DGIdb - ROSUVASTATIN Drug Record

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

(3 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: 4.91

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20347093

Sources:
PharmGKB
ROSUVASTATIN CRP

Interaction Score: 3.27

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21094359

Sources:
PharmGKB
ROSUVASTATIN HMGCR

Interaction Score: 2.94

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Competitive

Endogenous Drug? False

Direct Interaction? True

PMIDs:
11256847 11501230 12539816 12481202 16128575 11752352 11772327 12773150

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD
ROSUVASTATIN KIF6

Interaction Score: 2.45

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30304062

Sources:
PharmGKB
ROSUVASTATIN FMO3

Interaction Score: 1.23

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20679960

Sources:
PharmGKB
ROSUVASTATIN ABCG2

Interaction Score: 0.87

Interaction Types & Directionality:

n/a

Interaction Info:

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

Sources:
PharmGKB
ROSUVASTATIN ABCB11

Interaction Score: 0.61

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
ROSUVASTATIN HLA-DRB1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27839692

Sources:
PharmGKB
ROSUVASTATIN SLCO2B1

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
ROSUVASTATIN SLCO1B3

Interaction Score: 0.2

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
ROSUVASTATIN ABCC2

Interaction Score: 0.19

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30100615

Sources:
PharmGKB
ROSUVASTATIN CYP3A5

Interaction Score: 0.1

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

GuideToPharmacology: 135650928
- Version: 29-September-2020
Alternate Names:

ROSUVASTATIN GuideToPharmacology Ligand Name

Drug Info:

Publications:
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:

Specific Action of the Ligand	Competitive
Endogenous Drug?	False
Direct Interaction?	True

ROSUVASTATIN Drug Record

ROSUVASTATIN chembl:CHEMBL1496 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20347093

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21094359

Sources: PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Competitive Endogenous Drug? False Direct Interaction? True

PMIDs: 11256847 11501230 12539816 12481202 16128575 11752352 11772327 12773150

Sources: TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 30304062

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20679960

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

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

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27839692

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 30100615

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20207952

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: FDA

TEND: ROSUVASTATIN

Alternate Names: ROSUVASTATIN Primary Drug Name

Drug Info: Drug Class anticholesteremic agents Year of Approval 2003

Publications:

TdgClinicalTrial: ROSUVASTATIN

Alternate Names:

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

Publications:

PharmGKB: rosuvastatin

Alternate Names:

Drug Info:

GuideToPharmacology: 135650928

Alternate Names: ROSUVASTATIN GuideToPharmacology Ligand Name

Drug Info:

Publications:

TTD: Rosuvastatin

Alternate Names: D0JE2E TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL1496

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

n/a

PMIDs:
20347093

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
21094359

Sources:
PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Competitive

Endogenous Drug? False

Direct Interaction? True

PMIDs:
11256847 11501230 12539816 12481202 16128575 11752352 11772327 12773150

Sources:
TdgClinicalTrial TEND GuideToPharmacology TTD

Interaction Types & Directionality:

n/a

PMIDs:
30304062

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
20679960

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

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

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
27839692

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
30100615

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
20207952

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
FDA

Alternate Names:

ROSUVASTATIN Primary Drug Name

Drug Info:

Drug Class anticholesteremic agents

Year of Approval 2003

Drug Info:

Drug Indications antihypecholesterolemic agent

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

ROSUVASTATIN GuideToPharmacology Ligand Name

Alternate Names:

D0JE2E TTD Drug ID