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Chemical Compound Review

nelfinavir     (3S,4aS,8aR)-2-[(2R,3S)-2- hydroxy-3-[(3...

Synonyms: CHEMBL584, Viracept (TN), SureCN38218, VRX496, AG-1341, ...
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Disease relevance of nelfinavir


Psychiatry related information on nelfinavir


High impact information on nelfinavir


Chemical compound and disease context of nelfinavir

  • The HIV protease inhibitors nelfinavir and saquinavir, but not a variety of HIV reverse transcriptase inhibitors, adversely affect human proteasome function [13].
  • STUDY DESIGN AND METHODS: The database of the Swiss HIV Cohort Study was screened for all subjects naive to protease inhibitor (PI) treatment who started HAART with nelfinavir or indinavir, responded initially (HIV-RNA <400 copies/ml) and received >24 weeks of treatment [14].
  • In addition, in vivo, doses of amprenavir or nelfinavir comparable with the therapeutic levels achieved in HIV patients were sufficient to down-regulate phosphorylation of Akt in SQ20B and T24 xenografts [15].
  • METHODS: Adverse events, plasma HIV-1 RNA, CD4 cell counts, CD4 cell percentage (CD4%) and clinical progression were recorded at baseline and prospectively to 72 weeks in order to assess the toxicity, tolerability and efficacy of a combination of stavudine, didanosine and nelfinavir [16].
  • Adverse events during pregnancy were anaemia (n = 15), elevation of transaminases (n = 4), nausea/vomiting (n = 4), glucose intolerance (n = 2), nephrolithiasis (n = 2), diarrhoea (n = 2), hypertension (n = 1), insulin-requiring diabetes (n = 1) [17].

