Identification

Logo pink
Are you a
new drug developer?
Contact us to learn more about our customized products and solutions.
Logo pink
Stay in the know!
As part of our commitment to providing the most up-to-date drug information, we will be releasing #DrugBankUpdates with our newly added curated drug pages.
#DrugBankUpdates
Name
Rosuvastatin
Accession Number
DB01098  (APRD00546)
Type
Small Molecule
Groups
Approved
Description

Rosuvastatin, also known as the brand name product Crestor, is a lipid-lowering drug that belongs to the statin class of medications, which are used to lower the risk of cardiovascular disease and manage abnormal lipid levels by inhibiting the endogenous production of cholesterol in the liver. More specifically, statin medications competitively inhibit the enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) Reductase,24 which catalyzes the conversion of HMG-CoA to mevalonic acid and is the third step in a sequence of metabolic reactions involved in the production of several compounds involved in lipid metabolism and transport including cholesterol, low-density lipoprotein (LDL) (sometimes referred to as "bad cholesterol"), and very low-density lipoprotein (VLDL). Prescribing of statin medications is considered standard practice following any cardiovascular events and for people with a moderate to high risk of development of CVD, such as those with Type 2 Diabetes. The clear evidence of the benefit of statin use coupled with very minimal side effects or long term effects has resulted in this class becoming one of the most widely prescribed medications in North America.15,21

Rosuvastatin and other drugs from the statin class of medications including atorvastatin, pravastatin, simvastatin, fluvastatin, and lovastatin are considered first-line options for the treatment of dyslipidemia.15,21 This is largely due to the fact that cardiovascular disease (CVD), which includes heart attack, atherosclerosis, angina, peripheral artery disease, and stroke, has become a leading cause of death in high-income countries and a major cause of morbidity around the world.14 Elevated cholesterol levels, and in particular, elevated low-density lipoprotein (LDL) levels, are an important risk factor for the development of CVD.15,38 Use of statins to target and reduce LDL levels has been shown in a number of landmark studies to significantly reduce the risk of development of CVD and all-cause mortality.16,17,18,26,31 Statins are considered a cost-effective treatment option for CVD due to their evidence of reducing all-cause mortality including fatal and non-fatal CVD as well as the need for surgical revascularization or angioplasty following a heart attack.15,21 Evidence has shown that even for low-risk individuals (with <10% risk of a major vascular event occurring within 5 years) statins cause a 20%-22% relative reduction in major cardiovascular events (heart attack, stroke, coronary revascularization, and coronary death) for every 1 mmol/L reduction in LDL without any significant side effects or risks.19,20

While all statin medications are considered equally effective from a clinical standpoint, rosuvastatin is considered the most potent; doses of 10 to 40mg rosuvastatin per day were found in clinical studies to result in a 45.8% to 54.6% decreases in LDL cholesterol levels, which is about three-fold more potent than atorvastatin's effects on LDL cholesterol.22,4 However, the results of the SATURN trial26 concluded that despite this difference in potency, there was no difference in their effect on the progression of coronary atherosclerosis.

Rosuvastatin is also a unique member of the class of statins due to its high hydrophilicity which increases hepatic uptake at the site of action, low bioavailability, and minimal metabolism via the Cytochrome P450 system.37 This last point results in less risk of drug-drug interactions compared to atorvastatin, lovastatin, and simvastatin, which are all extensively metabolized by Cytochrome P450 (CYP) 3A4, an enzyme involved in the metabolism of many commonly used drugs.29 Drugs such as ciclosporin, gemfibrozil, and some antiretrovirals are more likely to interact with this statin through antagonism of OATP1B1 organic anion transporter protein 1B1-mediated hepatic uptake of rosuvastatin.42,43

