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ROSUVASTATIN Drug Record

  • Summary
  • Interactions
  • Claims
  • ROSUVASTATIN chembl:CHEMBL1496 Approved

    Alternate Names:

    ROSUVASTATIN
    ZD4522
    ZD-4522
    (3R,5S,6E)-7-(4-(4-FLUOROPHENYL)-6-(1-METHYLETHYL)-2-(ETHYL(METHYLSULFONYL)AMINO)-5-PYRIMIDINYL)-3,5-DIHYDROXY-6-HEPTENOIC ACID
    (3R,5S,6E)-7-{4-(4-FLUOROPHENYL)-6-ISOPROPYL-2-[METHYL(METHYLSULFONYL)AMINO]PYRIMIDIN-5-YL}-3,5-DIHYDROXYHEPT-6-ENOIC ACID
    CRESTOR®
    pubchem.compound:446157
    drugbank:01098
    rxcui:301542
    chembl:CHEMBL1496
    chemidplus:287714-41-4

    Drug Info:

    Year of Approval 2003
    Drug Class anticholesteremic agents
    FDA Approval approved
    Drug Class Small Molecule
    Drug Indications antihypecholesterolemic agent
    (2 More Sources)

    Publications:

    Bailey KM et al., 2010, Hepatic metabolism and transporter gene variants enhance response to rosuvastatin in patients with acute myocardial infarction: the GEOSTAT-1 Study., Circ Cardiovasc Genet
    Hu M et al., 2010, Effect of central obesity, low high-density lipoprotein cholesterol and C-reactive protein polymorphisms on C-reactive protein levels during treatment with Rosuvastatin (10 mg Daily)., Am J Cardiol
    Soko ND et al., 2019, An African-specific profile of pharmacogene variants for rosuvastatin plasma variability: limited role for SLCO1B1 c.521T>C and ABCG2 c.421A>C., Pharmacogenomics J
    McTaggart et al., 2001, Preclinical and clinical pharmacology of Rosuvastatin, a new 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor., Am. J. Cardiol.
    Hanefeld, Clinical rationale for rosuvastatin, a potent new HMG-CoA reductase inhibitor., Int. J. Clin. Pract.
    Chapman et al., 2003, New dimension of statin action on ApoB atherogenicity., Clin Cardiol
    Olsson et al., 2002, Rosuvastatin: a highly effective new HMG-CoA reductase inhibitor., Cardiovasc Drug Rev
    Carbonell et al., 2005, Binding thermodynamics of statins to HMG-CoA reductase., Biochemistry
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Davidson, 2002, Rosuvastatin: a highly efficacious statin for the treatment of dyslipidaemia., Expert Opin Investig Drugs
    Holdgate et al., 2003, Molecular mechanism for inhibition of 3-hydroxy-3-methylglutaryl CoA (HMG-CoA) reductase by rosuvastatin., Biochem. Soc. Trans.
    Ruiz-Iruela C et al., 2018, KIF6 gene as a pharmacogenetic marker for lipid-lowering effect in statin treatment., PLoS One
    Hu M et al., 2010, Pharmacogenetic analysis of lipid responses to rosuvastatin in Chinese patients., Pharmacogenet Genomics
    Puccetti L et al., 2010, Genetic involvement in statins induced myopathy. Preliminary data from an observational case-control study., Atherosclerosis
    Kashihara Y et al., 2017, Small-Dosing Clinical Study: Pharmacokinetic, Pharmacogenomic (SLCO2B1 and ABCG2), and Interaction (Atorvastatin and Grapefruit Juice) Profiles of 5 Probes for OATP2B1 and BCRP., J Pharm Sci
    Birmingham BK et al., 2015, Rosuvastatin pharmacokinetics and pharmacogenetics in Caucasian and Asian subjects residing in the United States., Eur J Clin Pharmacol
    Lee HK et al., 2013, Effects of polymorphisms in ABCG2, SLCO1B1, SLC10A1 and CYP2C9/19 on plasma concentrations of rosuvastatin and lipid response in Chinese patients., Pharmacogenomics
    Chasman DI et al., 2012, Genetic determinants of statin-induced low-density lipoprotein cholesterol reduction: the Justification for the Use of Statins in Prevention: an Intervention Trial Evaluating Rosuvastatin (JUPITER) trial., Circ Cardiovasc Genet
    Tomlinson B et al., 2010, ABCG2 polymorphism is associated with the low-density lipoprotein cholesterol response to rosuvastatin., Clin Pharmacol Ther
    Kitamura S et al., 2008, Involvement of multiple transporters in the hepatobiliary transport of rosuvastatin., Drug Metab Dispos
    Zhang W et al., 2006, Role of BCRP 421C>A polymorphism on rosuvastatin pharmacokinetics in healthy Chinese males., Clin Chim Acta
    Keskitalo JE et al., 2009, ABCG2 polymorphism markedly affects the pharmacokinetics of atorvastatin and rosuvastatin., Clin Pharmacol Ther
    Sai K et al., 2016, A possible role for HLA-DRB1*04:06 in statin-related myopathy in Japanese patients., Drug Metab Pharmacokinet
  • ROSUVASTATIN   COQ2

