NNRTIs: Pharmacological data

Medecine et Maladies Infectieuses

Volumn 42, Issue 7, 2012, Pages 287-295

  Dellamonica, P ^a   Di Perri, G ^b   Garraffo, R ^a  

^a UNIVERSITÉ CÔTE D'AZUR   (France)

^b UNIVERSITY OF TURIN   (Italy)

Author keywords

Efavirenz; HIV reservoir; Nevirapine

Indexed keywords

ABACAVIR; ANTIRETROVIRUS AGENT; ATAZANAVIR; DARUNAVIR; DELAVIRDINE; DIDANOSINE; EFAVIRENZ; ENFUVIRTIDE; ETRAVIRINE; FOSAMPRENAVIR; INDINAVIR; LAMIVUDINE; LERSIVIRINE; LOPINAVIR; MARAVIROC; NELFINAVIR; NEVIRAPINE; NONNUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITOR; RALTEGRAVIR; RILPIVIRINE; RITONAVIR; RNA DIRECTED DNA POLYMERASE INHIBITOR; SAQUINAVIR; STAVUDINE; TENOFOVIR; TIPRANAVIR; UNINDEXED DRUG; VICRIVIROC; ZALCITABINE; ZIDOVUDINE;

ANTIVIRAL ACTIVITY; ANTIVIRAL RESISTANCE; BLOOD BRAIN BARRIER; BLOOD TESTIS BARRIER; CLINICAL EFFECTIVENESS; DOSE RESPONSE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CEREBROSPINAL FLUID LEVEL; DRUG DISTRIBUTION; DRUG DOSE REDUCTION; DRUG EFFECT; DRUG EFFICACY; DRUG ELIMINATION; DRUG ERUPTION; DRUG HALF LIFE; DRUG HYPERSENSITIVITY; DRUG INDICATION; DRUG MECHANISM; DRUG METABOLISM; DRUG PENETRATION; DRUG SAFETY; DRUG WITHDRAWAL; EVENING DOSAGE; FEMALE GENITAL SYSTEM; HIGHLY ACTIVE ANTIRETROVIRAL THERAPY; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; IC 50; LIVER TOXICITY; MALE GENITAL SYSTEM; MORNING DOSAGE; NONHUMAN; PHARMACOGENETICS; REVIEW; SINGLE DRUG DOSE; TREATMENT DURATION; VIREMIA; VIRUS CARRIER; VIRUS REPLICATION;

FEMALE; HIV INFECTIONS; HUMANS; MALE; REVERSE TRANSCRIPTASE INHIBITORS;

EID: 84864527204     PISSN: 0399077X     EISSN: 17696690     Source Type: Journal    
DOI: 10.1016/j.medmal.2012.05.004     Document Type: Review

References (67)

