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Identification
NameRosuvastatin
Accession NumberDB01098  (APRD00546)
TypeSmall Molecule
GroupsApproved
Description

Rosuvastatin is an antilipemic agent that competitively inhibits hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase. HMG-CoA reducuase catalyzes the conversion of HMG-CoA to mevalonic acid, the rate-limiting step in cholesterol biosynthesis. Rosuvastatin belongs to a class of medications called statins and is used to reduce plasma cholesterol levels and prevent cardiovascular disease.

Structure
Thumb
Synonyms
(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
External Identifiers
  • ZD-4522
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ach-rosuvastatintablet5 mgoralAccord Healthcare IncNot applicableNot applicableCanada
Ach-rosuvastatintablet20 mgoralAccord Healthcare IncNot applicableNot applicableCanada
Ach-rosuvastatintablet10 mgoralAccord Healthcare IncNot applicableNot applicableCanada
Ach-rosuvastatintablet40 mgoralAccord Healthcare IncNot applicableNot applicableCanada
Act Rosuvastatintablet40 mgoralActavis Pharma Company2012-03-16Not applicableCanada
Act Rosuvastatintablet20 mgoralActavis Pharma Company2012-03-16Not applicableCanada
Act Rosuvastatintablet10 mgoralActavis Pharma Company2012-03-16Not applicableCanada
Act Rosuvastatintablet5 mgoralActavis Pharma Company2012-03-16Not applicableCanada
Auro-rosuvastatintablet40 mgoralAuro Pharma Inc2015-11-30Not applicableCanada
Auro-rosuvastatintablet20 mgoralAuro Pharma Inc2015-11-30Not applicableCanada
Auro-rosuvastatintablet10 mgoralAuro Pharma Inc2015-11-30Not applicableCanada
Auro-rosuvastatintablet5 mgoralAuro Pharma Inc2015-11-30Not applicableCanada
Bio-rosuvastatintablet10 mgoralBiomed PharmaNot applicableNot applicableCanada
Bio-rosuvastatintablet40 mgoralBiomed PharmaNot applicableNot applicableCanada
Bio-rosuvastatintablet5 mgoralBiomed PharmaNot applicableNot applicableCanada
Bio-rosuvastatintablet20 mgoralBiomed PharmaNot applicableNot applicableCanada
Crestortablet, coated10 mg/1oralLake Erie Medical DBA Quality Care Products LLC2010-11-09Not applicableUs
Crestortablet, film coated20 mg/1oralCardinal Health2010-12-01Not applicableUs
Crestortablet, film coated10 mg/1oralAstra Zeneca Pharmaceuticals Lp2003-08-18Not applicableUs
Crestortablet, film coated10 mg/1oralPd Rx Pharmaceuticals, Inc.2003-08-18Not applicableUs
Crestortablet, film coated5 mg/1oralREMEDYREPACK INC.2013-02-27Not applicableUs
Crestortablet, film coated40 mg/1oralRebel Distributors Corp2004-11-01Not applicableUs
Crestortablet, film coated10 mg/1oralPhysicians Total Care, Inc.2003-11-25Not applicableUs
Crestortablet, film coated40 mg/1oralMedsource Pharmaceuticals2003-08-18Not applicableUs
Crestortablet, film coated40 mg/1oralCardinal Health2010-12-01Not applicableUs
Crestortablet, film coated20 mg/1oralRebel Distributors Corp2004-06-07Not applicableUs
Crestortablet, film coated40 mg/1oralPhysicians Total Care, Inc.2004-11-01Not applicableUs
Crestortablet, film coated10 mg/1oralAphena Pharma Solutions Tennessee, Llc2003-08-18Not applicableUs
Crestortablet, film coated20 mg/1oralCardinal Health2010-12-01Not applicableUs
Crestortablet, film coated10 mg/1oralRebel Distributors Corp2003-11-25Not applicableUs
Crestortablet, film coated5 mg/1oralCarilion Materials Management2003-08-18Not applicableUs
Crestortablet, film coated5 mg/1oralA S Medication Solutions Llc2005-10-26Not applicableUs
Crestortablet, film coated20 mg/1oralAphena Pharma Solutions Tennessee, Llc2003-08-18Not applicableUs
Crestortablet, film coated5 mg/1oralCardinal Health2010-12-01Not applicableUs
Crestortablet, film coated5 mg/1oralAstra Zeneca Pharmaceuticals Lp2003-08-18Not applicableUs
Crestortablet, film coated5 mg/1oralbryant ranch prepack2010-12-01Not applicableUs
Crestortablet, film coated20 mg/1oralA S Medication Solutions Llc2005-04-14Not applicableUs
Crestortablet, film coated40 mg/1oralAphena Pharma Solutions Tennessee, Llc2003-08-18Not applicableUs
Crestortablet, film coated10 mg/1oralCardinal Health2010-12-01Not applicableUs
Crestortablet, film coated40 mg/1oralAstra Zeneca Pharmaceuticals Lp2003-08-18Not applicableUs
Crestortablet, film coated5 mg/1oralbryant ranch prepack2003-08-18Not applicableUs
Crestortablet, film coated10 mg/1oralA S Medication Solutions Llc2004-09-02Not applicableUs
Crestortablet, coated40 mg/1oralLake Erie Medical DBA Quality Care Products LLC2010-09-08Not applicableUs
Crestortablet, film coated5 mg/1oralPhysicians Total Care, Inc.2005-06-22Not applicableUs