    Interaction Score: 4.76

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20347093


    Sources:
    PharmGKB

  • ROSUVASTATIN   CRP

    Interaction Score: 3.17

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21094359


    Sources:
    PharmGKB

  • ROSUVASTATIN   HMGCR

    Interaction Score: 2.75

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Crestor
    Novel drug target Established target

    PMIDs:
    11256847 11501230 12539816 12481202 16128575 11752352 11772327 12773150


    Sources:
    TdgClinicalTrial TEND TTD

  • ROSUVASTATIN   KIF6

    Interaction Score: 2.38

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    30304062


    Sources:
    PharmGKB

  • ROSUVASTATIN   FMO3

    Interaction Score: 1.19

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20679960


    Sources:
    PharmGKB

  • ROSUVASTATIN   ABCG2

    Interaction Score: 0.84

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28322941 25630984 23930675 22331829 20679960 20207952 20130569 18617601 16784736 19474787


    Sources:
    PharmGKB

  • ROSUVASTATIN   ABCB11

    Interaction Score: 0.59

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • ROSUVASTATIN   HLA-DRB1

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27839692


    Sources:
    PharmGKB

  • ROSUVASTATIN   SLCO2B1

    Interaction Score: 0.26

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • ROSUVASTATIN   SLCO1B3

    Interaction Score: 0.24

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • ROSUVASTATIN   ABCC2

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    30100615


    Sources:
    PharmGKB

  • ROSUVASTATIN   CYP3A5

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20207952


    Sources:
    PharmGKB

  • ROSUVASTATIN   SLCO1B1

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    FDA

  • TEND: ROSUVASTATIN

    • Version: 01-August-2011

    Alternate Names:
    ROSUVASTATIN Primary Drug Name

    Drug Info:
    Drug Class anticholesteremic agents
    Year of Approval 2003

    Publications:

  • TdgClinicalTrial: ROSUVASTATIN

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications antihypecholesterolemic agent
    Drug Class Small Molecule
    FDA Approval approved

    Publications:

  • PharmGKB: rosuvastatin

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Bailey KM et al., 2010, Hepatic metabolism and transporter gene variants enhance response to rosuvastatin in patients with acute myocardial infarction: the GEOSTAT-1 Study., Circ Cardiovasc Genet
    Hu M et al., 2010, Pharmacogenetic analysis of lipid responses to rosuvastatin in Chinese patients., Pharmacogenet Genomics
    Soko ND et al., 2019, An African-specific profile of pharmacogene variants for rosuvastatin plasma variability: limited role for SLCO1B1 c.521T>C and ABCG2 c.421A>C., Pharmacogenomics J

  • TTD: Rosuvastatin

    • Version: 2020.06.01

    Alternate Names:
    D0JE2E TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL1496

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Rosuvastatin

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

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A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21