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
  • Rosuvastatin
  • Rosuvastatina
External IDs
ZD-4522 / ZD4522
Product Ingredients
IngredientUNIICASInChI Key
Rosuvastatin calcium83MVU38M7Q147098-20-2LALFOYNTGMUKGG-JGMJEEPBSA-L
Rosuvastatin zinc70VE4E19Z7953412-08-3KUQHZGJLQWUFPU-BGRFNVSISA-L
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act RosuvastatinTabletOralActavis Pharma Company2012-03-162019-07-09Canada
Act RosuvastatinTabletOralActavis Pharma Company2012-03-162019-07-09Canada
Act RosuvastatinTabletOralActavis Pharma Company2012-03-162019-07-09Canada
Act RosuvastatinTabletOralActavis Pharma Company2012-03-162019-07-09Canada
CrestorTablet, film coated10 mg/1OralRebel Distributors2003-11-25Not applicableUs
CrestorTablet, film coated10 mg/1OralPhysicians Total Care, Inc.2003-11-25Not applicableUs54868 496320180907 15195 1lbd1dh
CrestorTablet, film coated40 mg/1OralCardinal Health2010-12-012018-08-31Us55154 692520180913 8702 zm4pzq
CrestorTablet, film coated40 mg/1OralRebel Distributors2004-11-01Not applicableUs
CrestorTablet, film coated10 mg/1OralLake Erie Medical Dba Quality Care Produts Llc2010-11-092014-12-31Us
CrestorTablet, film coated5 mg/1OralA S Medication Solutions2005-10-26Not applicableUs54569 574620180819 11162 vjajp6
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ach-rosuvastatinTabletOralAccord Healthcare Inc2019-05-23Not applicableCanada
Ach-rosuvastatinTabletOralAccord Healthcare Inc2019-05-23Not applicableCanada
Ach-rosuvastatinTabletOralAccord Healthcare Inc2019-05-23Not applicableCanada
Ach-rosuvastatinTabletOralAccord Healthcare Inc2019-05-23Not applicableCanada
Ag-rosuvastatinTabletOralAngita Pharma Inc.2018-12-28Not applicableCanada
Ag-rosuvastatinTabletOralAngita Pharma Inc.2018-12-28Not applicableCanada
Ag-rosuvastatinTabletOralAngita Pharma Inc.2018-12-28Not applicableCanada
Ag-rosuvastatinTabletOralAngita Pharma Inc.2018-12-28Not applicableCanada
Apo-rosuvastatinTabletOralApotex Corporation2012-04-02Not applicableCanada
Apo-rosuvastatinTabletOralApotex Corporation2012-04-02Not applicableCanada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
International/Other Brands
Astende (Lazar (Argentina)) / Cirantan (AstraZeneca (Netherlands)) / Cresadex (Drugtech (Chile)) / Provisacor (AstraZeneca (Italy, Netherlands) ) / Razel (Glenmark (India)) / Rosedex (Roux-Ocefa (Argentina)) / Rosimol (Sandoz (Argentina)) / Rosumed (Labomed (Chile)) / Rosustatin (Montpellier (Argentina)) / Rosuvas (Ranbaxy (India)) / Rosuvast (Bago (Argentina)) / Rosvel (Laboratorios Chile (Chile)) / Rovartal (Roemmers (Argentina)) / Simestat (Simesa (Italy)) / Sinlip (Gador (Argentina)) / Visacor (AstraZeneca (Portugal)) / Vivacor (AstraZeneca (Brazil))
Categories
UNII
413KH5ZJ73
CAS number
287714-41-4
Weight
Average: 481.538
Monoisotopic: 481.168284538
Chemical Formula
C22H28FN3O6S
InChI Key
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

Pharmacology

Indication

The FDA monograph states that rosuvastatin is indicated as an adjunct to diet in the treatment of triglyceridemia, Primary Dysbetalipoproteinemia (Type III Hyperlipoproteinemia), and Homozygous Familial Hypercholesterolemia.42

The Health Canada monograph for rosuvastatin further specifies that rosuvastatin is indicated for the reduction of elevated total cholesterol (Total-C), LDL-C, ApoB, the Total-C/HDL-C ratio and triglycerides (TG) and for increasing HDL-C in hyperlipidemic and dyslipidemic conditions when response to diet and exercise alone has been inadequate. It is also indicated for the prevention of major cardiovascular events (including risk of myocardial infarction, nonfatal stroke, and coronary artery revascularization) in adult patients without documented history of cardiovascular or cerebrovascular events, but with at least two conventional risk factors for cardiovascular disease.43

