The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
Chemical Compound Review

Invirase     (2S)-N-[(2S,3R)-3-hydroxy-1- phenyl-4-[(3S)...

Synonyms: Fortovase, SAQUINAVIR, Saquinivir, saguinavir, Fortovase(TM), ...
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of SAQUINAVIR


Psychiatry related information on SAQUINAVIR


High impact information on SAQUINAVIR


Chemical compound and disease context of SAQUINAVIR


Biological context of SAQUINAVIR

  • Pharmacokinetics of once-daily saquinavir/ritonavir in HIV-infected subjects: comparison with the standard twice-daily regimen [15].
  • The human immunodeficiency virus (HIV)-1 protease inhibitor saquinavir inhibits proteasome function and causes apoptosis and radiosensitization in non-HIV-associated human cancer cells [16].
  • There was no significant difference between the groups for median saquinavir Cmin, Cmax, Cltot and AUC (LOPSAQ: 543 ng/ml, 2300 ng/ml, 1020 ml/min and 16 977 ng*h/ml; RITSAQ: 427 ng/ml, 2410 ng/ml, 1105 ml/min and 15 130 ng*h/ml) [17].
  • In these patients, there was no evidence of mutations suggestive of drug resistance, and plasma saquinavir levels were within the expected range [18].
  • HIV phenotype switching during antiretroviral therapy: emergence of saquinavir-resistant strains with less cytopathogenicity [19].

Anatomical context of SAQUINAVIR


Associations of SAQUINAVIR with other chemical compounds


Gene context of SAQUINAVIR

  • METHODS: Twenty healthy subjects received a single oral dose of saquinavir (600 mg) with water (control) and, on a separate occasion, with Seville orange juice (a selective intestinal CYP3A4/5 inhibitor) [29].
  • Among the 6 subjects expressing intestinal CYP3A5, the mean saquinavir CL/F was almost twice as high as for the 14 nonexpressors (36.7 L/h [95% confidence interval (CI), 18.7-54.6 L/h] and 19.3 L/h [95% CI, 11.2-27.4 L/h], respectively; P = .03) [29].
  • Functionally, although these correlates had no impact on HIV-1 production from either X4- or R5-tropic virus, expression correlated significantly with the activity of the HIV-1 protease inhibitor (PI) saquinavir for both P-gp (rho = 0.75; P = 0.0019) and CXCR4 (rho = 0.71; P = 0.0041) [30].
  • Collectively, the cytotoxicity and transport results provide direct evidence that saquinavir is transported by MRP1 and MRP2 [31].
  • Many drugs including saquinavir are substrates of both PGP and CYP3A [32].