Crestortablet, film coated20 mg/1oralLake Erie Medical & Surgucal Supply DBA Quality Care Products LLC2012-02-27Not applicableUs
Crestortablet, film coated20 mg/1oralPd Rx Pharmaceuticals, Inc.2003-08-18Not applicableUs
Crestortablet, film coated20 mg/1oralAstra Zeneca Pharmaceuticals Lp2003-08-18Not applicableUs
Crestortablet, film coated10 mg/1oralbryant ranch prepack2010-12-01Not applicableUs
Crestortablet, film coated20 mg/1oralH.J. Harkins Company, Inc.2011-07-21Not applicableUs
Crestortablet, film coated10 mg/1oralCardinal Health2010-12-01Not applicableUs
Crestortablet, film coated5 mg/1oralRebel Distributors Corp2005-06-22Not applicableUs
Crestortablet, film coated20 mg/1oralPhysicians Total Care, Inc.2004-06-07Not applicableUs
Crestor - 10mgtablet10 mgoralAstrazeneca Canada Inc2003-02-19Not applicableCanada
Crestor - 20mgtablet20 mgoralAstrazeneca Canada Inc2003-02-19Not applicableCanada
Crestor - 40mgtablet40 mgoralAstrazeneca Canada Inc2003-02-19Not applicableCanada
Crestor - 5mgtablet5 mgoralAstrazeneca Canada Inc2005-03-18Not applicableCanada
Dom-rosuvastatintablet20 mgoralDominion Pharmacal2013-09-28Not applicableCanada
Dom-rosuvastatintablet10 mgoralDominion Pharmacal2013-09-28Not applicableCanada
Dom-rosuvastatintablet40 mgoralDominion PharmacalNot applicableNot applicableCanada
Dom-rosuvastatintablet5 mgoralDominion Pharmacal2013-09-28Not applicableCanada
Ipg-rosuvastatintablet10 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Ipg-rosuvastatintablet5 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Ipg-rosuvastatintablet40 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Ipg-rosuvastatintablet20 mgoralMarcan Pharmaceuticals IncNot applicableNot applicableCanada
Jamp-rosuvastatintablet40.0 mgoralJamp Pharma Corporation2012-09-24Not applicableCanada
Jamp-rosuvastatintablet20.0 mgoralJamp Pharma Corporation2012-09-24Not applicableCanada
Jamp-rosuvastatintablet10.0 mgoralJamp Pharma Corporation2012-09-24Not applicableCanada
Jamp-rosuvastatintablet5 mgoralJamp Pharma Corporation2012-09-24Not applicableCanada
Mar-rosuvastatintablet20 mgoralMarcan Pharmaceuticals Inc2014-06-26Not applicableCanada
Mar-rosuvastatintablet10 mgoralMarcan Pharmaceuticals Inc2014-06-26Not applicableCanada
Mar-rosuvastatintablet5 mgoralMarcan Pharmaceuticals Inc2014-06-26Not applicableCanada
Mar-rosuvastatintablet40 mgoralMarcan Pharmaceuticals Inc2014-06-26Not applicableCanada
Med-rosuvastatintablet40 mgoralGeneric Medical Partners Inc2013-11-27Not applicableCanada
Med-rosuvastatintablet20 mgoralGeneric Medical Partners Inc2013-11-27Not applicableCanada
Med-rosuvastatintablet10 mgoralGeneric Medical Partners Inc2013-11-27Not applicableCanada
Med-rosuvastatintablet5 mgoralGeneric Medical Partners Inc2013-11-27Not applicableCanada
Mint-rosuvastatintablet10 mgoralMint Pharmaceuticals Inc2013-07-02Not applicableCanada
Mint-rosuvastatintablet40 mgoralMint Pharmaceuticals Inc2013-07-02Not applicableCanada
Mint-rosuvastatintablet5 mgoralMint Pharmaceuticals Inc2013-07-02Not applicableCanada
Mint-rosuvastatintablet20 mgoralMint Pharmaceuticals Inc2013-07-02Not applicableCanada
Mylan-rosuvastatintablet40 mgoralMylan Pharmaceuticals Ulc2012-04-17Not applicableCanada
Mylan-rosuvastatintablet20 mgoralMylan Pharmaceuticals Ulc2012-03-15Not applicableCanada
Mylan-rosuvastatintablet10 mgoralMylan Pharmaceuticals Ulc2012-03-15Not applicableCanada
Mylan-rosuvastatintablet5 mgoralMylan Pharmaceuticals Ulc2012-03-15Not applicableCanada
Novo-rosuvastatintablet40 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Novo-rosuvastatintablet20 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Novo-rosuvastatintablet10 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Novo-rosuvastatintablet5 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-rosuvastatintablet5 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-rosuvastatintablet40 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-rosuvastatintablet20 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-rosuvastatintablet10 mgoralTeva Canada LimitedNot applicableNot applicableCanada
PMS-rosuvastatintablet10 mgoralPharmascience Inc2012-03-15Not applicableCanada
PMS-rosuvastatintablet40 mgoralPharmascience Inc2012-03-15Not applicableCanada
PMS-rosuvastatintablet5 mgoralPharmascience Inc2012-03-15Not applicableCanada
PMS-rosuvastatintablet20 mgoralPharmascience Inc2012-03-15Not applicableCanada
Priva-rosuvastatintablet40 mgoralPharmapar IncNot applicableNot applicableCanada
Priva-rosuvastatintablet20 mgoralPharmapar IncNot applicableNot applicableCanada
Priva-rosuvastatintablet10 mgoralPharmapar IncNot applicableNot applicableCanada
