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Chemical Compound Review

Aptivus     N-[3-[(1R)-1-[(6R)-2-hydroxy- 4-oxo-6...

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Disease relevance of Aptivus


High impact information on Aptivus


Chemical compound and disease context of Aptivus


Biological context of Aptivus


Anatomical context of Aptivus


Associations of Aptivus with other chemical compounds


Gene context of Aptivus

  • At the end of the selection experiments, viruses harbouring 10 mutations in the protease (L10F, I13V, V32I, L33F, M36I, K45I, I54V, A71V, V82L, I84V) as well as a mutation in the CA/SP1 gag cleavage site were selected and showed 87-fold decreased susceptibility to tipranavir [18].
  • In vitro, tipranavir-resistant viruses had a reduced replicative capacity which could not be improved by the introduction of the CA/SP1 cleavage site mutation [18].

Analytical, diagnostic and therapeutic context of Aptivus


  1. Tipranavir inhibits broadly protease inhibitor-resistant HIV-1 clinical samples. Larder, B.A., Hertogs, K., Bloor, S., van den Eynde, C.H., DeCian, W., Wang, Y., Freimuth, W.W., Tarpley, G. AIDS (2000) [Pubmed]
  2. Genotypic changes in human immunodeficiency virus type 1 protease associated with reduced susceptibility and virologic response to the protease inhibitor tipranavir. Baxter, J.D., Schapiro, J.M., Boucher, C.A., Kohlbrenner, V.M., Hall, D.B., Scherer, J.R., Mayers, D.L. J. Virol. (2006) [Pubmed]
  3. Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors. Ntemgwa, M., Brenner, B.G., Oliveira, M., Moisi, D., Wainberg, M.A. Antimicrob. Agents Chemother. (2007) [Pubmed]
  4. Practical perspectives on the use of tipranavir in combination with other medications: lessons learned from pharmacokinetic studies. Boffito, M., Maitland, D., Pozniak, A. Journal of clinical pharmacology. (2006) [Pubmed]
  5. Food and Drug Administration analysis of tipranavir clinical resistance in HIV-1-infected treatment-experienced patients. Naeger, L.K., Struble, K.A. AIDS (2007) [Pubmed]
  6. How flexible is tipranavir in complex with the HIV-1 protease active site? Schake, D. AIDS (2004) [Pubmed]
  7. Susceptibility to PNU-140690 (Tipranavir) of human immunodeficiency virus type 1 isolates derived from patients with multidrug resistance to other protease inhibitors. Rusconi, S., La Seta Catamancio, S., Citterio, P., Kurtagic, S., Violin, M., Balotta, C., Moroni, M., Galli, M., d'Arminio-Monforte, A. Antimicrob. Agents Chemother. (2000) [Pubmed]
  8. Antiviral activity of the dihydropyrone PNU-140690, a new nonpeptidic human immunodeficiency virus protease inhibitor. Poppe, S.M., Slade, D.E., Chong, K.T., Hinshaw, R.R., Pagano, P.J., Markowitz, M., Ho, D.D., Mo, H., Gorman, R.R., Dueweke, T.J., Thaisrivongs, S., Tarpley, W.G. Antimicrob. Agents Chemother. (1997) [Pubmed]
  9. Susceptibility to protease inhibitors in HIV-2 primary isolates from patients failing antiretroviral therapy. Rodés, B., Sheldon, J., Toro, C., Jiménez, V., Alvarez, M.A., Soriano, V. J. Antimicrob. Chemother. (2006) [Pubmed]
  10. The Non-Peptidic HIV Protease Inhibitor Tipranavir and Two Synthetic Peptidomimetics (TS98 and TS102) Modulate Pneumocystis carinii Growth and Proteasome Activity of HEL299 Cell Line. Mazza, F., Tronconi, E., Valerio, A., Groettrup, M., Kremer, M., Tossi, A., Benedetti, F., Cargnel, A., Atzori, C. J. Eukaryot. Microbiol. (2006) [Pubmed]
  11. A 14-day dose-response study of the efficacy, safety, and pharmacokinetics of the nonpeptidic protease inhibitor tipranavir in treatment-naive HIV-1-infected patients. McCallister, S., Valdez, H., Curry, K., MacGregor, T., Borin, M., Freimuth, W., Wang, Y., Mayers, D.L. J. Acquir. Immune Defic. Syndr. (2004) [Pubmed]
  12. Tipranavir without ritonavir does not acutely induce peripheral insulin resistance in a rodent model. Hruz, P.W., Yan, Q. J. Acquir. Immune Defic. Syndr. (2006) [Pubmed]
  13. Resistance to HIV protease inhibitors: mechanisms and clinical consequences. de Mendoza, C., Soriano, V. Curr. Drug Metab. (2004) [Pubmed]
  14. Tipranavir: a novel second-generation nonpeptidic protease inhibitor. Kandula, V.R., Khanlou, H., Farthing, C. Expert review of anti-infective therapy. (2005) [Pubmed]
  15. Structure-based discovery of Tipranavir disodium (PNU-140690E): a potent, orally bioavailable, nonpeptidic HIV protease inhibitor. Thaisrivongs, S., Strohbach, J.W. Biopolymers (1999) [Pubmed]
  16. Unexpected drug-drug interaction between tipranavir/ritonavir and enfuvirtide. González de Requena, D., Calcagno, A., Bonora, S., Ladetto, L., D'Avolio, A., Sciandra, M., Siccardi, M., Bargiacchi, O., Sinicco, A., Di Perri, G. AIDS (2006) [Pubmed]
  17. Combined tipranavir and enfuvirtide use associated with higher plasma tipranavir concentrations but not with increased hepatotoxicity: sub-analysis from RESIST. Raffi, F., Battegay, M., Rusconi, S., Opravil, M., Blick, G., Steigbigel, R.T., Kraft, M., Neubacher, D., Sabo, J.P. AIDS (2007) [Pubmed]
  18. Selection and characterization of HIV-1 showing reduced susceptibility to the non-peptidic protease inhibitor tipranavir. Doyon, L., Tremblay, S., Bourgon, L., Wardrop, E., Cordingley, M.G. Antiviral Res. (2005) [Pubmed]
  19. Determination of tipranavir in human plasma by reverse phase liquid chromatography with UV detection using photodiode array. Keil, K., Difrancesco, R., Morse, G.D. Therapeutic drug monitoring. (2006) [Pubmed]
  20. Tipranavir: a protease inhibitor for HIV salvage therapy. Dong, B.J., Cocohoba, J.M. The Annals of pharmacotherapy. (2006) [Pubmed]
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