Analytical, diagnostic and therapeutic context of SAQUINAVIR


  1. Treatment of human immunodeficiency virus infection with saquinavir, zidovudine, and zalcitabine. AIDS Clinical Trials Group. Collier, A.C., Coombs, R.W., Schoenfeld, D.A., Bassett, R.L., Timpone, J., Baruch, A., Jones, M., Facey, K., Whitacre, C., McAuliffe, V.J., Friedman, H.M., Merigan, T.C., Reichman, R.C., Hooper, C., Corey, L. N. Engl. J. Med. (1996) [Pubmed]
  2. Resolution of refractory AIDS-related mucosal candidiasis after initiation of didanosine plus saquinavir. Zingman, B.S. N. Engl. J. Med. (1996) [Pubmed]
  3. Safety and activity of saquinavir in HIV infection. Kitchen, V.S., Skinner, C., Ariyoshi, K., Lane, E.A., Duncan, I.B., Burckhardt, J., Burger, H.U., Bragman, K., Pinching, A.J., Weber, J.N. Lancet (1995) [Pubmed]
  4. The effect of high-dose saquinavir on viral load and CD4+ T-cell counts in HIV-infected patients. Schapiro, J.M., Winters, M.A., Stewart, F., Efron, B., Norris, J., Kozal, M.J., Merigan, T.C. Ann. Intern. Med. (1996) [Pubmed]
  5. Saquinavir-induced hypoglycemia in type 2 diabetes. Zimhony, O., Stein, D. Ann. Intern. Med. (1999) [Pubmed]
  6. Pharmacokinetic interaction between rifampicin and the once-daily combination of saquinavir and low-dose ritonavir in HIV-infected patients with tuberculosis. Ribera, E., Azuaje, C., Lopez, R.M., Domingo, P., Curran, A., Feijoo, M., Pou, L., Sánchez, P., Sambeat, M.A., Colomer, J., Lopez-Colomes, J.L., Crespo, M., Falcó, V., Ocaña, I., Pahissa, A. J. Antimicrob. Chemother. (2007) [Pubmed]
  7. Evaluation of factors to decrease plasma concentration of an HIV protease inhibitor, saquinavir in ethanol-treated rats. Shibata, N., Kageyama, M., Kimura, K., Tadano, J., Hukushima, H., Namiki, H., Yoshikawa, Y., Takada, K. Biol. Pharm. Bull. (2004) [Pubmed]
  8. Dual vs single protease inhibitor therapy following antiretroviral treatment failure: a randomized trial. Hammer, S.M., Vaida, F., Bennett, K.K., Holohan, M.K., Sheiner, L., Eron, J.J., Wheat, L.J., Mitsuyasu, R.T., Gulick, R.M., Valentine, F.T., Aberg, J.A., Rogers, M.D., Karol, C.N., Saah, A.J., Lewis, R.H., Bessen, L.J., Brosgart, C., DeGruttola, V., Mellors, J.W. JAMA (2002) [Pubmed]
  9. Saquinavir 500 mg film-coated tablets demonstrate bioequivalence to saquinavir 200 mg hard capsules when boosted with twice-daily ritonavir in healthy volunteers. Bittner, B., Riek, M., Holmes, B., Grange, S. Antivir. Ther. (Lond.) (2005) [Pubmed]
  10. A randomized trial comparing initial HAART regimens of nelfinavir/nevirapine and ritonavir/saquinavir in combination with two nucleoside reverse transcriptase inhibitors. Kirk, O., Lundgren, J.D., Pedersen, C., Mathiesen, L.R., Nielsen, H., Katzenstein, T.L., Obel, N., Gerstoft, J. Antivir. Ther. (Lond.) (2003) [Pubmed]
  11. Patients failing saquinavir therapy require an early change to indinavir before HIV-1 viral load reaches high levels. Dronda, F., Pérez-Elías, M.J., Antela, A., Casado, J.L., Martí-Belda, P., Cobo, J. Antivir. Ther. (Lond.) (1999) [Pubmed]
  12. Long-term efficacy and safety of twice-daily saquinavir soft gelatin capsules (SGC), with or without nelfinavir, and three times daily saquinavir-SGC, in triple combination therapy for HIV infection: 100-week follow-up. Greenberg, R.N., Feinberg, J., Goodrich, J., Pilson, R.S., Siemon-Hryczyk, P. Antivir. Ther. (Lond.) (2003) [Pubmed]