1. Wilkin A, Pozniak A, Morales-Ramirez J, et al. Long-term efficacy, safety and tolerability of TMC278 in HIV-1-infected antiretroviral-naïve patients: week 192 results from a phase IIb randomized trial. AIDS Res Hum Retroviruses 2011 [Epub ahead of print].
2. Parienti J.J., Verdon R. Nevirapine and cardiovascular risk. Med Mal Infect 2010, 40:499-505.
3. Sluis-Cremer N., Tachedjian G. Mechanisms of inhibition of HIV replication by non-nucleosidereverse transcriptase inhibitors. Virus Res 2008, 134:147-156.
4. Van Leth F., Kappelhoff B.S., Johnson D., et al. Pharmacokinetic parameters of Nevirapone and Efavirens in relation to antiretroviral efficacy. AIDS Res Hum Retroviruses 2006, 22:232-239.
5. Gathe J, Bogner J, Santiago S, et al. Comparison of 48-week efficacy and safety of 400mg QD nevirapine extended release formulation (Viramune XR) versus 200mg BID nevirapine immediate release formulation (Viramune IR) in combination with Truvada in antiretroviral (ARV) naive HIV-1 infected patients (VERxVE). In: XVIII International AIDS Conference (IAS); July 18-23, 2010; Vienna, Austria: Abstract THLBB202.
6. McArthur J.C., Steiner J., Sacktor N., et al. Human immunodeficiency virus-associated neurocognitive disorders mind the gap. Ann Neurol 2010, 67:699-714.
7. Dahl V., Josefsson L., Palmera S. HIV reservoirs, latency, and reactivation: Prospects for eradication. Antiviral Res 2010, 85:286-294.
8. Furtado M.R., Callaway D.S., Phair J.P., et al. Persistence of HIV-1 transcription in peripheral-blood mononuclear cells in patients receiving potent antiretroviral therapy. N Engl J Med 1999, 340:1614-1622.
9. Chun T.W., Nickle D.C., Justement J.S., Large D., Semerjian A., Curlin M.E., et al. HIV-infected individuals receiving effective antiviral therapy for extended periods of time continually replenish their viral reservoir. J Clin Invest 2005, 115:3250-3255.
10. Siliciano J.D., Kajdas J., Finzi D., Quinn T.C., Chadwick K., Margolick J.B., et al. Long-term follow-up studies confirm the stability of the latent reservoir for HIV-1 in resting CD4+ T cells. Nat Med 2003, 9:727-728.
11. Chun T.W., Nickle D.C., Justement J.S., Meyers J.H., Roby G., Hallahan C.W., et al. Persistence of HIV in gut-associated lymphoid tissue despite long-term antiretroviral therapy. J Infect Dis 2008, 197:714-720.
12. Harrington P.R., Schnell G., Letendre S.L., Ritola K., Robertson K., Hall C., et al. Crosssectional characterization of HIV-1 env compartmentalization in cerebrospinal fluid over the full disease course. AIDS 2009, 23:907-915.
13. Lewis K., Schrager M., D'Souza P. Cellular and anatomical reservoirs of HIV-1 in patients receiving potent antiretroviral combination therapy. JAMA 1998, 280:67-71.
14. Chomont N., El-Far M., Ancuta P., Trautmann L., Procopio F.A., Yassine-Diab B., et al. HIV reservoir size and persistence are driven by T cell survival and homeostatic proliferation. Nat Med 2009, 15:893-900.
15. Aquaro S., Svicher V., Schols D., Pollicita M., Antinori A., Balzarini J., et al. Mechanisms underlying activity of antiretroviral drugs in HIV-1-infected macrophages: new therapeutic strategies. J Leukoc Biol 2006, 80:1103-1110.
16. Rotger M., Colombo S., Furrer H., Bleiber G., Buclin T., Lee B.L., et al. Swiss HIV Cohort Study. 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.
17. Sevigny J.J., Albert S.M., McDermott M.P., Schifitto H., McArthur J.C., Sacktor N., et al. An evaluation of neurocognitive status and markers of immune activation as predictors of time to death in advanced HIV. Infect Arch Neurol 2007, 64:97-102.
18. Jürgen Von Giesen H., Köller H., Theisen A., et al. Therapeutic effects of nonnucleoside reverse tanscriptase inhibitors on the central nervous system in HIV-1-infected patients. JAIDS 2002, 29:363-367.
19. Letendre S., Marquie-Beck J., Capparelli E., Best B., Clifford D., Collier A.C., et al. Validation of the CNS penetration-effectiveness rank for quantifying antiretroviral penetration into the central nervous system. Arch Neurol 2008, 65:65-70.
20. Glynn S.L., Yazdanian M. In vitro blood-brain barrier permeability of nevirapine compared to other HIV antiretroviral agents. J Pharm Sci 1998, 87:306-310.
21. Antinori A., Federico Perno C., Giancola M.L., Forbici F., Ippolito G., Hoetelmans R.M., et al. Efficacy of cerebrospinal fluid (CSF)-penetrating antiretroviral drugs against HIV in the neurological compartment: different patterns of phenotypic resistance in CSF and plasma. Clin Infect Dis 2005, 41:1787-1793.
22. Kearney B., Price R., Sheiner L., Bellibas E., Staprans S., Thevanayagam L., et al. Estimation of nevirapine exposure within the cerebrospinal fluid using CSF: plasma area under the curve ratios. J Acquir Immune Defic Syndr Hum Retrovirol 1999, 20:39-43.
