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Chemical Compound Review

SureCN12175481     1,3-thiazol-5-ylmethyl N-[(2S,5R)-3...

Synonyms: TMC 114r, AC1L1U86, UNII-O3J8G9O825
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Disease relevance of ritonavir


Psychiatry related information on ritonavir

  • OBJECTIVE: To determine the incidence of significant liver enzyme elevations following the initiation of protease inhibitor (PI)-based antiretroviral therapy (ART) with or without pharmacokinetic boosting with ritonavir (RTV), and to define the role of chronic viral hepatitis in its development [4].
  • After 3 months, statistically significant differences (P < 0.03) favoring the ritonavir-treated patients were seen on the physical health summary, mental health summary, and general health perceptions, social function, mental health, and energy/fatigue subscales [5].
  • Ritonavir increases levels of erectile dysfunction agent 49 fold [6].
  • Multiple factors influence the risk of liver toxicity under antiretroviral therapy, including the specific drug in use (e.g. use of full doses of ritonavir), and environmental factors (e.g. alcohol abuse) [7].
  • CASE PRESENTATION: We report a case of HIV dementia (MSK stage 3) in a 57 year old antiretroviral na??ve man who was introduced on zidovudine, lamivudine and ritonavir boosted indinavir, and followed with consecutive lumbar punctures before and after two and 15 months after initiation of HAART [8].

High impact information on ritonavir


Chemical compound and disease context of ritonavir


Biological context of ritonavir

  • Our previous studies indicated that ritonavir directly affects immune cell activation, proliferation, and susceptibility to apoptosis [16].
  • The model also reveals that ritonavir monotherapy is approximately 65% as efficacious as a recently used potent four-drug therapy, suggesting that selection for drug resistance may be facilitated by the relatively low efficacy of individual drugs, contributing in part to the inherent limitations of current therapies in combating HIV-1 infection [17].
  • Analysis of the virological response with respect to baseline viral phenotype and genotype in protease inhibitor-experienced HIV-1-infected patients receiving lopinavir/ritonavir therapy [18].
  • We examined the effect of ritonavir, an HIV protease inhibitor, on HTLV-I-infected T-cell lines and primary ATL cells and found that it induced apoptosis and inhibited transcriptional activation of NF-kappaB in these cells [19].
  • OBJECTIVE: To establish the bioequivalence of a 500 mg film-coated tablet of saquinavir mesylate (FCT SQV) to the 200 mg hard-capsule saquinavir mesylate (HC SQV), both boosted with ritonavir and administered under fed conditions [20].