  13. Quality of life outcomes of saquinavir, zalcitabine and combination saquinavir plus zalcitabine therapy for adults with advanced HIV infection with CD4 counts between 50 and 300 cells/mm3. Revicki, D.A., Swartz, C., Wu, A.W., Haubrich, R., Collier, A.C. Antivir. Ther. (Lond.) (1999) [Pubmed]
  14. Adherence over 48 weeks in an antiretroviral clinical trial: variable within patients, affected by toxicities and independently predictive of virological response. Nieuwkerk, P., Gisolf, E., Sprangers, M., Danner, S. Antivir. Ther. (Lond.) (2001) [Pubmed]
  15. Pharmacokinetics of once-daily saquinavir/ritonavir in HIV-infected subjects: comparison with the standard twice-daily regimen. Boffito, M., Dickinson, L., Hill, A., Back, D., Moyle, G., Nelson, M., Higgs, C., Fletcher, C., Mandalia, S., Gazzard, B., Pozniak, A. Antivir. Ther. (Lond.) (2004) [Pubmed]
  16. The human immunodeficiency virus (HIV)-1 protease inhibitor saquinavir inhibits proteasome function and causes apoptosis and radiosensitization in non-HIV-associated human cancer cells. Pajonk, F., Himmelsbach, J., Riess, K., Sommer, A., McBride, W.H. Cancer Res. (2002) [Pubmed]
  17. Saquinavir drug exposure is not impaired by the boosted double protease inhibitor combination of lopinavir/ritonavir. Stephan, C., Hentig, N., Kourbeti, I., Dauer, B., Mösch, M., Lutz, T., Klauke, S., Harder, S., Kurowski, M., Staszewski, S. AIDS (2004) [Pubmed]
  18. Failures of 1 week on, 1 week off antiretroviral therapies in a randomized trial. Ananworanich, J., Nuesch, R., Le Braz, M., Chetchotisakd, P., Vibhagool, A., Wicharuk, S., Ruxrungtham, K., Furrer, H., Cooper, D., Hirschel, B., Bernasconi, E., Cavassini, M., Ebnöther, C., Fagard, C., Genné, D., Khanna, N., Perrin, L., Phanupak, P., Ubolyam, S., Vernazza, P., Yerly, S. AIDS (2003) [Pubmed]
  19. HIV phenotype switching during antiretroviral therapy: emergence of saquinavir-resistant strains with less cytopathogenicity. Ercoli, L., Sarmati, L., Nicastri, E., Giannini, G., Galluzzo, C., Vella, S., Andreoni, M. AIDS (1997) [Pubmed]
  20. Effects of the membrane dipole potential on the interaction of saquinavir with phospholipid membranes and plasma membrane receptors of Caco-2 cells. Asawakarn, T., Cladera, J., O'Shea, P. J. Biol. Chem. (2001) [Pubmed]
  21. Cerebrospinal fluid HIV-1 RNA during treatment with ritonavir/saquinavir or ritonavir/saquinavir/stavudine. Gisolf, E.H., Enting, R.H., Jurriaans, S., de Wolf, F., van der Ende, M.E., Hoetelmans, R.M., Portegies, P., Danner, S.A. AIDS (2000) [Pubmed]
  22. Generation of a flexible cell line with regulatable, high-level expression of HIV Gag/Pol particles capable of packaging HIV-derived vectors. Sparacio, S., Pfeiffer, T., Schaal, H., Bosch, V. Mol. Ther. (2001) [Pubmed]
  23. P-glycoprotein limits oral availability, brain, and fetal penetration of saquinavir even with high doses of ritonavir. Huisman, M.T., Smit, J.W., Wiltshire, H.R., Hoetelmans, R.M., Beijnen, J.H., Schinkel, A.H. Mol. Pharmacol. (2001) [Pubmed]
  24. A randomized controlled trial of a protease inhibitor (saquinavir) in combination with zidovudine in previously untreated patients with advanced HIV infection. Vella, S., Lazzarin, A., Carosi, G., Sinicco, A., Armignacco, O., Angarano, G., Andreoni, M., Tambussi, G., Chiodera, A., Floridia, M., Scaccabarozzi, S., Facey, K., Duncan, I., Boudes, P., Bragman, K. Antivir. Ther. (Lond.) (1996) [Pubmed]