23. Van Praag R.M., Van Weert E.C., Van Heeswijk R.P., Zhou X.J., Sommadossi J.P., Jurriaans S., et al. Stable concentrations of zidovudine, stavudine, lamivudine, abacavir, and nevirapine in serum and cerebrospinal fluid during 2years of therapy. Antimicrob Agents Chemother 2002, 46:896-899.
24. Tashima K.T., Caliendo A.M., Ahmad M., Gormley J.M., Fiske W.D., Brennan J.M., et al. Cerebrospinal fluid human immunodeficiency virus type 1 (HIV-1) suppression and efavirenz drug concentrations in HIV-1-infected patients receiving combination therapy. J Infect Dis 1999, 180:862-864.
25. Letendre S.L., Ellis R.J., Everall I., Ances B., Bharti A., McCutchan J.A. Neurologic complications of HIV disease and their treatment. Top HIV Med 2009, 17:46-56.
26. Marra C.M., Zhao Y., Clifford D.B., Letendre S., Evans S., Henry K., et al. AIDS Clinical Trials Group 736 Study Team. Impact of combination antiretroviral therapy on cerebrospinal fluid HIV RNA and neurocognitive performance. AIDS 2009, 23:1359-1366.
27. Eggers C., Hertogs K., Stürenburg H.J., Van Lunzen J., Stellbrink H.J. Delayed central nervous system virus suppression during highly active antiretroviral therapy is associated with HIV encephalopathy, but not with viral drug resistance or poor central nervous system drug penetration. AIDS 2003, 17:1897-1906.
28. Christo P.P., Greco D.B., Aleixo A.W., Livramento J.A. Factors influencing cerebrospinal fluid and plasma HIV-1 RNA detection rate in patients with and without opportunistic neurological disease during the HAART era. BMC Infect Dis 2007, 7:147.
29. Schnell G., Price R.W., Swanstrom R., Spudich S. Compartmentalization and clonal amplification of HIV-1 variants in the cerebrospinal fluid during primary infection. J Virol 2010, 84:2395-2407.
30. Pasquier C.J., Moinard N., Sauné K., Souyris C., Lavit M., Daudin M., et al. Persistent differences in the antiviral effects of highly active antiretroviral therapy in the blood and male genital tract. AIDS 2008, 22:1894-1896.
31. Marchlewicz M., Wenda-Rozewicka L., Wiszniewska B., Piasecka M., Swider-al-Amawi M. Permeability of blood-testis and blood-epididymis barriers to Hoechst 33342 dye. Folia Histochem Cytobiol 1999, 37:85-86.
32. Lowe S.H., Sankatsing S.U.C., Repping S., Van der Veen F., Reiss P., Lange J.M.A., et al. Is the male genital tract really a sanctuary site for HIV. Arguments that it is not. AIDS 2004, 18:1353-1362.
33. Si-Mohamed A., Kazatchkine M.D., Heard I., Goujon C., Prazuck T., Aymard G., et al. Selection of drug-resistant variants in the female genital tract of human immunodeficiency virus type 1-infected women receiving antiretroviral therapy. J Infect Dis 2000, 182:112-122.
34. Kwara A., Delong A., Rezk N., Hogan J., Burtwell H., Chapman S., et al. Antiretroviral drug concentrations and HIV RNA in the genital tract of HIV-infected women receiving long-term highly active antiretroviral therapy. Clin Infect Dis 2008, 46:719-725.
35. Stratton P., Alexander N.J. Heterosexual spread of HIV infection. The medical management of AIDS in women cotton 1997, 15-43. Wiley-Liss, New York. D.H. Watts (Ed.).
36. Salas-Herrera I.G., Pearson R.M., Johnston A., Turner P. Concentration of metronidazole in cervical mucus and serum after single and repeated oral doses. J Antimicrob Chemother 1991, 28:283-289.
37. Dumond J.B., Yeh R.F., Patterson K.B., et al. Antiretroviral drug exposure in the female genital tract: implications for oral pre- and post-exposure prophylaxis. AIDS 2007, 21:1899-1907.
38. Patterson K., Jennings S., Falcon R., Mrus J., Kashuba A. Darunavir, ritonavir and etravirine pharmacokinetics in the cervicovaginal fluid blood plasma of HIV-infected women. Antimicrob Agents Chemother 2011, 55:1120-1122.
39. Aweeka F.T., Stek A., Best B.M., Hu C., Holland D., et al. Lopinavir protein binding in HIV-1 infected pregnant women. HIV Med 2010, 4:232-238.
40. Kashuba A. In: Conference on Retroviruses and Opportunistic Infections (CROI); February 3-6, 2008; Boston, USA: Abstract 95.
41. Tozzi V. Pharmacogenetics of antiretrovirals. Antiviral Res 2010, 85:190-200.
42. Dieterich D.T., Robinson P.A., Love J., Stern J.O. Drug-induced liver injury associated with the use of nonnucleoside reverse-transcriptase inhibitors. Clin Infect Dis 2004, 38:S80-S89.
43. Taiwo B.O. Nevirapine toxicity. Int J STD AIDS 2006, 17:364-370.
44. Martin J., Hitchcock M.J., De Clercq E., Prusoff W. Early nucleoside reverse transcriptase inhibitors for the treatment of HIV: a brief history of stavudine and its comparison with other dideoxynucleosides. Antiviral Res 2010, 85:34-38.