Prescribing of statin medications is considered standard practice following any cardiovascular events and for people with a moderate to high risk of development of CVD. Statin-indicated conditions include diabetes mellitus, clinical atherosclerosis (including myocardial infarction, acute coronary syndromes, stable angina, documented coronary artery disease, stroke, trans ischemic attack (TIA), documented carotid disease, peripheral artery disease, and claudication), abdominal aortic aneurysm, chronic kidney disease, and severely elevated LDL-C levels.15,21

Associated Conditions
Pharmacodynamics

Rosuvastatin 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.15,21

Elevated cholesterol levels, and in particular, elevated low-density lipoprotein (LDL) levels, are an important risk factor for the development of CVD.15 Use of statins to target and reduce LDL levels has been shown in a number of landmark studies to significantly reduce the risk of development of CVD and all-cause mortality.16,17,18,26,31 Statins are considered a cost-effective treatment option for CVD due to their evidence of reducing all-cause mortality including fatal and non-fatal CVD as well as the need for surgical revascularization or angioplasty following a heart attack.15,21 Evidence has shown that even for low-risk individuals (with <10% risk of a major vascular event occurring within 5 years) statins cause a 20%-22% relative reduction in major cardiovascular events (heart attack, stroke, coronary revascularization, and coronary death) for every 1 mmol/L reduction in LDL without any significant side effects or risks.19,20

Skeletal Muscle Effects

Cases of myopathy and rhabdomyolysis with acute renal failure secondary to myoglobinuria have been reported with HMG-CoA reductase inhibitors, including rosuvastatin. These risks can occur at any dose level, but are increased at the highest dose (40 mg). Rosuvastatin should be prescribed with caution in patients with predisposing factors for myopathy (e.g., age ≥ 65 years, inadequately treated hypothyroidism, renal impairment).

The risk of myopathy during treatment with rosuvastatin may be increased with concurrent administration of some other lipid-lowering therapies (such as fenofibrate or niacin), gemfibrozil, cyclosporine, atazanavir/ritonavir, lopinavir/ritonavir, or simeprevir. Cases of myopathy, including rhabdomyolysis, have been reported with HMG-CoA reductase inhibitors, including rosuvastatin, coadministered with colchicine, and caution should therefore be exercised when prescribing these two medications together.42

Real-world data from observational studies has suggested that 10-15% of people taking statins may experience muscle aches at some point during treatment.41

Liver Enzyme Abnormalities

Increases in serum transaminases have been reported with HMG-CoA reductase inhibitors, including rosuvastatin. In most cases, the elevations were transient and resolved or improved on continued therapy or after a brief interruption in therapy. There were two cases of jaundice, for which a relationship to rosuvastatin therapy could not be determined, which resolved after discontinuation of therapy. There were no cases of liver failure or irreversible liver disease in these trials.42

Endocrine Effects

Increases in HbA1c and fasting serum glucose levels have been reported with HMG-CoA reductase inhibitors, including rosuvastatin calcium tablets. Based on clinical trial data with rosuvastatin, in some instances these increases may exceed the threshold for the diagnosis of diabetes mellitus.42

An in vitro study found that atorvastatin, pravastatin, rosuvastatin, and pitavastatin exhibited a dose-dependent cytotoxic effect on human pancreas islet β cells, with reductions in cell viability of 32, 41, 34 and 29%, respectively, versus control]. Moreover, insulin secretion rates were decreased by 34, 30, 27 and 19%, respectively, relative to control.40

HMG-CoA reductase inhibitors interfere with cholesterol synthesis and lower cholesterol levels and, as such, might theoretically blunt adrenal or gonadal steroid hormone production. Rosuvastatin demonstrated no effect upon nonstimulated cortisol levels and no effect on thyroid metabolism as assessed by TSH plasma concentration. In rosuvastatin treated patients, there was no impairment of adrenocortical reserve and no reduction in plasma cortisol concentrations. Clinical studies with other HMG-CoA reductase inhibitors have suggested that these agents do not reduce plasma testosterone concentration. The effects of HMG-CoA reductase inhibitors on male fertility have not been studied. The effects, if any, on the pituitarygonadal axis in premenopausal women are unknown.43