Anatomical context of ritonavir


Associations of ritonavir with other chemical compounds


Gene context of ritonavir


Analytical, diagnostic and therapeutic context of ritonavir


  1. A preliminary study of ritonavir, an inhibitor of HIV-1 protease, to treat HIV-1 infection. Markowitz, M., Saag, M., Powderly, W.G., Hurley, A.M., Hsu, A., Valdes, J.M., Henry, D., Sattler, F., La Marca, A., Leonard, J.M. N. Engl. J. Med. (1995) [Pubmed]
  2. Resolution of chronic hepatitis B after ritonavir treatment in an HIV-infected patient. Velasco, M., Morán, A., Téllez, M.J. N. Engl. J. Med. (1999) [Pubmed]
  3. Ritonavir and renal failure. Chugh, S., Bird, R., Alexander, E.A. N. Engl. J. Med. (1997) [Pubmed]
  4. Hepatotoxicity associated with protease inhibitor-based antiretroviral regimens with or without concurrent ritonavir. Sulkowski, M.S., Mehta, S.H., Chaisson, R.E., Thomas, D.L., Moore, R.D. AIDS (2004) [Pubmed]
  5. A randomized trial of the effect of ritonavir in maintaining quality of life in advanced HIV disease. Advanced HIV Disease Ritonavir Study Group. Cohen, C., Revicki, D.A., Nabulsi, A., Sarocco, P.W., Jiang, P. AIDS (1998) [Pubmed]
  6. Ritonavir increases levels of erectile dysfunction agent 49 fold. Edmunds-Ogbuokiri, T. HIV clinician / Delta Region AIDS Education & Training Center. (2004) [Pubmed]
  7. Antiretroviral therapy in chronic liver disease: focus on HIV/HCV coinfection--statements of the First Italian Consensus Workshop. Carosi, G., Puoti, M., Antonucci, G., De Luca, A., Maserati, R., Torti, C., Bonfanti, P., Bonora, S., Bruno, R., Gaeta, G.B., Antinori, A., Monforte, A., Orani, A., Sagnelli, E., Cargnel, A., Cauda, R., Mazzotta, F., Pastore, G., Suter, F., Vullo, V. AIDS reviews. (2005) [Pubmed]
  8. Normalisation of cerebrospinal fluid biomarkers parallels improvement of neurological symptoms following HAART in HIV dementia - case report. Andersson, L.M., Hagberg, L., Rosengren, L., Fuchs, D., Blennow, K., Gissl??n, M. BMC Infect. Dis. (2006) [Pubmed]
  9. A short-term study of the safety, pharmacokinetics, and efficacy of ritonavir, an inhibitor of HIV-1 protease. European-Australian Collaborative Ritonavir Study Group. Danner, S.A., Carr, A., Leonard, J.M., Lehman, L.M., Gudiol, F., Gonzales, J., Raventos, A., Rubio, R., Bouza, E., Pintado, V. N. Engl. J. Med. (1995) [Pubmed]
  10. Rapid turnover of plasma virions and CD4 lymphocytes in HIV-1 infection. Ho, D.D., Neumann, A.U., Perelson, A.S., Chen, W., Leonard, J.M., Markowitz, M. Nature (1995) [Pubmed]
  11. The HIV protease inhibitor ritonavir blocks osteoclastogenesis and function by impairing RANKL-induced signaling. Wang, M.W., Wei, S., Faccio, R., Takeshita, S., Tebas, P., Powderly, W.G., Teitelbaum, S.L., Ross, F.P. J. Clin. Invest. (2004) [Pubmed]
  12. The influence of protease inhibitor resistance profiles on selection of HIV therapy in treatment-naive patients. Turner, D., Schapiro, J.M., Brenner, B.G., Wainberg, M.A. Antivir. Ther. (Lond.) (2004) [Pubmed]
  13. Pharmacokinetics of a once-daily regimen of lopinavir/ritonavir in HIV-1-infected children. van der Lee, M., Verweel, G., de Groot, R., Burger, D. Antivir. Ther. (Lond.) (2006) [Pubmed]
  14. The HIV protease inhibitors saquinavir, ritonavir, and nelfinavir induce apoptosis and decrease barrier function in human intestinal epithelial cells. Bode, H., Lenzner, L., Kraemer, O.H., Kroesen, A.J., Bendfeldt, K., Schulzke, J.D., Fromm, M., Stoltenburg-Didinger, G., Zeitz, M., Ullrich, R. Antivir. Ther. (Lond.) (2005) [Pubmed]
  15. Reductions in viral load and increases in T lymphocyte numbers in treatment-naive patients with advanced HIV-1 infection treated with ritonavir, zidovudine and zalcitabine triple therapy. Mathez, D., Bagnarelli, P., Gorin, I., Katlama, C., Pialoux, G., Saimot, G., Tubiana, P., De Truchis, P., Chauvin, J.P., Mills, R., Rode, R., Clementi, M., Leibowitch, J. Antivir. Ther. (Lond.) (1997) [Pubmed]
  16. Antitumorigenic effects of HIV protease inhibitor ritonavir: inhibition of Kaposi sarcoma. Pati, S., Pelser, C.B., Dufraine, J., Bryant, J.L., Reitz, M.S., Weichold, F.F. Blood (2002) [Pubmed]
  17. Estimates of intracellular delay and average drug efficacy from viral load data of HIV-infected individuals under antiretroviral therapy. Dixit, N.M., Markowitz, M., Ho, D.D., Perelson, A.S. Antivir. Ther. (Lond.) (2004) [Pubmed]
