Nevirapine once daily: Pharmacology, metabolic profile and efficacy data of the new extended-release formulation

Expert Opinion on Drug Metabolism and Toxicology

Volumn 7, Issue 4, 2011, Pages 495-503

  Parienti, Jean Jacques ^a   Peytavin, Gilles ^b  

^a CAEN UNIVERSITY HOSPITAL   (France)

^b BICHAT HOSPITAL   (France)

Author keywords

efficacy; extended release; HIV infection; nevirapine; once daily; tolerance

Indexed keywords

ATAZANAVIR PLUS RITONAVIR; CHOLESTEROL; EFAVIRENZ; EFAVIRENZ PLUS EMTRICITABINE PLUS TENOFOVIR DISOPROXIL; EMTRICITABINE; EMTRICITABINE PLUS RILPIVIRINE PLUS TENOFOVIR; EMTRICITABINE PLUS TENOFOVIR DISOPROXIL; ETRAVIRINE; HIGH DENSITY LIPOPROTEIN CHOLESTEROL; HYDROXYPROPYLMETHYLCELLULOSE; LAMIVUDINE PLUS NEVIRAPINE PLUS STAVUDINE; LERSIVIRINE; LOW DENSITY LIPOPROTEIN CHOLESTEROL; NEVIRAPINE; RILPIVIRINE; TENOFOVIR; UNCLASSIFIED DRUG;

ANTIVIRAL ACTIVITY; ANTIVIRAL THERAPY; ARTICLE; CONTROLLED DRUG RELEASE; CONTROLLED RELEASE FORMULATION; DOSAGE SCHEDULE COMPARISON; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DOSE REGIMEN; DRUG EFFICACY; DRUG ELIMINATION; DRUG FATALITY; DRUG METABOLISM; DRUG PENETRATION; DRUG PROTEIN BINDING; DRUG SAFETY; DRUG TOLERABILITY; EXTENDED RELEASE FORMULATION; GENETIC POLYMORPHISM; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS 1 INFECTION; IC 50; LIVER TOXICITY; MEDICAL LITERATURE; NONHUMAN; PATIENT COMPLIANCE; RANDOMIZED CONTROLLED TRIAL (TOPIC); RECOMMENDED DRUG DOSE; SIDE EFFECT; SKIN TOXICITY; STRUCTURE ACTIVITY RELATION; SYSTEMATIC REVIEW; TREATMENT RESPONSE; UNSPECIFIED SIDE EFFECT; VIRUS LOAD;

ANTI-HIV AGENTS; CHEMISTRY, PHARMACEUTICAL; CLINICAL TRIALS AS TOPIC; DELAYED-ACTION PREPARATIONS; DRUG EVALUATION; DRUG THERAPY, COMBINATION; DRUG TOLERANCE; DRUG TOXICITY; HIV INFECTIONS; HIV-1; HUMANS; NEVIRAPINE; TREATMENT OUTCOME;

EID: 79952916318     PISSN: 17425255     EISSN: None     Source Type: Journal    
DOI: 10.1517/17425255.2011.565331     Document Type: Article

References (67)

