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Chemical Compound Review

CHEBI:507351     calcium(E,3R,5R)-7-[4-(4- fluorophenyl)-2...

Synonyms: DNC013454, AKOS015967307, AC1O5M4W, Rosuvastatin calcium
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Disease relevance of HSDB 7317


Psychiatry related information on HSDB 7317


High impact information on HSDB 7317

  • On the basis of these criteria, rosuvastatin represents a step forward in efforts to optimize the pharmacologic properties of the statin class [6].
  • Compared with other statins, rosuvastatin has been found to be a relatively potent inhibitor of HMG-CoA reductase and to have a high degree of selectivity for effect in liver cells compared with a range of non-hepatic cells, including cultured human skeletal muscle cells [6].
  • In addition, rosuvastatin undergoes relatively little metabolism by the hepatic CYP system; it has a moderate degree of systemic bioavailability and a relatively long elimination half-life [6].
  • The effects of rosuvastatin are selective for hepatic cells, and there is minimal uptake of the drug by nonhepatic tissues [7].
  • Naturally occurring polymorphisms in OATP1B1, including *5, *9, *15, and *18, were associated with profound loss of activity toward rosuvastatin [8].

Chemical compound and disease context of HSDB 7317


Biological context of HSDB 7317


Anatomical context of HSDB 7317


Associations of HSDB 7317 with other chemical compounds

  • Effects of rosuvastatin on nitric oxide-dependent function in aorta and corpus cavernosum of diabetic mice: relationship to cholesterol biosynthesis pathway inhibition and lipid lowering [19].
  • Superoxide anion production induced by 500 mg/dl dextrose was inhibited by therapeutic concentrations of rosuvastatin or simvastatin (10 nmol/l), whereas the increased levels of cellular endothelin 1 mRNA and endothelin 1 in culture media was inhibited by supratherapeutic concentrations of statins (> or =0.1 micromol/l) [20].
  • RESULTS: Rosuvastatin reduced arterial pressure in SHR rats, but not in WKY/L-NAME rats [14].
  • Therefore rosuvastatin pharmacokinetic parameters were assessed in an open-label trial involving stable heart transplant recipients (> or =6 months after transplant) on an antirejection regimen including cyclosporine [21].
  • Platelets from rosuvastatin-treated non-fructose-fed (NFF) and fructose-fed (FF) hamsters were analyzed for aggregability and psPDI-denitrosation activity [16].