Priva-rosuvastatintablet5 mgoralPharmapar IncNot applicableNot applicableCanada
Q-rosuvastatintablet5 mgoralQd Pharmaceuticals UlcNot applicableNot applicableCanada
Q-rosuvastatintablet40.0 mgoralQd Pharmaceuticals UlcNot applicableNot applicableCanada
Q-rosuvastatintablet20.0 mgoralQd Pharmaceuticals UlcNot applicableNot applicableCanada
Q-rosuvastatintablet10.0 mgoralQd Pharmaceuticals UlcNot applicableNot applicableCanada
Ran-rosuvastatintablet10 mgoralRanbaxy Pharmaceuticals Canada Inc.2012-04-02Not applicableCanada
Ran-rosuvastatintablet40 mgoralRanbaxy Pharmaceuticals Canada Inc.2012-04-02Not applicableCanada
Ran-rosuvastatintablet5 mgoralRanbaxy Pharmaceuticals Canada Inc.2012-04-02Not applicableCanada
Ran-rosuvastatintablet20 mgoralRanbaxy Pharmaceuticals Canada Inc.2012-04-02Not applicableCanada
Riva-rosuvastatintablet40 mgoralLaboratoire Riva Inc2012-06-13Not applicableCanada
Riva-rosuvastatintablet20 mgoralLaboratoire Riva Inc2012-06-13Not applicableCanada
Riva-rosuvastatintablet10 mgoralLaboratoire Riva Inc2012-06-11Not applicableCanada
Riva-rosuvastatintablet5 mgoralLaboratoire Riva Inc2012-06-11Not applicableCanada
Rosuvastatintablet5 mgoralPro Doc Limitee2012-07-19Not applicableCanada
Rosuvastatintablet5 mgoralSivem Pharmaceuticals Ulc2012-07-11Not applicableCanada
Rosuvastatintablet10.0 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Rosuvastatintablet40 mgoralCobalt Pharmaceuticals CompanyNot applicableNot applicableCanada
Rosuvastatintablet5.0 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Rosuvastatintablet20 mgoralCobalt Pharmaceuticals CompanyNot applicableNot applicableCanada
Rosuvastatintablet40 mgoralSanis Health Inc2013-06-12Not applicableCanada
Rosuvastatintablet10 mgoralCobalt Pharmaceuticals CompanyNot applicableNot applicableCanada
Rosuvastatintablet20 mgoralSanis Health Inc2013-06-12Not applicableCanada
Rosuvastatintablet40 mgoralPro Doc Limitee2012-07-19Not applicableCanada
Rosuvastatintablet40 mgoralSivem Pharmaceuticals Ulc2012-07-11Not applicableCanada
Rosuvastatintablet5 mgoralCobalt Pharmaceuticals CompanyNot applicableNot applicableCanada
Rosuvastatintablet10 mgoralSanis Health Inc2013-06-12Not applicableCanada
Rosuvastatintablet20 mgoralPro Doc Limitee2012-07-19Not applicableCanada
Rosuvastatintablet20 mgoralSivem Pharmaceuticals Ulc2012-07-11Not applicableCanada
Rosuvastatintablet40.0 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Rosuvastatintablet5 mgoralSanis Health Inc2013-06-12Not applicableCanada
Rosuvastatintablet10 mgoralPro Doc Limitee2012-07-19Not applicableCanada
Rosuvastatintablet10 mgoralSivem Pharmaceuticals Ulc2012-07-11Not applicableCanada
Rosuvastatintablet20.0 mgoralRanbaxy Pharmaceuticals Canada Inc.Not applicableNot applicableCanada
Rosuvastatin-10tablet10 mgoralSivem Pharmaceuticals Ulc2013-10-23Not applicableCanada
Rosuvastatin-20tablet20 mgoralSivem Pharmaceuticals Ulc2013-10-23Not applicableCanada
Rosuvastatin-40tablet40 mgoralSivem Pharmaceuticals Ulc2013-10-23Not applicableCanada
Rosuvastatin-5tablet5 mgoralSivem Pharmaceuticals Ulc2013-10-23Not applicableCanada
Sandoz Rosuvastatintablet40 mgoralSandoz Canada Incorporated2012-03-15Not applicableCanada
Sandoz Rosuvastatintablet20 mgoralSandoz Canada Incorporated2012-03-15Not applicableCanada
Sandoz Rosuvastatintablet10 mgoralSandoz Canada Incorporated2012-03-15Not applicableCanada
Sandoz Rosuvastatintablet5 mgoralSandoz Canada Incorporated2012-03-15Not applicableCanada
Teva-rosuvastatintablet5 mgoralTeva Canada Limited2012-03-15Not applicableCanada
Teva-rosuvastatintablet20 mgoralTeva Canada Limited2012-03-15Not applicableCanada
Teva-rosuvastatintablet10 mgoralTeva Canada Limited2012-03-15Not applicableCanada
Teva-rosuvastatintablet40 mgoralTeva Canada Limited2012-03-15Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-rosuvastatintablet5 mgoralApotex Inc2012-04-02Not applicableCanada
Apo-rosuvastatintablet40 mgoralApotex Inc2012-04-02Not applicableCanada
Apo-rosuvastatintablet20 mgoralApotex Inc2012-04-02Not applicableCanada
Apo-rosuvastatintablet10 mgoralApotex Inc2012-04-02Not applicableCanada
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AstendeLazar (Argentina)
CirantanAstraZeneca (Netherlands)
CresadexDrugtech (Chile)
Provisacor AstraZeneca (Italy, Netherlands)
RazelGlenmark (India)
RosedexRoux-Ocefa (Argentina)
RosimolSandoz (Argentina)
RosumedLabomed (Chile)
RosustatinMontpellier (Argentina)
RosuvasRanbaxy (India)
RosuvastBago (Argentina)
RosvelLaboratorios Chile (Chile)
RovartalRoemmers (Argentina)
SimestatSimesa (Italy)
SinlipGador (Argentina)