  18. Analysis of the virological response with respect to baseline viral phenotype and genotype in protease inhibitor-experienced HIV-1-infected patients receiving lopinavir/ritonavir therapy. Kempf, D.J., Isaacson, J.D., King, M.S., Brun, S.C., Sylte, J., Richards, B., Bernstein, B., Rode, R., Sun, E. Antivir. Ther. (Lond.) (2002) [Pubmed]
  19. Efficient intervention of growth and infiltration of primary adult T-cell leukemia cells by an HIV protease inhibitor, ritonavir. Dewan, M.Z., Uchihara, J.N., Terashima, K., Honda, M., Sata, T., Ito, M., Fujii, N., Uozumi, K., Tsukasaki, K., Tomonaga, M., Kubuki, Y., Okayama, A., Toi, M., Mori, N., Yamamoto, N. Blood (2006) [Pubmed]
  20. 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]
  21. 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]
  22. Changes in body fat composition after 1 year of salvage therapy with lopinavir/ritonavir-containing regimens and its relationship with lopinavir plasma concentrations. Gutiérrez, F., Padilla, S., Masiá, M., Navarro, A., Gallego, J., Hernández, I., Ramos, J.M., Martin-Hidalgo, A. Antivir. Ther. (Lond.) (2004) [Pubmed]
  23. A prospective study of efficacy and safety of once-daily saquinavir/ritonavir plus two nucleoside reverse transcriptase inhibitors in treatment-naive Thai patients. Ananworanich, J., Hill, A., Siangphoe, U., Ruxrungtham, K., Prasithsirikul, W., Chetchotisakd, P., Kiertiburanakul, S., Munsakul, W., Raksakulkarn, P., Tansuphasawadikul, S., Nuesch, R., Cooper, D.A., Hirschel, B. Antivir. Ther. (Lond.) (2005) [Pubmed]
  24. Pharmacokinetics of reduced-dose indinavir/ritonavir 400/100 mg twice daily in HIV-1-infected Thai patients. Boyd, M., Mootsikapun, P., Burger, D., Chuenyam, T., Ubolyam, S., Mahanontharit, A., Sangkote, J., Bunyaprawit, P., Horsakulchai, M., Lange, J., Cooper, D., Phanuphak, P., Ruxrungtham, K. Antivir. Ther. (Lond.) (2005) [Pubmed]
  25. Salvage therapy with atazanavir/ritonavir combined to tenofovir in HIV-infected patients with multiple treatment failures: randomized ANRS 107 trial. Piketty, C., Gérard, L., Chazallon, C., Marcelin, A.G., Clavel, F., Taburet, A.M., Calvez, V., Madelaine-Chambrin, I., Molina, J.M., Aboulker, J.P., Girard, P.M. Antivir. Ther. (Lond.) (2006) [Pubmed]
  26. Salvage therapy with amprenavir, lopinavir and ritonavir 200 mg/d or 400 mg/d in HIV-infected patients in virological failure. Raguin, G., Chêne, G., Morand-Joubert, L., Taburet, A.M., Droz, C., Le Tiec, C., Clavel, F., Girard, P.M. Antivir. Ther. (Lond.) (2004) [Pubmed]
  27. Combination of protease inhibitors for the treatment of HIV-1-infected patients: a review of pharmacokinetics and clinical experience. van Heeswijk, R.P., Veldkamp, A., Mulder, J.W., Meenhorst, P.L., Lange, J.M., Beijnen, J.H., Hoetelmans, R.M. Antivir. Ther. (Lond.) (2001) [Pubmed]
  28. Estrogen receptor-alpha mediates gender differences in atherosclerosis induced by HIV protease inhibitors. Allred, K.F., Smart, E.J., Wilson, M.E. J. Biol. Chem. (2006) [Pubmed]
  29. Effects of HIV protease inhibitor ritonavir on Akt-regulated cell proliferation in breast cancer. Srirangam, A., Mitra, R., Wang, M., Gorski, J.C., Badve, S., Baldridge, L., Hamilton, J., Kishimoto, H., Hawes, J., Li, L., Orschell, C.M., Srour, E.F., Blum, J.S., Donner, D., Sledge, G.W., Nakshatri, H., Potter, D.A. Clin. Cancer Res. (2006) [Pubmed]
  30. Potent cytochrome P450 2C19 genotype-related interaction between voriconazole and the cytochrome P450 3A4 inhibitor ritonavir. Mikus, G., Schöwel, V., Drzewinska, M., Rengelshausen, J., Ding, R., Riedel, K.D., Burhenne, J., Weiss, J., Thomsen, T., Haefeli, W.E. Clin. Pharmacol. Ther. (2006) [Pubmed]
  31. Renal failure after treatment with ritonavir. Duong, M., Sgro, C., Grappin, M., Biron, F., Boibieux, A. Lancet (1996) [Pubmed]
  32. Elucidation of crystal form diversity of the HIV protease inhibitor ritonavir by high-throughput crystallization. Morissette, S.L., Soukasene, S., Levinson, D., Cima, M.J., Almarsson, O. Proc. Natl. Acad. Sci. U.S.A. (2003) [Pubmed]
  33. An inhibitor of HIV-1 protease modulates proteasome activity, antigen presentation, and T cell responses. André, P., Groettrup, M., Klenerman, P., de Giuli, R., Booth, B.L., Cerundolo, V., Bonneville, M., Jotereau, F., Zinkernagel, R.M., Lotteau, V. Proc. Natl. Acad. Sci. U.S.A. (1998) [Pubmed]
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