1. Thompson MA, Aberg JA, Cahn P, et al. Antiretroviral treatment of adult HIV infection: 2010 recommendations of the International AIDS Society-USA panel. JAMA 2010;304:321-33
2. Zhang Z, Hamatake R, Hong Z. Clinical utility of current NNRTIs and perspectives of new agents in this class under development. Antivir Chem Chemother 2004;15:121-34 (Pubitemid 38787607)
3. Gazzard B, Bernard AJ, Boffito M, et al. British HIV Association (BHIVA) guidelines for the treatment of HIV-infected adults with antiretroviral therapy (2006). HIV Med 2006;7:487-503 (Pubitemid 44742349)
4. Descamps D, Flandre P, Calvez V, et al. Mechanisms of virologic failure in previously untreated HIV-infected patients from a trial of induction-maintenance therapy. Trilege (Agence Nationale de Recherches sur le SIDA 072) Study Team). JAMA 2000;283:205-11 (Pubitemid 30039220)
5. Bangsberg DR, Perry S, Charlebois ED, et al. Non-adherence to highly active antiretroviral therapy predicts progression to AIDS. AIDS 2001;15:1181-3 (Pubitemid 32549871)
6. Garcia de Olalla P, Knobel H, Carmona A, et al. Impact of adherence and highly active antiretroviral therapy on survival in HIV-infected patients. J Acquir Immune Defic Syndr 2002;30:105-10 (Pubitemid 34506694)
7. Parienti JJ, Massari V, Descamps D, et al. Predictors of virologic failure and resistance in HIV-infected patients treated with nevirapine-or efavirenz-based antiretroviral therapy. Clin Infect Dis 2004;38:1311-6 (Pubitemid 38608576)
8. Parienti JJ, Das-Douglas M, Massari V, et al. Not all missed doses are the same: sustained NNRTI treatment interruptions predict HIV rebound at low-to-moderate adherence levels. PLoS One 2008;3:e2783
9. 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;65:445-8 (Pubitemid 32959067)
10. 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 (Pubitemid 32448520)
11. Antinori A, Zaccarelli M, Cingolani A, et al. Cross-resistance among nonnucleoside reverse transcriptase inhibitors limits recycling efavirenz after nevirapine failure. AIDS Res Hum Retroviruses 2002;18:835-8 (Pubitemid 35034664)
12. Perrin L, Kaiser L, Yerly S. Travel and the spread of HIV-1 genetic variants. Lancet Infect Dis 2003;3:22-7 (Pubitemid 36041785)
13. Andries K, Azijn H, Thielemans T, et al. TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1. Antimicrob Agents Chemother 2004;48:4680-6 (Pubitemid 39577672)
14. Janssen PA, Lewi PJ, Arnold E, et al. In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2- cyanoethenyl]-2,6-dimethylphenyl] amino]-2-pyrimidinyl]amino] benzonitrile (R278474, rilpivirine). J Med Chem 2005;48:1901-9 (Pubitemid 40396320)
15. Lazzarin A, Campbell T, Clotet B, et al. Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-2: 24-week results from a randomised, double-blind, placebo-controlled trial. Lancet 2007;370:39-48 (Pubitemid 47017467)
16. Azijn H, Tirry I, Vingerhoets J, et al. TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. Antimicrob Agents Chemother 2010;54:718-27
17. Corbau R, Mori J, Phillips C, et al. Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1. Antimicrob Agents Chemother 2010;54:4451-63
18. Parienti JJ, Bangsberg DR, Verdon R, Gardner EM. Better adherence with once-daily antiretroviral regimens: a meta-analysis. Clin Infect Dis 2009;48:484-8
19. Laurent C, Kouanfack C, Koulla-Shiro S, et al. Effectiveness and safety of a generic fixed-dose combination of nevirapine, stavudine, and lamivudine in HIV-1-infected adults in Cameroon: open-label multicentre trial. Lancet 2004;364:29-34 (Pubitemid 38968622)