Cardiovascular

Ubiquinone levels were not measured in rosuvastatin clinical trials, however significant decreases in circulating ubiquinone levels in patients treated with other statins have been observed. The clinical significance of a potential long-term statin-induced deficiency of ubiquinone has not been established. It has been reported that a decrease in myocardial ubiquinone levels could lead to impaired cardiac function in patients with borderline congestive heart failure.43

Lipoprotein A

In some patients, the beneficial effect of lowered total cholesterol and LDL-C levels may be partly blunted by a concomitant increase in the Lipoprotein(a) [Lp(a)] concentrations. Present knowledge suggests the importance of high Lp(a) levels as an emerging risk factor for coronary heart disease. It is thus desirable to maintain and reinforce lifestyle changes in high-risk patients placed on rosuvastatin therapy.43 Further studies have demonstrated statins affect Lp(a) levels differently in patients with dyslipidemia depending on their apo(a) phenotype; statins increase Lp(a) levels exclusively in patients with the low molecular weight apo(a) phenotype.23

Mechanism of action

Rosuvastatin is a statin medication and a competitive inhibitor of the enzyme HMG-CoA (3-hydroxy-3-methylglutaryl coenzyme A) reductase, which catalyzes the conversion of HMG-CoA to mevalonate, an early rate-limiting step in cholesterol biosynthesis.24 Rosuvastatin acts primarily in the liver, where 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).42 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, also known as the pleiotropic effects of statins.25 This includes improvement in endothelial function, enhanced stability of atherosclerotic plaques, reduced oxidative stress and inflammation, and inhibition of the thrombogenic response.

Statins have also been found to bind allosterically to β2 integrin function-associated antigen-1 (LFA-1), which plays an important role in leukocyte trafficking and in T cell activation.39

Rosuvastatin exerts an anti-inflammatory effect on rat mesenteric microvascular endothelium by attenuating leukocyte rolling, adherence and transmigration.11 The drug also modulates nitric oxide synthase (NOS) expression and reduces ischemic-reperfusion injuries in rat hearts.1 Rosuvastatin increases the bioavailability of nitric oxide11,7,1 by upregulating NOS3 and by increasing the stability of NOS through post-transcriptional polyadenylation.6 It is unclear as to how rosuvastatin brings about these effects though they may be due to decreased concentrations of mevalonic acid.

TargetActionsOrganism
A3-hydroxy-3-methylglutaryl-coenzyme A reductase
inhibitor
Humans
UIntegrin alpha-L
inhibitory allosteric modulator
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

Learn more
Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

Learn more
Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

Learn more
Absorption

In a study of healthy white male volunteers, the absolute oral bioavailability of rosuvastatin was found to be approximately 20% while absorption was estimated to be 50%, which is consistent with a substantial first-pass effect after oral dosing.27,28 Another study in healthy volunteers found that the peak plasma concentration (Cmax) of rosuvastatin was 6.06ng/mL and was reached at a median of 5 hours following oral dosing.30 Both Cmax and AUC increased in approximate proportion to dose. Neither food nor evening versus morning administration was shown to have an effect on the AUC of rosuvastatin.42,43 Many statins are known to interact with hepatic uptake transporters and thus reach high concentrations at their site of action in the liver.