VisacorAstraZeneca (Portugal)
VivacorAstraZeneca (Brazil)
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Rosuvastatin calcium
Thumb
  • InChI Key: LALFOYNTGMUKGG-BGRFNVSISA-L
  • Monoisotopic Mass: 1000.283510167
  • Average Mass: 1001.137
DBSALT000154
Rosuvastatin zinc
ThumbNot applicableDBSALT001337
Categories
UNII413KH5ZJ73
CAS number287714-41-4
WeightAverage: 481.538
Monoisotopic: 481.168284538
Chemical FormulaC22H28FN3O6S
InChI KeyInChIKey=BPRHUIZQVSMCRT-VEUZHWNKSA-N
InChI
InChI=1S/C22H28FN3O6S/c1-13(2)20-18(10-9-16(27)11-17(28)12-19(29)30)21(14-5-7-15(23)8-6-14)25-22(24-20)26(3)33(4,31)32/h5-10,13,16-17,27-28H,11-12H2,1-4H3,(H,29,30)/b10-9+/t16-,17-/m1/s1
IUPAC Name
(3R,5S,6E)-7-[4-(4-fluorophenyl)-2-(N-methylmethanesulfonamido)-6-(propan-2-yl)pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid
SMILES
CC(C)C1=NC(=NC(C2=CC=C(F)C=C2)=C1\C=C\[C@@H](O)C[C@@H](O)CC(=O)O)N(C)S(C)(=O)=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylpyrimidines. These are polycyclic aromatic compounds containing a benzene ring linked to a pyrimidine ring through a CC or CN bond. Pyrimidine is a 6-membered ring consisting of four carbon atoms and two nitrogen centers at the 1- and 3- ring positions.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassDiazines
Sub ClassPyrimidines and pyrimidine derivatives
Direct ParentPhenylpyrimidines
Alternative Parents
Substituents
  • 4-phenylpyrimidine
  • Medium-chain hydroxy acid
  • Medium-chain fatty acid
  • Heterocyclic fatty acid
  • Halogenated fatty acid
  • Halobenzene
  • Fluorobenzene
  • Beta-hydroxy acid
  • Fatty acyl
  • Fatty acid
  • Benzenoid
  • Unsaturated fatty acid
  • Hydroxy acid
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Heteroaromatic compound
  • Aminosulfonyl compound
  • Sulfonyl
  • Sulfonic acid derivative
  • Sulfonamide
  • Secondary alcohol
  • Azacycle
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Carbonyl group
  • Alcohol
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationUsed as an adjunct to dietary therapy to treat primary hyperlipidemia (heterozygous familial and nonfamilial), mixed dyslipidemia and hypertriglyceridemia. Also indicated for homozygous familial hypercholesterolemia as an adjunct to other lipid-lowering therapies or when other such therapies are not available. Furthermore, it is used to slow the progression of atherosclerosis and for primary prevention of cardiovascular disease.
PharmacodynamicsRosuvastatin is a synthetic, enantiomerically pure antilipemic agent. It is used to lower total cholesterol, low density lipoprotein-cholesterol (LDL-C), apolipoprotein B (apoB), non-high density lipoprotein-cholesterol (non-HDL-C), and trigleride (TG) plasma concentrations while increasing HDL-C concentrations. High LDL-C, low HDL-C and high TG concentrations in the plasma are associated with increased risk of atherosclerosis and cardiovascular disease. The total cholesterol to HDL-C ratio is a strong predictor of coronary artery disease and high ratios are associated with higher risk of disease. Increased levels of HDL-C are associated with lower cardiovascular risk. By decreasing LDL-C and TG and increasing HDL-C, rosuvastatin reduces the risk of cardiovascular morbidity and mortality.
Mechanism of actionRosuvastatin is a competitive inhibitor of HMG-CoA reductase. HMG-CoA reductase catalyzes the conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol biosynthesis. Rosuvastatin acts primarily in the liver. Decreased hepatic cholesterol concentrations stimulate the upregulation of hepatic low density lipoprotein (LDL) receptors which increases hepatic uptake of LDL. Rosuvastatin also inhibits hepatic synthesis of very low density lipoprotein (VLDL). The overall effect is a decrease in plasma LDL and VLDL. In vitro and in vivo animal studies also demonstrate that rosuvastatin exerts vasculoprotective effects independent of its lipid-lowering properties. Rosuvastatin exerts an anti-inflammatory effect on rat mesenteric microvascular endothelium by attenuating leukocyte rolling, adherence and transmigration (PMID: 11375257). The drug also modulates nitric oxide synthase (NOS) expression and reduces ischemic-reperfusion injuries in rat hearts (PMID: 15914111). Rosuvastatin increases the bioavailability of nitric oxide (PMID: 11375257, 12031849, 15914111) by upregulating NOS (PMID: 12354446) and by increasing the stability of NOS through post-transcriptional polyadenylation (PMID: 17916773). It is unclear as to how rosuvastatin brings about these effects though they may be due to decreased concentrations of mevalonic acid.