Gene context of HSDB 7317


Analytical, diagnostic and therapeutic context of HSDB 7317


  1. Rosuvastatin treatment prevents progressive kidney inflammation and fibrosis in stroke-prone rats. Gianella, A., Nobili, E., Abbate, M., Zoja, C., Gelosa, P., Mussoni, L., Bellosta, S., Canavesi, M., Rottoli, D., Guerrini, U., Brioschi, M., Banfi, C., Tremoli, E., Remuzzi, G., Sironi, L. Am. J. Pathol. (2007) [Pubmed]
  2. Direct vascular and cardioprotective effects of rosuvastatin, a new HMG-CoA reductase inhibitor. Jones, S.P., Gibson, M.F., Rimmer, D.M., Gibson, T.M., Sharp, B.R., Lefer, D.J. J. Am. Coll. Cardiol. (2002) [Pubmed]
  3. Short-term memory loss associated with rosuvastatin. Galatti, L., Polimeni, G., Salvo, F., Romani, M., Sessa, A., Spina, E. Pharmacotherapy (2006) [Pubmed]
  4. Rosuvastatin: a risk-benefit assessment for intensive lipid lowering. Ferdinand, K.C. Expert opinion on pharmacotherapy. (2005) [Pubmed]
  5. Treatment with rosuvastatin for severe dyslipidemia in patients with schizophrenia and schizoaffective disorder. De Hert, M., Kalnicka, D., van Winkel, R., Wampers, M., Hanssens, L., Van Eyck, D., Scheen, A., Peuskens, J. The Journal of clinical psychiatry (2006) [Pubmed]
  6. Comparative pharmacology of rosuvastatin. McTaggart, F. Atherosclerosis. Supplements. (2003) [Pubmed]
  7. Optimizing the pharmacology of statins: characteristics of rosuvastatin. Chapman, M.J., McTaggart, F. Atherosclerosis. Supplements. (2002) [Pubmed]
  8. Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics. Ho, R.H., Tirona, R.G., Leake, B.F., Glaeser, H., Lee, W., Lemke, C.J., Wang, Y., Kim, R.B. Gastroenterology (2006) [Pubmed]
  9. A comparative study with rosuvastatin in subjects with metabolic syndrome: results of the COMETS study. Stalenhoef, A.F., Ballantyne, C.M., Sarti, C., Murin, J., Tonstad, S., Rose, H., Wilpshaar, W. Eur. Heart J. (2005) [Pubmed]
  10. Strategies to enhance epidermal growth factor inhibition: targeting the mevalonate pathway. Dimitroulakos, J., Lorimer, I.A., Goss, G. Clin. Cancer Res. (2006) [Pubmed]
  11. Cross-talk between dyslipidemia and renin-angiotensin system and the role of LOX-1 and MAPK in atherogenesis studies with the combined use of rosuvastatin and candesartan. Chen, J., Li, D., Schaefer, R., Mehta, J.L. Atherosclerosis (2006) [Pubmed]
  12. Improved endothelial function and reduced platelet activation by chronic HMG-CoA-reductase inhibition with rosuvastatin in rats with streptozotocin-induced diabetes mellitus. Schäfer, A., Fraccarollo, D., Vogt, C., Flierl, U., Hemberger, M., Tas, P., Ertl, G., Bauersachs, J. Biochem. Pharmacol. (2007) [Pubmed]
  13. Rhabdomyolysis associated with pomegranate juice consumption. Sorokin, A.V., Duncan, B., Panetta, R., Thompson, P.D. Am. J. Cardiol. (2006) [Pubmed]
  14. Beneficial pleiotropic vascular effects of rosuvastatin in two hypertensive models. Susic, D., Varagic, J., Ahn, J., Slama, M., Frohlich, E.D. J. Am. Coll. Cardiol. (2003) [Pubmed]
  15. The effect of gemfibrozil on the pharmacokinetics of rosuvastatin. Schneck, D.W., Birmingham, B.K., Zalikowski, J.A., Mitchell, P.D., Wang, Y., Martin, P.D., Lasseter, K.C., Brown, C.D., Windass, A.S., Raza, A. Clin. Pharmacol. Ther. (2004) [Pubmed]
  16. Antioxidant and antiplatelet effects of rosuvastatin in a hamster model of prediabetes. Miersch, S., Sliskovic, I., Raturi, A., Mutus, B. Free Radic. Biol. Med. (2007) [Pubmed]
  17. Rapid immunomodulation by rosuvastatin in patients with acute coronary syndrome. Link, A., Ayadhi, T., B??hm, M., Nickenig, G. Eur. Heart J. (2006) [Pubmed]
  18. Effects of rosuvastatin on postprandial leukocytes in mildly hyperlipidemic patients with premature coronary sclerosis. van Oostrom, A.J., Plokker, H.W., van Asbeck, B.S., Rabelink, T.J., van Kessel, K.P., Jansen, E.H., Stehouwer, C.D., Cabezas, M.C. Atherosclerosis (2006) [Pubmed]
  19. Effects of rosuvastatin on nitric oxide-dependent function in aorta and corpus cavernosum of diabetic mice: relationship to cholesterol biosynthesis pathway inhibition and lipid lowering. Nangle, M.R., Cotter, M.A., Cameron, N.E. Diabetes (2003) [Pubmed]
  20. Statins prevent dextrose-induced endothelial barrier dysfunction, possibly through inhibition of superoxide formation. Haas, M.J., Horani, M.H., Parseghian, S.A., Mooradian, A.D. Diabetes (2006) [Pubmed]
  21. Rosuvastatin pharmacokinetics in heart transplant recipients administered an antirejection regimen including cyclosporine. Simonson, S.G., Raza, A., Martin, P.D., Mitchell, P.D., Jarcho, J.A., Brown, C.D., Windass, A.S., Schneck, D.W. Clin. Pharmacol. Ther. (2004) [Pubmed]
  22. Effect of itraconazole on the pharmacokinetics of rosuvastatin. Cooper, K.J., Martin, P.D., Dane, A.L., Warwick, M.J., Schneck, D.W., Cantarini, M.V. Clin. Pharmacol. Ther. (2003) [Pubmed]
  23. ATP-dependent transport of rosuvastatin in membrane vesicles expressing breast cancer resistance protein. Huang, L., Wang, Y., Grimm, S. Drug Metab. Dispos. (2006) [Pubmed]
  24. The effect of fluconazole on the pharmacokinetics of rosuvastatin. Cooper, K.J., Martin, P.D., Dane, A.L., Warwick, M.J., Schneck, D.W., Cantarini, M.V. Eur. J. Clin. Pharmacol. (2002) [Pubmed]
  25. Rosuvastatin. Carswell, C.I., Plosker, G.L., Jarvis, B. Drugs (2002) [Pubmed]
  26. Phenotype-dependent and -independent actions of rosuvastatin on atherogenic lipoprotein subfractions in hyperlipidaemia. Caslake, M.J., Stewart, G., Day, S.P., Daly, E., McTaggart, F., Chapman, M.J., Durrington, P., Laggner, P., Mackness, M., Pears, J., Packard, C.J. Atherosclerosis (2003) [Pubmed]
  27. Rosuvastatin attenuates monocyte-endothelial cell interactions and vascular free radical production in hypercholesterolemic mice. Li, W., Asagami, T., Matsushita, H., Lee, K.H., Tsao, P.S. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
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