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Chemical Compound Review

Acifugan     (3,5-dibromo-4-hydroxy- phenyl)-(2...

Synonyms: Besuric, Desuric, Urinorm, Narcaricin, Benzbromaron, ...
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Disease relevance of Benzbromaron


High impact information on Benzbromaron


Chemical compound and disease context of Benzbromaron


Biological context of Benzbromaron


Anatomical context of Benzbromaron

  • In vitro inhibition constants (K(i)) of benzbromarone for (S)-warfarin 7-hydroxylation were determined with use of human CYP2C9 and liver microsomes [2].
  • The uricosuric drug benzbromarone (3,5-dibromo-4-hydroxyphenyl)-1-(2-ethyl-3-benzofuranyl)methanone, a benzofurane derivative, was studied for its effects on parameters related to hepatic peroxisome proliferation [15].
  • By contrast, using the same range of concentrations, human hepatocytes in primary culture treated with benzbromarone revealed no enhancement of enzymatic activity and no concomitant statistically significant increase in the number of peroxisomes; the same observations were reported with clofibric acid and MEHP [16].

Associations of Benzbromaron with other chemical compounds


Gene context of Benzbromaron

  • Benzbromarone, a specific MRP1 inhibitor, decreased the initial efflux rate in 2008/MRP1 cells (4-fold) and in 2008wt cells (2-fold) [22].
  • In our efforts to identify agents that would specifically inhibit the two enzymes, benzbromarone and 3',3",5',5"-tetrabromophenolphthalein were found to be relatively selective and potent inhibitors of AKR1C1 [23].
  • Charge and substituent effects on affinity and metabolism of benzbromarone-based CYP2C19 inhibitors [24].
  • A new class of CYP2C9 inhibitors: probing 2C9 specificity with high-affinity benzbromarone derivatives [13].
  • The polarization of fluorescein transport was almost completely abolished by MRP inhibitor, benzbromarone (50 or 100 microM, applied apically), and by MRP/P-glycoprotein inhibitor, verapamil (200 microM, applied apically) [25].