Related Articles
AbsorptionBioavailability is approximately 20%. Peak plasma concentrations were reached 3 to 5 hours following oral dosing. Both Cmax and AUC increased in approximate proportion to CRESTOR dose. Food has no effect on the AUC of rosuvastatin.
Volume of distribution
  • 134 L [steady-state]
Protein binding88% bound to plasma proteins (mostly albumin). Binding is reversible and independent of plasma concentrations.
Metabolism

Not extensively metabolized. Only ~10% is excreted as metabolite. Cytochrome P450 (CYP) 2C9 is primarily responsible for the formation of rosuvastatin's major metabolite, N-desmethylrosuvastatin. N-desmethylrosuvastatin has approximately 50% of the pharmacological activity of its parent compound in vitro. Rosuvastatin clearance is not dependent on metabolism by cytochrome P450 3A4 to a clinically significant extent. Rosuvastatin accounts for greater than 90% of the pharmacologic action. Inhibitors of CYP2C9 increase the AUC by less than 2-fold. This interaction does not appear to be clinically significant.

SubstrateEnzymesProduct
Rosuvastatin
Rosuvastatin 5 S-lactoneDetails
Rosuvastatin
N-DesmethylrosuvastatinDetails
Route of eliminationRosuvastatin is not extensively metabolized; approximately 10% of a radiolabeled dose is recovered as metabolite. Following oral administration, rosuvastatin and its metabolites are primarily excreted in the feces (90%). After an intravenous dose, approximately 28% of total body clearance was via the renal route, and 72% by the hepatic route.
Half life19 hours
ClearanceNot Available
ToxicityGenerally well-tolerated. Side effects may include myalgia, constipation, asthenia, abdominal pain, and nausea. Other possible side effects include myotoxicity (myopathy, myositis, rhabdomyolysis) and hepatotoxicity. To avoid toxicity in Asian patients, lower doses should be considered. Pharmacokinetic studies show an approximately two-fold increase in peak plasma concentration and AUC in Asian patients (Philippino, Chinese, Japanese, Korean, Vietnamese, or Asian-Indian descent) compared to Caucasians patients.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Rosuvastatin Action PathwayDrug actionSMP00092
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
Kinesin-like protein KIF6
Gene symbol: KIF6
UniProt: Q6ZMV9
rs20455 Not AvailableC AlleleImproved response to statin drugs18222353
3-hydroxy-3-methylglutaryl-coenzyme A reductase
Gene symbol: HMGCR
UniProt: P04035
rs17244841 Not AvailableT AlleleReduced response to statin drugs15199031
ATP-binding cassette sub-family G member 2
Gene symbol: ABCG2
UniProt: Q9UNQ0
rs2231142 Not AvailableG > TGreater response to drug therapy20130569
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9791
Blood Brain Barrier-0.6815
Caco-2 permeable-0.5818
P-glycoprotein substrateNon-substrate0.6962
P-glycoprotein inhibitor INon-inhibitor0.5099
P-glycoprotein inhibitor IINon-inhibitor0.8987
Renal organic cation transporterNon-inhibitor0.9467
CYP450 2C9 substrateNon-substrate0.5544
CYP450 2D6 substrateNon-substrate0.8633
CYP450 3A4 substrateNon-substrate0.584
CYP450 1A2 substrateNon-inhibitor0.6896
CYP450 2C9 inhibitorNon-inhibitor0.5957
CYP450 2D6 inhibitorNon-inhibitor0.8609
CYP450 2C19 inhibitorNon-inhibitor0.6414
CYP450 3A4 inhibitorNon-inhibitor0.8308
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6226
Ames testNon AMES toxic0.662
CarcinogenicityNon-carcinogens0.6578
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.5599 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9856
hERG inhibition (predictor II)Non-inhibitor0.8117
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tablet, coatedoral10 mg/1
Tablet, coatedoral40 mg/1
Tablet, film coatedoral10 mg/1
Tablet, film coatedoral20 mg/1
Tablet, film coatedoral40 mg/1
Tablet, film coatedoral5 mg/1
Tabletoral10 mg
Tabletoral20 mg
Tabletoral40 mg
Tabletoral5 mg
Tabletoral10.0 mg
Tabletoral20.0 mg
Tabletoral40.0 mg
Tabletoral5.0 mg
Prices
Unit descriptionCostUnit
Crestor 40 mg tablet4.7USD tablet
Crestor 20 mg tablet4.69USD tablet
Crestor 10 mg tablet4.68USD tablet
Crestor 5 mg tablet4.68USD tablet
Crestor 40 mg Tablet2.24USD tablet
Crestor 20 mg Tablet1.91USD tablet
Crestor 10 mg Tablet1.53USD tablet
Crestor 5 mg Tablet1.45USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2072945 No2001-07-312012-07-02Canada
CA2315141 No2009-08-182020-08-04Canada
US6316460 Yes2001-02-042021-02-04Us
US6858618 Yes2002-06-172022-06-17Us
US7030152 Yes1998-10-022018-10-02Us
US7964614 Yes1998-10-022018-10-02Us
USRE37314 Yes1996-07-082016-07-08Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilitySparingly soluble in waterFDA label
logP0.13 FDA label
Predicted Properties
PropertyValueSource
Water Solubility0.0886 mg/mLALOGPS
logP1.47ALOGPS
logP1.92ChemAxon
logS-3.7ALOGPS
pKa (Strongest Acidic)4ChemAxon
pKa (Strongest Basic)-2.8ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area140.92 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity121.44 m3·mol-1ChemAxon
Polarizability48.55 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Valerie Niddam-Hildesheim, Greta Sterimbaum, “Process for preparation of rosuvastatin calcium.” U.S. Patent US20050080134, issued April 14, 2005.

