and pharmacodynamics of boosted once-daily darunavir. J Antimicrob Chemother 2014;69(10):2591-605
  • German P, Liu HC, Szwarcberg J, et al. Effect of cobicistat on glomerular filtration rate in subjects with normal and impaired renal function. J Acquir Immune Defic Syndr 2012;61(1):32-40
  • Lepist EI, Zhang X, Hao J, et al. Contribution of the organic anion transporter OAT2 to the renal active tubular secretion of creatinine and mechanism for serum creatinine elevations caused by cobicistat. Kidney Int 2014;86(2):350-7
  • Lepist EI, Phan TK, Roy A, et al. Cobicistat boosts the intestinal absorption of transport substrates, including HIV protease inhibitors and GS-7340, in vitro. Antimicrob Agents Chemother 2012;56(10):5409-13
  • Lee WA, He GX, Eisenberg E, et al. Selective intracellular activation of a novel prodrug of the human immunodeficiency virus reverse transcriptase inhibitor tenofovir leads to preferential distribution and accumulation in lymphatic tissue. Antimicrob Agents Chemother 2005;49(5):1898-906
  • Ruane PJ, DeJesus E, Berger D, et al. Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of tenofovir alafenamide as 10-day monotherapy in HIV-1-positive adults. J Acquir Immune Defic Syndr 2013;63(4):449-55
  • Foisy MM, Yakiwchuk EM, Hughes CA. Induction effects of ritonavir: implications for drug interactions. Ann Pharmacother 2008;42(7):1048-59
  • Yeh RF, Gaver VE, Patterson KB, et al. Lopinavir/ritonavir induces the hepatic activity of cytochrome P450 enzymes CYP2C9, CYP2C19, and CYP1A2 but inhibits the hepatic and intestinal activity of CYP3A as measured by a phenotyping drug cocktail in healthy volunteers. J Acquir Immune Defic Syndr 2006;42(1):52-60
  • Custodio J, Garner W, Jin F, et al. Evaluation of the drug interaction potential between the pharmacokinetic enhancer cobicistat and tenofovir disoproxil fumarate in healthy subjects. 14th International Workshop on Clinical Pharmacology of HIV Therapy; Amsterdam, The Netherlands. O_07 2013
  • Stray KM, Bam RA, Birkus G, et al. Evaluation of the effect of cobicistat on the in vitro renal transport and cytotoxicity potential of tenofovir. Antimicrob Agents Chemother 2013;57(10):4982-9
  • German P, et al. The effect of cobicistat and cytochrome P450 2D6, 2B6 and P-glycoprotein using phenotypic probes. 12th International Workshop on Clinical Pharmacology of HIV Therapy. Abstract in Virology Education B.V Utrecht, The Netherlands; 2011
  • Custodio JM, Wang H, Hao J, et al. Pharmacokinetics of cobicistat boosted-elvitegravir administered in combination with rosuvastatin. J Clin Pharmacol 2013;54(6):649-56
  • Bruce RD, Winkle P, Custodio JM, et al. Investigation of the interactions between methadone and elvitegravir-cobicistat in subjects receiving chronic methadone maintenance. Antimicrob Agents Chemother 2013;57(12):6154-7
  • Bruce RD, Winkle P, Custodio JM, et al. The pharmacokinetic and pharmacodynamic interactions between buprenorphine/naloxone and elvitegravir/cobicistat in subjects receiving chronic buprenorphine/naloxone treatment. J Acquir Immune Defic Syndr 2013;63(4):480-4
  • Ramanathan S, Wang H, Custodio J, et al. Lack of clinically relevant drug interactions between GS-7340 and efavirenz. 13th International Workshop on Clinical Pharmacology of HIV Therapy; April 16-18 2012. Barcelona; Abstract P_08
  • Mathias AA, Liu HC, Warren D, et al. Relative bioavailability and pharmacokinetics of darunavir when boosted with the pharmacoenhancer GS-9350 versus ritonavir. 11th International Workshop on Clinical Pharmacology of HIV Therapy; Sorrento, Italy. 28 2010
  • Kakuda TN, Opsomer M, Timmers M, et al. Pharmacokinetics of darunavir in fixed-dose combination with cobicistat compared with coadministration of darunavir and ritonavir as single agents in healthy volunteers. J Clin Pharmacol 2014;54(8):949-57