20. Frampton JE, Croom KF. Efavirenz/emtricitabine/tenofovir disoproxil fumarate: triple combination tablet. Drugs 2006;66:1501-12; discussion 1513-14
21. Merluzzi VJ, Hargrave KD, Labadia M, et al. Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor. Science 1990;250:1411-13 (Pubitemid 120031860)
22. Montaner JS, Reiss P, Cooper D, et al. A randomized, double-blind trial comparing combinations of nevirapine, didanosine, and zidovudine for HIV-infected patients: the INCAS Trial. Italy, The Netherlands, Canada and Australia Study. JAMA 1998;279:930-7 (Pubitemid 28136082)
23. Smerdon SJ, Jager J, Wang J, et al. Structure of the binding site for nonnucleoside inhibitors of the reverse transcriptase of human immunodeficiency virus type 1. Proc Natl Acad Sci USA 1994;91:3911-15 (Pubitemid 24139542)
24. Esnouf R, Ren J, Ross C, et al. Mechanism of inhibition of HIV-1 reverse transcriptase by non-nucleoside inhibitors. Nat Struct Biol 1995;2:303-8
25. Zhang H, Dornadula G, Wu Y, et al. Kinetic analysis of intravirion reverse transcription in the blood plasma of human immunodeficiency virus type 1-infected individuals: direct assessment of resistance to reverse transcriptase inhibitors in vivo. J Virol 1996;70:628-34 (Pubitemid 126508837)
26. Koup RA, Merluzzi VJ, Hargrave KD, et al. Inhibition of human immunodeficiency virus type 1 (HIV-1) replication by the dipyridodiazepinone BI-RG-587. J Infect Dis 1991;163:966-70
27. Havlir DV, Eastman S, Gamst A, Richman DD. Nevirapine-resistant human immunodeficiency virus: kinetics of replication and estimated prevalence in untreated patients. J Virol 1996;70:7894-9 (Pubitemid 26339097)
28. Cheeseman SH, Havlir D, McLaughlin MM, et al. Phase I/II evaluation of nevirapine alone and in combination with zidovudine for infection with human immunodeficiency virus. J Acquir Immune Defic Syndr Hum Retrovirol 1995;8:141-51
29. Raffi F, Bonnet B, Ferre V, et al. Substitution of a nonnucleoside reverse transcriptase inhibitor for a protease inhibitor in the treatment of patients with undetectable plasma human immunodeficiency virus type 1 RNA. Clin Infect Dis 2000;31:1274-8 (Pubitemid 32295461)
30. Mirochnick M, Fenton T, Gagnier P, et al. Pharmacokinetics of nevirapine in human immunodeficiency virus type 1-infected pregnant women and their neonates. Pediatric AIDS Clinical Trials Group Protocol 250 Team. J Infect Dis 1998;178:368-74 (Pubitemid 28347918)
31. Havlir D, Cheeseman SH, McLaughlin M, et al. High-dose nevirapine: safety, pharmacokinetics, and antiviral effect in patients with human immunodeficiency virus infection. J Infect Dis 1995;171:537-45
32. Rotger M, Colombo S, Furrer H, et al. Influence of CYP2B6 polymorphism on plasma and intracellular concentrations and toxicity of efavirenz and nevirapine in HIV-infected patients. Pharmacogenet Genomics 2005;15:1-5 (Pubitemid 43205520)
33. Penzak SR, Kabuye G, Mugyenyi P, et al. Cytochrome P450 2B6 (CYP2B6) G516T influences nevirapine plasma concentrations in HIV-infected patients in Uganda. HIV Med 2007;8:86-91 (Pubitemid 46390844)
34. Mahungu T, Smith C, Turner F, et al. Cytochrome P450 2B6 516G-T is associated with plasma concentrations of nevirapine at both 200 mg twice daily and 400 mg once daily in an ethnically diverse population. HIV Med 2009;10:310-17
35. Ritchie MD, Haas DW, Motsinger AA, et al. Drug transporter and metabolizing enzyme gene variants and nonnucleoside reverse-transcriptase inhibitor hepatotoxicity. Clin Infect Dis 2006;43:779-82 (Pubitemid 44330745)
36. Haas DW, Bartlett JA, Andersen JW, et al. Pharmacogenetics of nevirapine-associated hepatotoxicity: an Adult AIDS Clinical Trials Group collaboration. Clin Infect Dis 2006;43:783-6 (Pubitemid 44330746)