US20050080134
General References
  1. Di Napoli P, Taccardi AA, Grilli A, De Lutiis MA, Barsotti A, Felaco M, De Caterina R: Chronic treatment with rosuvastatin modulates nitric oxide synthase expression and reduces ischemia-reperfusion injury in rat hearts. Cardiovasc Res. 2005 Jun 1;66(3):462-71. Epub 2005 Mar 2. [PubMed:15914111 ]
  2. Everett BM, Glynn RJ, MacFadyen JG, Ridker PM: Rosuvastatin in the prevention of stroke among men and women with elevated levels of C-reactive protein: justification for the Use of Statins in Prevention: an Intervention Trial Evaluating Rosuvastatin (JUPITER). Circulation. 2010 Jan 5;121(1):143-50. doi: 10.1161/CIRCULATIONAHA.109.874834. Epub 2009 Dec 21. [PubMed:20026779 ]
  3. Jones SP, Gibson MF, Rimmer DM 3rd, Gibson TM, Sharp BR, Lefer DJ: Direct vascular and cardioprotective effects of rosuvastatin, a new HMG-CoA reductase inhibitor. J Am Coll Cardiol. 2002 Sep 18;40(6):1172-8. [PubMed:12354446 ]
  4. Jones PH, Davidson MH, Stein EA, Bays HE, McKenney JM, Miller E, Cain VA, Blasetto JW: Comparison of the efficacy and safety of rosuvastatin versus atorvastatin, simvastatin, and pravastatin across doses (STELLAR* Trial). Am J Cardiol. 2003 Jul 15;92(2):152-60. [PubMed:12860216 ]
  5. Kilic E, Kilic U, Matter CM, Luscher TF, Bassetti CL, Hermann DM: Aggravation of focal cerebral ischemia by tissue plasminogen activator is reversed by 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor but does not depend on endothelial NO synthase. Stroke. 2005 Feb;36(2):332-6. Epub 2004 Dec 29. [PubMed:15625301 ]
  6. Kosmidou I, Moore JP, Weber M, Searles CD: Statin treatment and 3' polyadenylation of eNOS mRNA. Arterioscler Thromb Vasc Biol. 2007 Dec;27(12):2642-9. Epub 2007 Oct 4. [PubMed:17916773 ]
  7. Laufs U, Gertz K, Dirnagl U, Bohm M, Nickenig G, Endres M: Rosuvastatin, a new HMG-CoA reductase inhibitor, upregulates endothelial nitric oxide synthase and protects from ischemic stroke in mice. Brain Res. 2002 Jun 28;942(1-2):23-30. [PubMed:12031849 ]
  8. McKillop T: The statin wars. Lancet. 2003 Nov 1;362(9394):1498. [PubMed:14602449 ]
  9. McTaggart F, Buckett L, Davidson R, Holdgate G, McCormick A, Schneck D, Smith G, Warwick M: Preclinical and clinical pharmacology of Rosuvastatin, a new 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor. Am J Cardiol. 2001 Mar 8;87(5A):28B-32B. [PubMed:11256847 ]
  10. Nissen SE, Nicholls SJ, Sipahi I, Libby P, Raichlen JS, Ballantyne CM, Davignon J, Erbel R, Fruchart JC, Tardif JC, Schoenhagen P, Crowe T, Cain V, Wolski K, Goormastic M, Tuzcu EM: Effect of very high-intensity statin therapy on regression of coronary atherosclerosis: the ASTEROID trial. JAMA. 2006 Apr 5;295(13):1556-65. Epub 2006 Mar 13. [PubMed:16533939 ]
  11. Stalker TJ, Lefer AM, Scalia R: A new HMG-CoA reductase inhibitor, rosuvastatin, exerts anti-inflammatory effects on the microvascular endothelium: the role of mevalonic acid. Br J Pharmacol. 2001 Jun;133(3):406-12. [PubMed:11375257 ]
  12. Authors unspecified: The statin wars: why AstraZeneca must retreat. Lancet. 2003 Oct 25;362(9393):1341. [PubMed:14585629 ]
  13. Ho RH, Tirona RG, Leake BF, Glaeser H, Lee W, Lemke CJ, Wang Y, Kim RB: Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics. Gastroenterology. 2006 May;130(6):1793-806. Epub 2006 Mar 6. [PubMed:16697742 ]
External Links
ATC CodesC10AA07C10BA06C10BX05C10BX07C10BX09C10BX10
AHFS Codes
  • 24:06.08
PDB EntriesNot Available
FDA labelDownload (270 KB)
MSDSDownload (57.8 KB)
Interactions
Drug Interactions
Drug
AcipimoxAcipimox may increase the myopathic rhabdomyolysis activities of Rosuvastatin.
Aluminum hydroxideThe serum concentration of Rosuvastatin can be decreased when it is combined with Aluminum hydroxide.
AmiodaroneThe metabolism of Rosuvastatin can be decreased when combined with Amiodarone.
AtazanavirThe serum concentration of Rosuvastatin can be increased when it is combined with Atazanavir.
BatimastatThe serum concentration of Rosuvastatin can be increased when it is combined with Batimastat.