45. *01 associated with cutaneous hypersensitivity induced by nevirapine and efavirenz. AIDS 2008, 22:539-544.
46. Littera R., Carcassi C., Masala A., Piano P., Serra P., Ortu F., et al. HLA-dependent hypersensitivity to nevirapine in Sardinian HIV patients. AIDS 2006, 20:1621-1626.
47. Gatanaga H., Yazaki H., Tanuma J., Honda M., Genka I., Teruya K., et al. HLA-Cw8 primarily associated with hypersensitivity to nevirapine. AIDS 2007, 21:264-265.
48. Ritchie M.D., Haas D.W., Motsinger A.A., Donahue J.P., ErdemH., RaffantiS., et al. Drug transporter and metabolizing enzyme gene variants and nonnucleoside reverse-transcriptase inhibitor hepatotoxicity. Clin Infect Dis 2006, 43:779-782.
49. Haas D.W., Bartlett J.A., Andersen J.W., Sanne I., Wilkinson G.R., Hinkle J., et al. Adult AIDS Clinical Trials Group. Pharmacogenetics of nevirapine-associated hepatotoxicity: an Adult AIDS Clinical Trials Group Collaboration. Clin Infect Dis 2006, 43:783-786.
50. Saitoh A., Fletcher C.V., Brundage R., et al. Efavirenz pharmacokinetics in HIV-1-infected children are associated with CYP2B6-G516-T polymorphism. J Acquir Immune Defic Syndr 2007, 45:280-285.
51. Ribaudo H.J., Haas D.W., Tierney C., et al. Pharmacogenetics of plasma efavirenz exposure after treatment discontinuation: an Adult AIDS Clinical Trials Group Study. Clin Inf Dis 2006, 42:401-407.
52. Taylor S., Boffito M., Khoo S., Smit E., Back D. Opinion stopping antiretroviral therapy (ART). AIDS 2007, 21:1673-1682.
53. Marzolini C., Paus E., Buclin T., Kim R.B. Polymorphisms in human MDR1 (P-glycoprotein): recent advances and clinical relevance. Clin Pharmacol Ther 2004, 75:13-33.
54. Winzer R., Langmann P., Zylli M., et al. No influence of the Pglycoprotein polymorphisms MDR1 G2677T/A and C3435T on the virological and immunological response in treatment naive HIVpositive patients. Ann Clin Microbiol Antimicrob 2005, 4:3.
55. Motsinger A.A., Ritchie M.D., Shafer R.W., et al. Multilocus genetic interactions and response to efavirenz-containing regimens: an adult AIDS clinical trials group study. Pharmacogenet Genomics 2006, 16:837-845.
56. Garraffo R, Le Guellec C, Meynard JL, Peytavin G, Solas C, Taburet AM, et al. Pharmacologie des antirétroviraux dans. Prise en charge médicale des personnes infectées par le VIH. Recommandations du groupe d'experts sous la documentation de Yeni P. La documentation Française 2010:222-35.
57. Bonora S., Nicastri E., Calcagno A., et al. Ultrasensible assessment of residual HIV viraemia in HAART-treated patients with persistenly undectectable plasma HIV-RNA: a cross-sectional evaluation. J Med Virol 2009, 81:400-405.
58. FDA Intelence Prescribing Information, January 2008:1.
59. Lazzarin A., 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.
60. Madruga J.V., et al. Efficacy and safety of TMC125 (etravirine) in treatment experienced HIV-1-infected patients in DUET-1: 24-week results from a randomised, double-blind, placebo-controlled trial. Lancet 2007, 370:29-38.
61. Gazzard B, et al. The SENSE Trial: Etravirine® (ETR) shows fewer neuropsychiatric adverse events than Efavirenz® (EFV) in treatment-naïve HIV-1 infected patients. In: XVIII International AIDS Conference (IAS); July 18-23, 2010; Vienna, Austria: Abstract LBPE19.
62. Cohen C, et al. Pooled week 48 efficacy and safety results from ECHO and THRIVE, two double-blind, randomised, phase III trials comparing TMC278 versus Efavirenz® in treatment-naïve, HIV-1-infected patients. In: XVIII International AIDS Conference (IAS); July 18-23, 2010; Vienna, Austria: Abstract THLBB206.
63. Sweeney Z.K., Klumpp K. Improving non-nucleoside reverse transcriptase inhibitors for first-line treatment of HIV infection: the development pipeline and recent clinical data. Curr Opin Drug Discov Devel 2008, 11:458-470.
64. Kwara A., DeLong A., Rezk N., Hogan J., Burtwell H., Chapman S., et al. Antiretroviral drug concentrations and HIV RNA in the genital tract of HIV-infected women receiving long-term highly active antiretroviral therapy. CID 2008, 46:719-725.
65. Calcagno A., Bonora S., D'Avolio A., Siccardi M., Simiele M., Chiesa M., et al. Raltegravir penetration in seminal plasma of healthy volunteers. Antimicrob Agents Chemother 2010, 54:2744-2745.
66. Solas C., Lafeuillade A., Halfon P., Chadapaud S., Hittinger G., Lacarelle B. Discrepancies between protease inhibitor concentrations and viral load in reservoirs and sanctuary sites in human immunodeficiency virus-infected patients. Antimicrob Agents Chemother 2003, 47:238-243.
67. Chan DJ, Ray JF. Differential penetration of antiretroviral agents in semen and effect on seminal plasma HIV-1 RNA load. XVII International AIDS Conference. August 3-8, 2008. Mexico City. Abstract TUPE0077.