37. Veldkamp AI, Weverling GJ, Lange JM, et al. High exposure to nevirapine in plasma is associated with an improved virological response in HIV-1-infected individuals. AIDS 2001;15:1089-95 (Pubitemid 32549859)
38. Macha S, Yong CL, Darrington T, et al. In vitro-in vivo correlation for nevirapine extended release tablets. Biopharm Drug Dispos 2009;30:542-50
39. Battegay ME, Arasteh K, Plettenberg A, et al. Assessment of the steady-state PK parameters of two extended release (XR) nevirapine (NVP) tablets 400 mg and 300 mg QD compared with immediate release (IR) NVP tablets 200 mg BID in HIV-1-infected patients -the ERVIR study [abstract PE4.1/2]. 12th Eur AIDS Conf (EACS); 11 -14 November 2009; Cologne
40. van Leth F, Phanuphak P, Ruxrungtham K, et al. Comparison of first-line antiretroviral therapy with regimens including nevirapine, efavirenz, or both drugs, plus stavudine and lamivudine: a randomised open-label trial, the 2NN Study. Lancet 2004;363:1253-63 (Pubitemid 38496486)
41. Soriano V, Koeppe S, Mingrone H, et al. Prospective comparison of nevirapine and atazanavir/ritonavir both combined with tenofovir DF/emtricitabine in treatment-naive HIV-1 infected patients: ARTEN study week 48 results [abstract LBPEB07]. 5th International AIDS Society Conference on HIV Pathogenesis, Treatment, and Prevention (IAS); 19 -22 July 2009; Cape Town, South Africa
42. DeJesus E, Mills A, Bhatti L, et al. Nevirapine (NVP) vs ritonavir-boosted atazanavir (ATV/r) combined with tenofovir/emtricitabine (TDF/FTC) in first-line therapy: NEWART 48-week data. J Int AIDS Soc 2010;13(Suppl 4):P4
43. Gathe J, Knecht G, Orrell C, et al. 48 Week efficacy, pharmacokinetics and safety of once a day 400 mg nevirapine extended release formulation for treatment of antiretroviral naive HIV-1 infected patients (VERxVE) [abstract H-1808]. 50th Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC); 12 -15 September 2010; Boston
44. Negredo E, Cruz L, Paredes R, et al. Virological, immunological, and clinical impact of switching from protease inhibitors to nevirapine or to efavirenz in patients with human immunodeficiency virus infection and long-lasting viral suppression. Clin Infect Dis 2002;34:504-10 (Pubitemid 34112272)
45. Ena J, Leach A, Nguyen P. Switching from suppressive protease inhibitor-based regimens to nevirapine-based regimens: a meta-analysis of randomized controlled trials. HIV Med 2008;9:747-56
46. Martinez E, Arnaiz JA, Podzamczer D, et al. Substitution of nevirapine, efavirenz, or abacavir for protease inhibitors in patients with human immunodeficiency virus infection. N Engl J Med 2003;349:1036-46 (Pubitemid 37087618)
47. Arasteh K, Ward D, Plettenberg A, et al. 48 Wk efficacy and safety of switching virologically stable HIV-1 patients from nevirapine IR 200 mg BID to nevirapine XR 400 mg QD (TRANxITION). 10th International Congress on Drug Therapy in HIV Infection; 7 -11 November 2010; Glasgow
48. Kesselring AM, Wit FW, Sabin CA, et al. Risk factors for treatment-limiting toxicities in patients starting nevirapine-containing antiretroviral therapy. AIDS 2009;23:1689-99
49. Parienti JJ, Verdon R. Nevirapine and cardiovascular risk. Med Mal Infect 2010;40:499-505
50. Calza L, Manfredi R, Colangeli V, et al. Substitution of nevirapine or efavirenz for protease inhibitor versus lipid-lowering therapy for the management of dyslipidaemia. AIDS 2005;19:1051-8 (Pubitemid 40961145)