  25. Pharmacokinetics of lower doses of saquinavir soft-gel caps (800 and 1200 mg twice daily) boosted with itraconazole in HIV-1-positive patients. Cardiello, P.G., Samor, T., Burger, D., Hoetelmans, R., Mahanontharit, A., Ruxrungtham, K., Lange, J.M., Cooper, D.A., Phanuphak, P. Antivir. Ther. (Lond.) (2003) [Pubmed]
  26. Evidence for two interacting ligand binding sites in human multidrug resistance protein 2 (ATP binding cassette C2). Zelcer, N., Huisman, M.T., Reid, G., Wielinga, P., Breedveld, P., Kuil, A., Knipscheer, P., Schellens, J.H., Schinkel, A.H., Borst, P. J. Biol. Chem. (2003) [Pubmed]
  27. Clinical outcome and predictive factors of failure of highly active antiretroviral therapy in antiretroviral-experienced patients in advanced stages of HIV-1 infection. d'Arminio Monforte, A., Testa, L., Adorni, F., Chiesa, E., Bini, T., Moscatelli, G.C., Abeli, C., Rusconi, S., Sollima, S., Balotta, C., Musicco, M., Galli, M., Moroni, M. AIDS (1998) [Pubmed]
  28. MDR1 G1199A polymorphism alters permeability of HIV protease inhibitors across P-glycoprotein-expressing epithelial cells. Woodahl, E.L., Yang, Z., Bui, T., Shen, D.D., Ho, R.J. AIDS (2005) [Pubmed]
  29. Variation in oral clearance of saquinavir is predicted by CYP3A5*1 genotype but not by enterocyte content of cytochrome P450 3A5. Mouly, S.J., Matheny, C., Paine, M.F., Smith, G., Lamba, J., Lamba, V., Pusek, S.N., Schuetz, E.G., Stewart, P.W., Watkins, P.B. Clin. Pharmacol. Ther. (2005) [Pubmed]
  30. Functional correlation of P-glycoprotein expression and genotype with expression of the human immunodeficiency virus type 1 coreceptor CXCR4. Owen, A., Chandler, B., Bray, P.G., Ward, S.A., Hart, C.A., Back, D.J., Khoo, S.H. J. Virol. (2004) [Pubmed]
  31. Direct evidence that saquinavir is transported by multidrug resistance-associated protein (MRP1) and canalicular multispecific organic anion transporter (MRP2). Williams, G.C., Liu, A., Knipp, G., Sinko, P.J. Antimicrob. Agents Chemother. (2002) [Pubmed]
  32. Dose-dependent increase of saquinavir bioavailability by the pharmaceutic aid cremophor EL. Martin-Facklam, M., Burhenne, J., Ding, R., Fricker, R., Mikus, G., Walter-Sack, I., Haefeli, W.E. British journal of clinical pharmacology. (2002) [Pubmed]
  33. Virologic responses to a ritonavir--saquinavir-containing regimen in patients who had previously failed nelfinavir. Tebas, P., Patick, A.K., Kane, E.M., Klebert, M.K., Simpson, J.H., Erice, A., Powderly, W.G., Henry, K. AIDS (1999) [Pubmed]
  34. Predictors of virological success and ensuing failure in HIV-positive patients starting highly active antiretroviral therapy in Europe: results from the EuroSIDA study. Paredes, R., Mocroft, A., Kirk, O., Lazzarin, A., Barton, S.E., van Lunzen, J., Katzenstein, T.L., Antunes, F., Lundgren, J.D., Clotet, B. Arch. Intern. Med. (2000) [Pubmed]
  35. Once-daily dosing of saquinavir and low-dose ritonavir in HIV-1-infected individuals: a pharmacokinetic pilot study. van Heeswijk, R.P., Veldkamp, A.I., Mulder, J.W., Meenhorst, P.L., Lange, J.M., Beijnen, J.H., Hoetelmans, R.M. AIDS (2000) [Pubmed]
  36. Efficacy of salvage therapy containing ritonavir and saquinavir after failure of single protease inhibitor-containing regimens. Hall, C.S., Raines, C.P., Barnett, S.H., Moore, R.D., Gallant, J.E. AIDS (1999) [Pubmed]
WikiGenes - Universities