Biological context of nelfinavir


Anatomical context of nelfinavir


Associations of nelfinavir with other chemical compounds


Gene context of nelfinavir


Analytical, diagnostic and therapeutic context of nelfinavir


  1. Combination therapy with efavirenz, nelfinavir, and nucleoside reverse-transcriptase inhibitors in children infected with human immunodeficiency virus type 1. Pediatric AIDS Clinical Trials Group 382 Team. Starr, S.E., Fletcher, C.V., Spector, S.A., Yong, F.H., Fenton, T., Brundage, R.C., Manion, D., Ruiz, N., Gersten, M., Becker, M., McNamara, J., Mofenson, L.M., Purdue, L., Siminski, S., Graham, B., Kornhauser, D.M., Fiske, W., Vincent, C., Lischner, H.W., Dankner, W.M., Flynn, P.M. N. Engl. J. Med. (1999) [Pubmed]
  2. Pharmacokinetics of nelfinavir in children: influencing factors and dose implications. Bergshoeff, A.S., Fraaij, P.L., van Rossum, A.M., Wolfs, T.F., Geelen, S.P., de Groot, R., Burger, D.M. Antivir. Ther. (Lond.) (2003) [Pubmed]
  3. Nelfinavir Down-regulates Hypoxia-Inducible Factor 1{alpha} and VEGF Expression and Increases Tumor Oxygenation: Implications for Radiotherapy. Pore, N., Gupta, A.K., Cerniglia, G.J., Jiang, Z., Bernhard, E.J., Evans, S.M., Koch, C.J., Hahn, S.M., Maity, A. Cancer Res. (2006) [Pubmed]
  4. Dynamic correlation of apoptosis and immune activation during treatment of HIV infection. Badley, A.D., Parato, K., Cameron, D.W., Kravcik, S., Phenix, B.N., Ashby, D., Kumar, A., Lynch, D.H., Tschopp, J., Angel, J.B. Cell Death Differ. (1999) [Pubmed]
  5. Phosphatase and tensin homologue deficiency in glioblastoma confers resistance to radiation and temozolomide that is reversed by the protease inhibitor nelfinavir. Jiang, Z., Pore, N., Cerniglia, G.J., Mick, R., Georgescu, M.M., Bernhard, E.J., Hahn, S.M., Gupta, A.K., Maity, A. Cancer Res. (2007) [Pubmed]
  6. The impact of pharmacologic and genetic knockout of P-glycoprotein on nelfinavir levels in the brain and other tissues in mice. Salama, N.N., Kelly, E.J., Bui, T., Ho, R.J. Journal of pharmaceutical sciences. (2005) [Pubmed]
  7. Failure to detect nelfinavir in the cerebrospinal fluid of HIV-1--infected patients with and without AIDS dementia complex. Aweeka, F., Jayewardene, A., Staprans, S., Bellibas, S.E., Kearney, B., Lizak, P., Novakovic-Agopian, T., Price, R.W. J. Acquir. Immune Defic. Syndr. Hum. Retrovirol. (1999) [Pubmed]
  8. Nelfinavir, efavirenz, or both after the failure of nucleoside treatment of HIV infection. Albrecht, M.A., Bosch, R.J., Hammer, S.M., Liou, S.H., Kessler, H., Para, M.F., Eron, J., Valdez, H., Dehlinger, M., Katzenstein, D.A. N. Engl. J. Med. (2001) [Pubmed]
  9. Inhibition of adenine nucleotide translocator pore function and protection against apoptosis in vivo by an HIV protease inhibitor. Weaver, J.G., Tarze, A., Moffat, T.C., Lebras, M., Deniaud, A., Brenner, C., Bren, G.D., Morin, M.Y., Phenix, B.N., Dong, L., Jiang, S.X., Sim, V.L., Zurakowski, B., Lallier, J., Hardin, H., Wettstein, P., van Heeswijk, R.P., Douen, A., Kroemer, R.T., Hou, S.T., Bennett, S.A., Lynch, D.H., Kroemer, G., Badley, A.D. J. Clin. Invest. (2005) [Pubmed]
  10. The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors. Kim, R.B., Fromm, M.F., Wandel, C., Leake, B., Wood, A.J., Roden, D.M., Wilkinson, G.R. J. Clin. Invest. (1998) [Pubmed]
  11. Response to antiretroviral treatment in HIV-1-infected individuals with allelic variants of the multidrug resistance transporter 1: a pharmacogenetics study. Fellay, J., Marzolini, C., Meaden, E.R., Back, D.J., Buclin, T., Chave, J.P., Decosterd, L.A., Furrer, H., Opravil, M., Pantaleo, G., Retelska, D., Ruiz, L., Schinkel, A.H., Vernazza, P., Eap, C.B., Telenti, A. Lancet (2002) [Pubmed]
  12. Altered adipokine response in murine 3T3-F442A adipocytes treated with protease inhibitors and nucleoside reverse transcriptase inhibitors. Jones, S.P., Janneh, O., Back, D.J., Pirmohamed, M. Antivir. Ther. (Lond.) (2005) [Pubmed]
  13. The HIV protease inhibitors nelfinavir and saquinavir, but not a variety of HIV reverse transcriptase inhibitors, adversely affect human proteasome function. Piccinini, M., Rinaudo, M.T., Anselmino, A., Buccinnà, B., Ramondetti, C., Dematteis, A., Ricotti, E., Palmisano, L., Mostert, M., Tovo, P.A. Antivir. Ther. (Lond.) (2005) [Pubmed]
  14. Drug resistance mutations in HIV-1-infected subjects during protease inhibitor-containing highly active antiretroviral therapy with nelfinavir or indinavir. Yerly, S., Rickenbach, M., Popescu, M., Taffe, P., Craig, C., Perrin, L. Antivir. Ther. (Lond.) (2001) [Pubmed]
  15. HIV protease inhibitors block Akt signaling and radiosensitize tumor cells both in vitro and in vivo. Gupta, A.K., Cerniglia, G.J., Mick, R., McKenna, W.G., Muschel, R.J. Cancer Res. (2005) [Pubmed]
  16. Highly active antiretroviral therapy started in infants under 3 months of age: 72-week follow-up for CD4 cell count, viral load and drug resistance outcome. Aboulker, J.P., Babiker, A., Chaix, M.L., Compagnucci, A., Darbyshire, J., Debré, M., Faye, A., Giaquinto, C., Gibb, D.M., Harper, L., Saïdi, Y., Walker, A.S. AIDS (2004) [Pubmed]