51. Parienti JJ, Massari V, Rey D, et al. Efavirenz to nevirapine switch in HIV-1-infected patients with dyslipidemia: a randomized, controlled study. Clin Infect Dis 2007;45:263-6 (Pubitemid 47041021)
52. Sankatsing RR, Wit FW, Pakker N, et al. Effects of nevirapine, compared with lamivudine, on lipids and lipoproteins in HIV-1-uninfected newborns: the stopping infection from mother-to-child via breast-feeding in Africa lipid substudy. J Infect Dis 2007;196:15-22 (Pubitemid 46982732)
53. Friis-Moller N, Reiss P, Sabin CA, et al. Class of antiretroviral drugs and the risk of myocardial infarction. N Engl J Med 2007;356:1723-35 (Pubitemid 46658704)
54. Phillips AN, Carr A, Neuhaus J. Interruption of ART and risk of cardiovascular disease:findings from SMART [abstract 41]. 14th Conference on Retroviruses and Opportunistic Infection (CROI); 25 -28 February 2007; Los Angeles
55. Clotet B, van der Valk M, Negredo E, Reiss P. Impact of nevirapine on lipid metabolism. J Acquir Immune Defic Syndr 2003;34(Suppl 1):S79-84 . An important review of the impact of nevirapine on lipid profile (Pubitemid 37158637)
56. Lundgren JD, Reiss P, Worm S. Risk of myocardial infarction with exposure to specific ARV from the PI, NNRTI, and NRTI drug classes: The D:A:D study [abstract 44LB]. 16th Conference on Retroviruses and Opportunistic Infections (CROI); 8 -11 February 2009; Montreal, Canada
57. Letendre S, Ellis R, Deutsch R, et al.; and the Charter group. Correlates of time-to-loss-of-viral-response in CSF and plasma in the CHARTER Cohort [abstract 430]. Seventeenth Conference on Retroviruses and Opportunistic Infections; San Francisco; 2010
58. Bonora S, Nicastri E, Calcagno A, et al. Ultrasensitive assessment of residual HIV viraemia in HAART-treated patients with persistently undetectable plasma HIV-RNA: a cross-sectional evaluation. J Med Virol 2009;81:400-5
59. Haim-Boukobzai S, Morand-Joubert L, Flandre P, et al. Residual plasma viraemia below 40 copies/ml under NNRTI-based regimen [abstract 134]. International HIV and Hepatitis Drug Resistance Workshop; 8 -12 June 2010; Dubrovnik, Croatia
60. Reliquet V, Allavena C, Morineau-Le Houssine P, et al. Twelve-year experience of nevirapine use: benefits and convenience for long-term management in a French cohort of HIV-1-infected patients. HIV Clin Trials 2010;11:110-17
61. Elzi L, Marzolini C, Furrer H, et al. Treatment modification in human immunodeficiency virus-infected individuals starting combination antiretroviral therapy between 2005 and 2008. Arch Intern Med 2010;170:57-65
62. Willig JH, Abroms S, Westfall AO, et al. Increased regimen durability in the era of once-daily fixed-dose combination antiretroviral therapy. AIDS 2008;22:1951-60
63. Parienti JJ, Massari V, Reliquet V, et al. Effect of twice-daily nevirapine on adherence in HIV-1-infected patients: a randomized controlled study. AIDS 2007;21:2217-22 (Pubitemid 350287220)
64. Martin AM, Nolan D, James I, et al. Predisposition to nevirapine hypersensitivity associated with HLA-DRB1*0101 and abrogated by low CD4 T-cell counts. AIDS 2005;19:97-9 (Pubitemid 40111026)
65. Vitezica ZG, Milpied B, Lonjou C, et al. HLA-DRB1*01 associated with cutaneous hypersensitivity induced by nevirapine and efavirenz. AIDS 2008;22:540-1 (Pubitemid 351317299)
66. Rodriguez-Arrondo F, Aguirrebengoa K, Portu J, et al. Long-term effectiveness and safety outcomes in HIV-1-infected patients after a median time of 6 years on nevirapine. Curr HIV Res 2009;7:526-32
67. Schouten JT, Krambrink A, Ribaudo HJ, et al. Substitution of nevirapine because of efavirenz toxicity in AIDS clinical trials group A5095. Clin Infect Dis 2010;50:787-91