Breast Cancer Resistance Protein (BCRP) is a membrane-bound protein that plays an important role in the absorption of rosuvastatin, particularly as CYP3A4 has minimal involvement in its metabolism.29 Evidence from pharmacogenetic studies of c.421C>A single nucleotide polymorphisms (SNPs) in the gene for BCRP has demonstrated that individuals with the 421AA genotype have reduced functional activity and 2.4-fold higher AUC and Cmax values for rosuvastatin compared to study individuals with the control 421CC genotype. This has important implications for the variation in response to the drug in terms of efficacy and toxicity, particularly as the BCRP c.421C>A polymorphism occurs more frequently in Asian populations than in Caucasians.32,33 Other statin drugs impacted by this polymorphism include fluvastatin and atorvastatin.32

Genetic differences in the OATP1B1 (organic-anion-transporting polypeptide 1B1) hepatic transporter have also been shown to impact rosuvastatin pharmacokinetics. Evidence from pharmacogenetic studies of the c.521T>C SNP showed that rosuvastatin AUC was increased 1.62-fold for individuals homozygous for 521CC compared to homozygous 521TT individuals.36 Other statin drugs impacted by this polymorphism include simvastatin, pitavastatin, atorvastatin, and pravastatin.29

For patients known to have the above-mentioned c.421AA BCRP or c.521CC OATP1B1 genotypes, a maximum daily dose of 20mg of rosuvastatin is recommended to avoid adverse effects from the increased exposure to the drug, such as muscle pain and risk of rhabdomyolysis.43

Volume of distribution

Rosuvastatin undergoes first-pass extraction in the liver, which is the primary site of cholesterol synthesis and LDL-C clearance. The mean volume of distribution at steady-state of rosuvastatin is approximately 134 litres.42,43

Protein binding

Rosuvastatin is 88% bound to plasma proteins, mostly albumin. This binding is reversible and independent of plasma concentrations.42,43

Metabolism

Rosuvastatin is not extensively metabolized, as demonstrated by the small amount of radiolabeled dose that is recovered as a metabolite (~10%). Cytochrome P450 (CYP) 2C9 is primarily responsible for the formation of rosuvastatin's major metabolite, N-desmethylrosuvastatin, which has approximately 20-50% of the pharmacological activity of its parent compound in vitro.42,43 However, this metabolic pathway isn't deemed to be clinically significant as there were no observable effects found on rosuvastatin pharmacokinetics when rosuvastatin was coadministered with fluconazole, a potent CYP2C9 inhibitor.34

In vitro and in vivo data indicate that rosuvastatin has no clinically significant cytochrome P450 interactions (as substrate, inhibitor or inducer). Consequently, there is little potential for drug-drug interactions upon coadministration with agents that are metabolized by cytochrome P450.43

Route of elimination

Rosuvastatin 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.42,43,27

A study in healthy adult male volunteers found that approximately 90% of the rosuvastatin dose was recovered in feces within 72 hours after dose, while the remaining 10% was recovered in urine. The drug was completely excreted from the body after 10 days of dosing. They also found that approximately 76.8% of the excreted dose was unchanged from the parent compound, with the remaining dose recovered as the metabolites n-desmethyl rosuvastatin and rosuvastatin-5S-lactone.30

Renal tubular secretion is responsible for >90% of total renal clearance, and is believed to be mediated primarily by the uptake transporter OAT3 (Organic anion transporter 1), while OAT1 had minimal involvement.35

Half life

The elimination half-life (t½) of rosuvastatin is approximately 19 hours and does not increase with increasing doses.42,43

Clearance
Not Available
Toxicity

Generally 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 Caucasian patients.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Rosuvastatin Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Kinesin-like protein KIF6---(C;C) / (C;T)C AlleleEffect Directly StudiedPatients with this genotype have a greater reduction in risk of a major cardiovascular event with high dose rosuvastatin.Details
3-hydroxy-3-methylglutaryl-coenzyme A reductase---(A;T)T AlleleEffect Directly StudiedPatients with this genotype have a lesser reduction in LDL cholesterol with rosuvastatin.Details
ATP-binding cassette sub-family G member 2---(A;A) / (A;C)G > TEffect Directly StudiedPatients with this genotype have a greater reduction in LDL cholesterol with rosuvastatin.Details