  17. Antiretroviral therapies in pregnancy: maternal, fetal and neonatal effects. Swiss HIV Cohort Study, the Swiss Collaborative HIV and Pregnancy Study, and the Swiss Neonatal HIV Study. Lorenzi, P., Spicher, V.M., Laubereau, B., Hirschel, B., Kind, C., Rudin, C., Irion, O., Kaiser, L. AIDS (1998) [Pubmed]
  18. Influence of single-nucleotide polymorphisms in the multidrug resistance-1 gene on the cellular export of nelfinavir and its clinical implication for highly active antiretroviral therapy. Zhu, D., Taguchi-Nakamura, H., Goto, M., Odawara, T., Nakamura, T., Yamada, H., Kotaki, H., Sugiura, W., Iwamoto, A., Kitamura, Y. Antivir. Ther. (Lond.) (2004) [Pubmed]
  19. Metabolic and immunological effects of antiretroviral agents in healthy individuals receiving post-exposure prophylaxis. Garcia, F., Plana, M., Mestre, G., Cruceta, A., Martinez, E., Miró, J.M., Mallolas, J., Tuset, M., Pumorola, T., Gallart, T., Gatell, J.M. Antivir. Ther. (Lond.) (2002) [Pubmed]
  20. Antiapoptotic mechanism of HIV protease inhibitors: preventing mitochondrial transmembrane potential loss. Phenix, B.N., Lum, J.J., Nie, Z., Sanchez-Dardon, J., Badley, A.D. Blood (2001) [Pubmed]
  21. Select HIV protease inhibitors alter bone and fat metabolism ex vivo. Jain, R.G., Lenhard, J.M. J. Biol. Chem. (2002) [Pubmed]
  22. Suppression of preadipocyte differentiation and promotion of adipocyte death by HIV protease inhibitors. Dowell, P., Flexner, C., Kwiterovich, P.O., Lane, M.D. J. Biol. Chem. (2000) [Pubmed]
  23. Some HIV protease inhibitors alter lamin A/C maturation and stability, SREBP-1 nuclear localization and adipocyte differentiation. Caron, M., Auclair, M., Sterlingot, H., Kornprobst, M., Capeau, J. AIDS (2003) [Pubmed]
  24. HIV-1 protease inhibitors. A review for clinicians. Deeks, S.G., Smith, M., Holodniy, M., Kahn, J.O. JAMA (1997) [Pubmed]
  25. Predictors of the virological response to a change in the antiretroviral treatment regimen in HIV-1-infected patients enrolled in a randomized trial comparing genotyping, phenotyping and standard of care (Narval trial, ANRS 088). Vray, M., Meynard, J.L., Dalban, C., Morand-Joubert, L., Clavel, F., Brun-Vézinet, F., Peytavin, G., Costagliola, D., Girard, P.M. Antivir. Ther. (Lond.) (2003) [Pubmed]
  26. Antiretroviral activity and safety of abacavir in combination with selected HIV-1 protease inhibitors in therapy-naive HIV-1-infected adults. McMahon, D., Lederman, M., Haas, D.W., Haubrich, R., Stanford, J., Cooney, E., Horton, J., Kelleher, D., Ross, L., Cutrell, A., Lee, D., Spreen, W., Mellors, J.W. Antivir. Ther. (Lond.) (2001) [Pubmed]
  27. The steady-state pharmacokinetics of nelfinavir in combination with tenofovir in HIV-infected patients. Kruse, G., Esser, S., Stocker, H., Breske, A., Koerber, A., Kopperman, M., Wiehler, H., Ross, B., Möcklinghoff, C., Hill, A., Becker, M., Kurowski, M. Antivir. Ther. (Lond.) (2005) [Pubmed]
  28. Intracellular accumulation of nelfinavir and its relationship to P-glycoprotein expression and function in HIV-infected patients. Hennessy, M., Clarke, S., Spiers, J.P., Kelleher, D., Mulcahy, F., Hoggard, P., Back, D., Barry, M. Antivir. Ther. (Lond.) (2004) [Pubmed]
  29. Nelfinavir-induced insulin resistance is associated with impaired plasma membrane recruitment of the PI 3-kinase effectors Akt/PKB and PKC-zeta. Ben-Romano, R., Rudich, A., Tirosh, A., Potashnik, R., Sasaoka, T., Riesenberg, K., Schlaeffer, F., Bashan, N. Diabetologia (2004) [Pubmed]
  30. Pharmacogenetics of long-term responses to antiretroviral regimens containing Efavirenz and/or Nelfinavir: an Adult Aids Clinical Trials Group Study. Haas, D.W., Smeaton, L.M., Shafer, R.W., Robbins, G.K., Morse, G.D., Labbe, L., Wilkinson, G.R., Clifford, D.B., D'Aquila, R.T., De Gruttola, V., Pollard, R.B., Merigan, T.C., Hirsch, M.S., George, A.L., Donahue, J.P., Kim, R.B. J. Infect. Dis. (2005) [Pubmed]
  31. HIV protease inhibitors are inhibitors but not substrates of the human breast cancer resistance protein (BCRP/ABCG2). Gupta, A., Zhang, Y., Unadkat, J.D., Mao, Q. J. Pharmacol. Exp. Ther. (2004) [Pubmed]
  32. Characterization of the selectivity and mechanism of human cytochrome P450 inhibition by the human immunodeficiency virus-protease inhibitor nelfinavir mesylate. Lillibridge, J.H., Liang, B.H., Kerr, B.M., Webber, S., Quart, B., Shetty, B.V., Lee, C.A. Drug Metab. Dispos. (1998) [Pubmed]
  33. HIV protease inhibitors decrease VEGF/HIF-1alpha expression and angiogenesis in glioblastoma cells. Pore, N., Gupta, A.K., Cerniglia, G.J., Maity, A. Neoplasia (2006) [Pubmed]
  34. Phenotypic HIV-1 resistance correlates with treatment outcome of nelfinavir salvage therapy. Walter, H., Schmidt, B., Rascu, A., Helm, M., Moschik, B., Paatz, C., Kurowski, M., Korn, K., Uberla, K., Harrer, T. Antivir. Ther. (Lond.) (2000) [Pubmed]
  35. Predictors of virological response in HIV-infected patients to salvage antiretroviral therapy that includes nelfinavir. Walmsley, S.L., Becker, M.I., Zhang, M., Humar, A., Harrigan, P.R. Antivir. Ther. (Lond.) (2001) [Pubmed]
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