Analytical, diagnostic and therapeutic context of Benzbromaron


  1. Mechanisms of benzarone and benzbromarone-induced hepatic toxicity. Kaufmann, P., Török, M., Hänni, A., Roberts, P., Gasser, R., Krähenbühl, S. Hepatology (2005) [Pubmed]
  2. Potentiation of anticoagulant effect of warfarin caused by enantioselective metabolic inhibition by the uricosuric agent benzbromarone. Takahashi, H., Sato, T., Shimoyama, Y., Shioda, N., Shimizu, T., Kubo, S., Tamura, N., Tainaka, H., Yasumori, T., Echizen, H. Clin. Pharmacol. Ther. (1999) [Pubmed]
  3. Fatal fulminant hepatic failure associated with benzbromarone. Wagayama, H., Shiraki, K., Sugimoto, K., Fujikawa, K., Shimizu, A., Takase, K., Nakano, T., Tameda, Y. J. Hepatol. (2000) [Pubmed]
  4. EULAR evidence based recommendations for gout. Part II: Management. Report of a task force of the EULAR Standing Committee For International Clinical Studies Including Therapeutics (ESCISIT). Zhang, W., Doherty, M., Bardin, T., Pascual, E., Barskova, V., Conaghan, P., Gerster, J., Jacobs, J., Leeb, B., Lioté, F., McCarthy, G., Netter, P., Nuki, G., Perez-Ruiz, F., Pignone, A., Pimentão, J., Punzi, L., Roddy, E., Uhlig, T., Zimmermann-Gòrska, I. Ann. Rheum. Dis. (2006) [Pubmed]
  5. Efficacy of allopurinol and benzbromarone for the control of hyperuricaemia. A pathogenic approach to the treatment of primary chronic gout. Perez-Ruiz, F., Alonso-Ruiz, A., Calabozo, M., Herrero-Beites, A., García-Erauskin, G., Ruiz-Lucea, E. Ann. Rheum. Dis. (1998) [Pubmed]
  6. Clinical and molecular analysis of patients with renal hypouricemia in Japan-influence of URAT1 gene on urinary urate excretion. Ichida, K., Hosoyamada, M., Hisatome, I., Enomoto, A., Hikita, M., Endou, H., Hosoya, T. J. Am. Soc. Nephrol. (2004) [Pubmed]
  7. CYP2C9 genotype-dependent effects on in vitro drug-drug interactions: switching of benzbromarone effect from inhibition to activation in the CYP2C9.3 variant. Hummel, M.A., Locuson, C.W., Gannett, P.M., Rock, D.A., Mosher, C.M., Rettie, A.E., Tracy, T.S. Mol. Pharmacol. (2005) [Pubmed]
  8. Differential roles of Arg97, Asp293, and Arg108 in enzyme stability and substrate specificity of CYP2C9. Dickmann, L.J., Locuson, C.W., Jones, J.P., Rettie, A.E. Mol. Pharmacol. (2004) [Pubmed]
  9. Biotransformation and uric acid lowering effect of benzbromarone in patients with liver cirrhosis - evidence for active benzbromarone metabolites? Walter-Sack, I., de Vries, J.X., von Bubnoff, A., Pfleilschifter, V., Raedsch, R. Eur. J. Med. Res. (1995) [Pubmed]
  10. Urate transport via human PAH transporter hOAT1 and its gene structure. Ichida, K., Hosoyamada, M., Kimura, H., Takeda, M., Utsunomiya, Y., Hosoya, T., Endou, H. Kidney Int. (2003) [Pubmed]
  11. Renal handling of uric acid in normal and gouty subject: evidence for a 4-component system. Levinson, D.J., Sorensen, L.B. Ann. Rheum. Dis. (1980) [Pubmed]
  12. Amiodarone Analog-Dependent Effects on CYP2C9-Mediated Metabolism and Kinetic Profiles. Kumar, V., Locuson, C.W., Sham, Y.Y., Tracy, T.S. Drug Metab. Dispos. (2006) [Pubmed]
  13. A new class of CYP2C9 inhibitors: probing 2C9 specificity with high-affinity benzbromarone derivatives. Locuson, C.W., Wahlstrom, J.L., Rock, D.A., Rock, D.A., Jones, J.P. Drug Metab. Dispos. (2003) [Pubmed]
  14. Variation of benzbromarone elimination in man--a population study. Walter-Sack, I., Gresser, U., Adjan, M., Kamilli, I., Ittensohn, A., de Vries, J.X., Weber, E., Zöllner, N. Eur. J. Clin. Pharmacol. (1990) [Pubmed]
  15. Toxicological studies on a benzofurane derivative. II. Demonstration of peroxisome proliferation in rat liver. Butler, E.G., Ichida, T., Maruyama, H., Schulte-Hermann, R., Williams, G.M. Toxicol. Appl. Pharmacol. (1990) [Pubmed]
  16. Toxicological studies on a benzofuran derivative. III. Comparison of peroxisome proliferation in rat and human hepatocytes in primary culture. Bichet, N., Cahard, D., Fabre, G., Remandet, B., Gouy, D., Cano, J.P. Toxicol. Appl. Pharmacol. (1990) [Pubmed]
  17. Micellar electrokinetic capillary chromatographic method for the quantitative analysis of uricosuric and antigout drugs in pharmaceutical preparations. Kou, H.S., Lin, T.P., Chung, T.C., Wu, H.L. Electrophoresis (2006) [Pubmed]
  18. Possible role of the multidrug resistance-associated protein (MRP) in chemoresistance of human melanoma cells. Berger, W., Hauptmann, E., Elbling, L., Vetterlein, M., Kokoschka, E.M., Micksche, M. Int. J. Cancer (1997) [Pubmed]
  19. Does a relationship exist between the urate pool in the body and lipid peroxidation during exercise? Mikami, T., Yoshino, Y., Ito, A. Free Radic. Res. (2000) [Pubmed]
  20. Involvement of uric acid transporter in increased renal clearance of the xanthine oxidase inhibitor oxypurinol induced by a uricosuric agent, benzbromarone. Iwanaga, T., Kobayashi, D., Hirayama, M., Maeda, T., Tamai, I. Drug Metab. Dispos. (2005) [Pubmed]
  21. Excellent uricosuric efficacy of benzbromarone in cyclosporin-A-treated renal transplant patients: a prospective study. Zürcher, R.M., Bock, H.A., Thiel, G. Nephrol. Dial. Transplant. (1994) [Pubmed]
  22. Folate concentration dependent transport activity of the Multidrug Resistance Protein 1 (ABCC1). Hooijberg, J.H., Jansen, G., Assaraf, Y.G., Kathmann, I., Pieters, R., Laan, A.C., Veerman, A.J., Kaspers, G.J., Peters, G.J. Biochem. Pharmacol. (2004) [Pubmed]
  23. Selective and potent inhibitors of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1) that metabolizes neurosteroids derived from progesterone. Higaki, Y., Usami, N., Shintani, S., Ishikura, S., El-Kabbani, O., Hara, A. Chem. Biol. Interact. (2003) [Pubmed]
  24. Charge and substituent effects on affinity and metabolism of benzbromarone-based CYP2C19 inhibitors. Locuson, C.W., Suzuki, H., Rettie, A.E., Jones, J.P. J. Med. Chem. (2004) [Pubmed]
  25. D-glucose triggers multidrug resistance-associated protein (MRP)-mediated secretion of fluorescein across rat jejunum in vitro. Legen, I., Kristl, A. Pharm. Res. (2004) [Pubmed]
  26. Analysis of benzbromarone in human plasma and urine by high-performance liquid chromatography and gas chromatography-mass spectrometry. de Vries, J.X., Walter-Sack, I., Ittensohn, A. J. Chromatogr. (1987) [Pubmed]
  27. Rapid and slow benzbromarone elimination phenotypes in man: benzbromarone and metabolite profiles. Walter-Sack, I., de Vries, J.X., Ittensohn, A., Weber, E. Eur. J. Clin. Pharmacol. (1990) [Pubmed]
  28. Efficacy of benzbromarone compared to allopurinol in lowering serum uric acid level in hyperuricemic patients. Hanvivadhanakul, P., Akkasilpa, S., Deesomchok, U. Journal of the Medical Association of Thailand = Chotmaihet thangphaet. (2002) [Pubmed]
  29. Distal permeability to urate and effects of benzofuran derivatives in the rat kidney. Kramp, R.A., Lenoir, R. Am. J. Physiol. (1975) [Pubmed]
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