  • Clinicaltrials.gov. A study to assess the bioequivalence of darunavir when co-administrated with cobicistat under fed and fasted conditions. Available from: https://clinicaltrials.gov/ct2/show/NCT01619527
  • Kakuda TN, Van De Casteele T, Petrovic R, et al. Bioequivalence of a darunavir/cobicistat fixed-dose combination tablet versus single agents and food effect in healthy volunteers. Antivir Ther 2014;19(6):597-606
  • Clinicaltrials.gov. Safety and efficacy of cobicistat-boosted darunavir in HIV infected adults. Available from: https://clinicaltrials.gov/ct2/show/NCT01440569
  • Tashima K, Ortiz R, Kakuda TN, et al. Cobicistat-boosted darunavir in HIV-1-infected adults: week 48 results of a phase 3b, open-label single-arm trial. AIDS Res Ther 2014;11:39
  • Pharmacokinetics, safety, and efficacy of cobicistat-boosted atazanavir or cobicistat-boosted darunavir in HIV-1 infected, treatment-experienced, virologically suppressed pediatric subjects. Available from: https://clinicaltrials.gov/ct2/show/NCT02016924
  • Safety and efficacy of darunavir/cobicistat/emtricitabine/GS-7340 single tablet regimen versus cobicistat-boosted darunavir plus emtricitabine/tenofovir disoproxil fumarate fixed dose combination in HIV-1 infected, antiretroviral treatment naive adults. Available from: https://clinicaltrials.gov/ct2/show/NCT01565850
  • Mills A, Ortiz R, Crofoot G, et al. 48 Week study of the first PI-based single tablet-regimen (STR) darunavir/cobicistat/emtricitabine/tenofovir alafenamide (D/C/F/TAF) vs. cobicistat (COBI)-boosted darunavir (DRV) and emtricitabine/tenofovir disoproxil fumarate (F/TDF) in treatment-naïve (TN) adults. 54th Interscience Conference on Antimicrobial Agents and Chemotherapy. Washington, DC, USA. H-647c 2014
  • Sekar V, Vanden Abeele C, Van Baelen B, et al. Pharmacokinetic-pharmacodynamic analyses of once-daily darunavir-ritonavir in the ARTEMIS study. 15th Conference on Retroviruses and Opportunistic Infections; Boston, MA, USA. 769 2008
  • Sekar V, De La Rosa G, Van de Casteele T, et al. Pharmacokinetic (PK) and pharmacodynamic analyses of once- and twice-daily darunavir/ritonavir (DRV/r) in the ODIN trial. 10th International Conference on Drug Therapy in HIV Infection; Glasgow, UK. P185 2010
  • Van Sanden S, Thilakarathne P, Opsomer M, et al. Non-inferiority of once-daily cobicistat-boosted darunavir versus ritonavir-boosted darunavir in HIV-1-infected patients: a comparative analysis of pooled phase 3 data. ISPOR 17th Annual European Congress. Amsterdam, The Netherlands. PIN1 2014
  • Clotet B, Feinberg J, van Lunzen J, et al. Once-daily dolutegravir versus darunavir plus ritonavir in antiretroviral-naive adults with HIV-1 infection (FLAMINGO): 48 week results from the randomised open-label phase 3b study. Lancet 2014;383(9936):2222-31
  • Molina JM, Clotet B, van Lunzen J, et al. Once-daily dolutegravir is superior to once-daily darunavir/ritonavir in treatment-naïve HIV-1-positive individuals: 96 week results from FLAMINGO. J Int AIDS Soc 2014;17(4 Suppl 3):19490
  • Custodio JM, Guo S, Lawson EB, et al. Lack of clinically relevant drug interactions between elvitegravir/cobicistat/emtricitabine/tenofovir disoproxil fumarate and telaprevir. 53rd Interscience Conference on Antimicrobial Agents and Chemotherapy. Denver, CO, USA. A-1576 2013
  • Ramanathan S, Wang H, Stondell T, et al. Pharmacokinetics and drug interaction profile of cobicistat boosted-EVG with atazanavir, rosuvastatin or rifabutin. 13th International Workshop on Clinical Pharmacology of HIV Therapy; Barcelona, Spain. O_03 2012

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