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
2,4-thiazolidinedioneThe therapeutic efficacy of 2,4-thiazolidinedione can be increased when used in combination with Rosuvastatin.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Rosuvastatin.
6-Deoxyerythronolide BThe metabolism of Rosuvastatin can be decreased when combined with 6-Deoxyerythronolide B.
7-ethyl-10-hydroxycamptothecinThe metabolism of Rosuvastatin can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
9-aminocamptothecinThe metabolism of 9-aminocamptothecin can be decreased when combined with Rosuvastatin.
AbataceptThe metabolism of Rosuvastatin can be increased when combined with Abatacept.
AbemaciclibAbemaciclib may decrease the excretion rate of Rosuvastatin which could result in a higher serum level.
AbirateroneThe metabolism of Rosuvastatin can be decreased when combined with Abiraterone.
AcalabrutinibThe metabolism of Rosuvastatin can be decreased when combined with Acalabrutinib.
AcarboseThe therapeutic efficacy of Acarbose can be increased when used in combination with Rosuvastatin.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

    Learn more
  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

    Learn more
  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

    Learn more
Food Interactions
Not 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]
  14. Kreatsoulas C, Anand SS: The impact of social determinants on cardiovascular disease. Can J Cardiol. 2010 Aug-Sep;26 Suppl C:8C-13C. doi: 10.1016/s0828-282x(10)71075-8. [PubMed:20847985]
  15. Anderson TJ, Gregoire J, Pearson GJ, Barry AR, Couture P, Dawes M, Francis GA, Genest J Jr, Grover S, Gupta M, Hegele RA, Lau DC, Leiter LA, Lonn E, Mancini GB, McPherson R, Ngui D, Poirier P, Sievenpiper JL, Stone JA, Thanassoulis G, Ward R: 2016 Canadian Cardiovascular Society Guidelines for the Management of Dyslipidemia for the Prevention of Cardiovascular Disease in the Adult. Can J Cardiol. 2016 Nov;32(11):1263-1282. doi: 10.1016/j.cjca.2016.07.510. Epub 2016 Jul 25. [PubMed:27712954]
  16. Authors unspecified: Prevention of cardiovascular events and death with pravastatin in patients with coronary heart disease and a broad range of initial cholesterol levels. N Engl J Med. 1998 Nov 5;339(19):1349-57. doi: 10.1056/NEJM199811053391902. [PubMed:9841303]
  17. Cannon CP, Braunwald E, McCabe CH, Rader DJ, Rouleau JL, Belder R, Joyal SV, Hill KA, Pfeffer MA, Skene AM: Intensive versus moderate lipid lowering with statins after acute coronary syndromes. N Engl J Med. 2004 Apr 8;350(15):1495-504. doi: 10.1056/NEJMoa040583. Epub 2004 Mar 8. [PubMed:15007110]
  18. Ridker PM, Danielson E, Fonseca FA, Genest J, Gotto AM Jr, Kastelein JJ, Koenig W, Libby P, Lorenzatti AJ, MacFadyen JG, Nordestgaard BG, Shepherd J, Willerson JT, Glynn RJ: Rosuvastatin to prevent vascular events in men and women with elevated C-reactive protein. N Engl J Med. 2008 Nov 20;359(21):2195-207. doi: 10.1056/NEJMoa0807646. Epub 2008 Nov 9. [PubMed:18997196]
  19. Mihaylova B, Emberson J, Blackwell L, Keech A, Simes J, Barnes EH, Voysey M, Gray A, Collins R, Baigent C: The effects of lowering LDL cholesterol with statin therapy in people at low risk of vascular disease: meta-analysis of individual data from 27 randomised trials. Lancet. 2012 Aug 11;380(9841):581-90. doi: 10.1016/S0140-6736(12)60367-5. Epub 2012 May 17. [PubMed:22607822]