BezafibrateBezafibrate may increase the myopathic rhabdomyolysis activities of Rosuvastatin.
BoceprevirThe serum concentration of Rosuvastatin can be increased when it is combined with Boceprevir.
Calcium carbonateThe serum concentration of Rosuvastatin can be decreased when it is combined with Calcium carbonate.
CiprofibrateThe risk or severity of adverse effects can be increased when Ciprofibrate is combined with Rosuvastatin.
ClopidogrelThe serum concentration of Rosuvastatin can be increased when it is combined with Clopidogrel.
ColchicineColchicine may increase the myopathic rhabdomyolysis activities of Rosuvastatin.
CyclosporineThe serum concentration of Rosuvastatin can be increased when it is combined with Cyclosporine.
DaclatasvirThe serum concentration of Rosuvastatin can be increased when it is combined with Daclatasvir.
DaptomycinThe risk or severity of adverse effects can be increased when Rosuvastatin is combined with Daptomycin.
DarunavirThe serum concentration of Rosuvastatin can be increased when it is combined with Darunavir.
DicoumarolRosuvastatin may increase the anticoagulant activities of Dicoumarol.
DronedaroneThe serum concentration of Rosuvastatin can be increased when it is combined with Dronedarone.
EltrombopagThe serum concentration of Rosuvastatin can be increased when it is combined with Eltrombopag.
EluxadolineThe serum concentration of Rosuvastatin can be increased when it is combined with Eluxadoline.
Eslicarbazepine acetateThe serum concentration of Rosuvastatin can be decreased when it is combined with Eslicarbazepine acetate.
FenofibrateThe risk or severity of adverse effects can be increased when Fenofibrate is combined with Rosuvastatin.
FosamprenavirThe serum concentration of Rosuvastatin can be increased when it is combined with Fosamprenavir.
Fusidic AcidThe risk or severity of adverse effects can be increased when Fusidic Acid is combined with Rosuvastatin.
GemfibrozilGemfibrozil may increase the myopathic rhabdomyolysis activities of Rosuvastatin.
IndinavirThe serum concentration of Rosuvastatin can be increased when it is combined with Indinavir.
IsoflurophateThe serum concentration of Rosuvastatin can be increased when it is combined with Isoflurophate.
ItraconazoleThe serum concentration of Rosuvastatin can be increased when it is combined with Itraconazole.
LanthanumThe serum concentration of Lanthanum can be decreased when it is combined with Rosuvastatin.
LedipasvirThe serum concentration of Rosuvastatin can be increased when it is combined with Ledipasvir.
Magnesium oxideThe serum concentration of Rosuvastatin can be decreased when it is combined with Magnesium oxide.
NelfinavirThe serum concentration of Rosuvastatin can be increased when it is combined with Nelfinavir.
NiacinThe risk or severity of adverse effects can be increased when Niacin is combined with Rosuvastatin.
NicotinamideThe risk or severity of adverse effects can be increased when Nicotinamide is combined with Rosuvastatin.
PazopanibRosuvastatin may increase the hepatotoxic activities of Pazopanib.
RaltegravirRaltegravir may increase the myopathic rhabdomyolysis activities of Rosuvastatin.
RitonavirThe serum concentration of Rosuvastatin can be increased when it is combined with Ritonavir.
RolapitantThe serum concentration of Rosuvastatin can be increased when it is combined with Rolapitant.
SaquinavirThe serum concentration of Rosuvastatin can be increased when it is combined with Saquinavir.
SimeprevirThe serum concentration of Rosuvastatin can be increased when it is combined with Simeprevir.
TelaprevirThe serum concentration of Rosuvastatin can be increased when it is combined with Telaprevir.
TeriflunomideThe serum concentration of Rosuvastatin can be increased when it is combined with Teriflunomide.
TipranavirThe serum concentration of Rosuvastatin can be increased when it is combined with Tipranavir.
TrabectedinRosuvastatin may increase the myopathic rhabdomyolysis activities of Trabectedin.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Nadph binding
Specific Function:
Transmembrane glycoprotein that is the rate-limiting enzyme in cholesterol biosynthesis as well as in the biosynthesis of nonsterol isoprenoids that are essential for normal cell function including ubiquinone and geranylgeranyl proteins.
