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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

References

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  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]
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  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]
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  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]
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  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]
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  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]
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  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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