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
Drug Categories	sulfonamides
Drug Categories	hydrocarbons, fluorinated
Drug Categories	fluorobenzenes
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antihypecholesterolemic agent
Drug Categories	agents causing muscle toxicity
Drug Categories	alimentary tract and metabolism
Drug Categories	benzene derivatives
Drug Categories	bsep/abcb11 substrates
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a4 substrates (strength unknown)
Drug Categories	cytochrome p-450 cyp3a5 inhibitors
Drug Categories	cytochrome p-450 cyp3a5 substrates
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	drugs used in diabetes
Drug Categories	genito urinary system and sex hormones
Drug Categories	gynecological antiinfectives and antiseptics
Drug Categories	hypolipidemic agents indicated for hyperlipidemia
Drug Categories	lipid modifying agents, plain
Drug Categories	oat3/slc22a8 inhibitors
Drug Categories	oat3/slc22a8 substrates
Drug Categories	oatp1b1/slco1b1 inhibitors

(4 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
Weitz-Schmidt G et al., 2001, Statins selectively inhibit leukocyte function antigen-1 by binding to a novel regulatory integrin site., Nat Med
Liao JK et al., 2005, Pleiotropic effects of statins., Annu Rev Pharmacol Toxicol
Katano et al., 2004, Simvastatin induces apoptosis of Epstein-Barr virus (EBV)-transformed lymphoblastoid cell lines and delays development of EBV lymphomas., Proc. Natl. Acad. Sci. U.S.A.

ROSUVASTATIN COQ2

Interaction Score: 4.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20347093

Sources:
PharmGKB
ROSUVASTATIN KIF6

Interaction Score: 2.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30304062

Sources:
PharmGKB
ROSUVASTATIN CRP

Interaction Score: 2.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21094359

Sources:
PharmGKB
ROSUVASTATIN HMGCR

Interaction Score: 1.88

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:
DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD
ROSUVASTATIN FMO3

Interaction Score: 1.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20679960

Sources:
PharmGKB
ROSUVASTATIN ABCG2

Interaction Score: 0.7

Interaction Types & Directionality:

n/a

Interaction Info:

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

Sources:
PharmGKB
ROSUVASTATIN ITGAL

Interaction Score: 0.65

Interaction Types & Directionality:

inhibitory allosteric modulator (inhibitory)

Interaction Info:

PMIDs:
11385505 15822172 15041742

Sources:
DrugBank
ROSUVASTATIN ABCB11

Interaction Score: 0.41

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
ROSUVASTATIN HLA-DRB1

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27839692

Sources:
PharmGKB
ROSUVASTATIN SLCO2B1

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
ROSUVASTATIN ABCC2

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
30100615

Sources:
PharmGKB
ROSUVASTATIN SLCO1B3

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
ROSUVASTATIN CYP3A5

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20207952

Sources:
PharmGKB
ROSUVASTATIN SLCO1B1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
FDA

DrugBank: DB01098

Version: 5.1.7

Alternate Names:

ROSUVASTATIN DrugBank Drug Name

287714-41-4 CAS Number

Ach-rosuvastatin Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories agents causing muscle toxicity

Publications:

Katano et al., 2004, Simvastatin induces apoptosis of Epstein-Barr virus (EBV)-transformed lymphoblastoid cell lines and delays development of EBV lymphomas., Proc. Natl. Acad. Sci. U.S.A.

Liao JK et al., 2005, Pleiotropic effects of statins., Annu Rev Pharmacol Toxicol

Weitz-Schmidt G et al., 2001, Statins selectively inhibit leukocyte function antigen-1 by binding to a novel regulatory integrin site., Nat Med

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	DrugBank Drug Name
287714-41-4	CAS Number
Ach-rosuvastatin	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Categories	agents causing muscle toxicity

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: 30304062

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: DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD

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: inhibitory allosteric modulator (inhibitory)

Interaction Info:

PMIDs: 11385505 15822172 15041742

Sources: DrugBank

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: 30100615

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

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

DrugBank: DB01098

Alternate Names: ROSUVASTATIN DrugBank Drug Name 287714-41-4 CAS Number Ach-rosuvastatin Drug Brand

Drug Info: Drug Type small molecule Drug Groups approved Drug Categories agents causing muscle toxicity

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

Interaction Types & Directionality:

n/a

PMIDs:
20347093

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
30304062

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:
DrugBank TdgClinicalTrial TEND GuideToPharmacology TTD

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:

inhibitory allosteric modulator (inhibitory)

PMIDs:
11385505 15822172 15041742

Sources:
DrugBank

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:
30100615

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
20207952

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
FDA

Alternate Names:

ROSUVASTATIN DrugBank Drug Name

287714-41-4 CAS Number

Ach-rosuvastatin Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories agents causing muscle toxicity

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