Gene Name:
HMGCR
Uniprot ID:
P04035
Molecular Weight:
97475.155 Da
References
  1. Carbonell T, Freire E: Binding thermodynamics of statins to HMG-CoA reductase. Biochemistry. 2005 Sep 6;44(35):11741-8. [PubMed:16128575 ]
  2. Chapman MJ, Caslake M, Packard C, McTaggart F: New dimension of statin action on ApoB atherogenicity. Clin Cardiol. 2003 Jan;26(1 Suppl 1):I7-10. [PubMed:12539816 ]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  4. Davidson MH: Rosuvastatin: a highly efficacious statin for the treatment of dyslipidaemia. Expert Opin Investig Drugs. 2002 Jan;11(1):125-41. [PubMed:11772327 ]
  5. Hanefeld M: Clinical rationale for rosuvastatin, a potent new HMG-CoA reductase inhibitor. Int J Clin Pract. 2001 Jul-Aug;55(6):399-405. [PubMed:11501230 ]
  6. Holdgate GA, Ward WH, McTaggart F: Molecular mechanism for inhibition of 3-hydroxy-3-methylglutaryl CoA (HMG-CoA) reductase by rosuvastatin. Biochem Soc Trans. 2003 Jun;31(Pt 3):528-31. [PubMed:12773150 ]
  7. McTaggart F, Buckett L, Davidson R, Holdgate G, McCormick A, Schneck D, Smith G, Warwick M: Preclinical and clinical pharmacology of Rosuvastatin, a new 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor. Am J Cardiol. 2001 Mar 8;87(5A):28B-32B. [PubMed:11256847 ]
  8. Olsson AG, McTaggart F, Raza A: Rosuvastatin: a highly effective new HMG-CoA reductase inhibitor. Cardiovasc Drug Rev. 2002 Winter;20(4):303-28. [PubMed:12481202 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Olsson AG, McTaggart F, Raza A: Rosuvastatin: a highly effective new HMG-CoA reductase inhibitor. Cardiovasc Drug Rev. 2002 Winter;20(4):303-28. [PubMed:12481202 ]
  2. Neuvonen PJ, Niemi M, Backman JT: Drug interactions with lipid-lowering drugs: mechanisms and clinical relevance. Clin Pharmacol Ther. 2006 Dec;80(6):565-81. [PubMed:17178259 ]
  3. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  4. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Transporter activity
Specific Function:
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotrexate, antiviral drugs and other xenobiotics. Confers resistance to anticancer drugs. Hydrolyzes ATP with low efficiency.
Gene Name:
ABCC1
Uniprot ID:
P33527
Molecular Weight:
171589.5 Da
References
  1. Knauer MJ, Urquhart BL, Meyer zu Schwabedissen HE, Schwarz UI, Lemke CJ, Leake BF, Kim RB, Tirona RG: Human skeletal muscle drug transporters determine local exposure and toxicity of statins. Circ Res. 2010 Feb 5;106(2):297-306. doi: 10.1161/CIRCRESAHA.109.203596. Epub 2009 Nov 25. [PubMed:19940267 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Atpase activity, coupled to transmembrane movement of substances
Specific Function:
May be an organic anion pump relevant to cellular detoxification.
Gene Name:
ABCC4
Uniprot ID:
O15439
Molecular Weight:
149525.33 Da
References
  1. Knauer MJ, Urquhart BL, Meyer zu Schwabedissen HE, Schwarz UI, Lemke CJ, Leake BF, Kim RB, Tirona RG: Human skeletal muscle drug transporters determine local exposure and toxicity of statins. Circ Res. 2010 Feb 5;106(2):297-306. doi: 10.1161/CIRCRESAHA.109.203596. Epub 2009 Nov 25. [PubMed:19940267 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibited by the grapefruit juice component naringin.
Gene Name:
SLCO1A2
Uniprot ID:
P46721
Molecular Weight:
74144.105 Da
References
  1. Ho RH, Tirona RG, Leake BF, Glaeser H, Lee W, Lemke CJ, Wang Y, Kim RB: Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics. Gastroenterology. 2006 May;130(6):1793-806. Epub 2006 Mar 6. [PubMed:16697742 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
Molecular Weight:
76447.99 Da
References
  1. van de Steeg E, Greupink R, Schreurs M, Nooijen IH, Verhoeckx KC, Hanemaaijer R, Ripken D, Monshouwer M, Vlaming ML, DeGroot J, Verwei M, Russel FG, Huisman MT, Wortelboer HM: Drug-drug interactions between rosuvastatin and oral antidiabetic drugs occurring at the level of OATP1B1. Drug Metab Dispos. 2013 Mar;41(3):592-601. doi: 10.1124/dmd.112.049023. Epub 2012 Dec 17. [PubMed:23248200 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP). Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B3
Uniprot ID:
Q9NPD5
Molecular Weight:
77402.175 Da
References
  1. Ho RH, Tirona RG, Leake BF, Glaeser H, Lee W, Lemke CJ, Wang Y, Kim RB: Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics. Gastroenterology. 2006 May;130(6):1793-806. Epub 2006 Mar 6. [PubMed:16697742 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
Gene Name:
SLCO2B1
Uniprot ID:
O94956
Molecular Weight:
76709.98 Da
References
  1. Ho RH, Tirona RG, Leake BF, Glaeser H, Lee W, Lemke CJ, Wang Y, Kim RB: Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics. Gastroenterology. 2006 May;130(6):1793-806. Epub 2006 Mar 6. [PubMed:16697742 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Cystine:glutamate antiporter activity
Specific Function:
Sodium-independent, high-affinity exchange of anionic amino acids with high specificity for anionic form of cystine and glutamate.
Gene Name:
SLC7A11
Uniprot ID:
Q9UPY5
Molecular Weight:
55422.44 Da
References
  1. Ho RH, Tirona RG, Leake BF, Glaeser H, Lee W, Lemke CJ, Wang Y, Kim RB: Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics. Gastroenterology. 2006 May;130(6):1793-806. Epub 2006 Mar 6. [PubMed:16697742 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Transporter activity
Specific Function:
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name:
ABCB11
Uniprot ID:
O95342
Molecular Weight:
146405.83 Da
References
  1. Jemnitz K, Veres Z, Tugyi R, Vereczkey L: Biliary efflux transporters involved in the clearance of rosuvastatin in sandwich culture of primary rat hepatocytes. Toxicol In Vitro. 2010 Mar;24(2):605-10. doi: 10.1016/j.tiv.2009.10.009. Epub 2009 Oct 21. [PubMed:19853032 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
Comments
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Drug created on June 13, 2005 07:24 / Updated on July 27, 2016 03:12