  20. Taylor F, Huffman MD, Macedo AF, Moore TH, Burke M, Davey Smith G, Ward K, Ebrahim S: Statins for the primary prevention of cardiovascular disease. Cochrane Database Syst Rev. 2013 Jan 31;(1):CD004816. doi: 10.1002/14651858.CD004816.pub5. [PubMed:23440795]
  21. Grundy SM, Stone NJ: 2018 American Heart Association/American College of Cardiology Multisociety Guideline on the Management of Blood Cholesterol: Primary Prevention. JAMA Cardiol. 2019 Apr 10. pii: 2730287. doi: 10.1001/jamacardio.2019.0777. [PubMed:30969322]
  22. Adams SP, Sekhon SS, Wright JM: Lipid-lowering efficacy of rosuvastatin. Cochrane Database Syst Rev. 2014 Nov 21;(11):CD010254. doi: 10.1002/14651858.CD010254.pub2. [PubMed:25415541]
  23. Yahya R, Berk K, Verhoeven A, Bos S, van der Zee L, Touw J, Erhart G, Kronenberg F, Timman R, Sijbrands E, Roeters van Lennep J, Mulder M: Statin treatment increases lipoprotein(a) levels in subjects with low molecular weight apolipoprotein(a) phenotype. Atherosclerosis. 2019 Jul 3. pii: S0021-9150(19)31392-9. doi: 10.1016/j.atherosclerosis.2019.07.001. [PubMed:31327478]
  24. Moghadasian MH: Clinical pharmacology of 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors. Life Sci. 1999;65(13):1329-37. doi: 10.1016/s0024-3205(99)00199-x. [PubMed:10503952]
  25. Liao JK, Laufs U: Pleiotropic effects of statins. Annu Rev Pharmacol Toxicol. 2005;45:89-118. doi: 10.1146/annurev.pharmtox.45.120403.095748. [PubMed:15822172]
  26. Nicholls SJ, Ballantyne CM, Barter PJ, Chapman MJ, Erbel RM, Libby P, Raichlen JS, Uno K, Borgman M, Wolski K, Nissen SE: Effect of two intensive statin regimens on progression of coronary disease. N Engl J Med. 2011 Dec 1;365(22):2078-87. doi: 10.1056/NEJMoa1110874. Epub 2011 Nov 15. [PubMed:22085316]
  27. Martin PD, Warwick MJ, Dane AL, Brindley C, Short T: Absolute oral bioavailability of rosuvastatin in healthy white adult male volunteers. Clin Ther. 2003 Oct;25(10):2553-63. [PubMed:14667956]
  28. Birmingham BK, Bujac SR, Elsby R, Azumaya CT, Zalikowski J, Chen Y, Kim K, Ambrose HJ: Rosuvastatin pharmacokinetics and pharmacogenetics in Caucasian and Asian subjects residing in the United States. Eur J Clin Pharmacol. 2015 Mar;71(3):329-40. doi: 10.1007/s00228-014-1800-0. Epub 2015 Jan 30. [PubMed:25630984]
  29. Elsby R, Hilgendorf C, Fenner K: Understanding the critical disposition pathways of statins to assess drug-drug interaction risk during drug development: it's not just about OATP1B1. Clin Pharmacol Ther. 2012 Nov;92(5):584-98. doi: 10.1038/clpt.2012.163. Epub 2012 Oct 10. [PubMed:23047648]
  30. Martin PD, Warwick MJ, Dane AL, Hill SJ, Giles PB, Phillips PJ, Lenz E: Metabolism, excretion, and pharmacokinetics of rosuvastatin in healthy adult male volunteers. Clin Ther. 2003 Nov;25(11):2822-35. [PubMed:14693307]
  31. Authors unspecified: MRC/BHF Heart Protection Study of cholesterol lowering with simvastatin in 20,536 high-risk individuals: a randomised placebo-controlled trial. Lancet. 2002 Jul 6;360(9326):7-22. doi: 10.1016/S0140-6736(02)09327-3. [PubMed:12114036]
  32. Keskitalo JE, Zolk O, Fromm MF, Kurkinen KJ, Neuvonen PJ, Niemi M: ABCG2 polymorphism markedly affects the pharmacokinetics of atorvastatin and rosuvastatin. Clin Pharmacol Ther. 2009 Aug;86(2):197-203. doi: 10.1038/clpt.2009.79. Epub 2009 May 27. [PubMed:19474787]
  33. Lee E, Ryan S, Birmingham B, Zalikowski J, March R, Ambrose H, Moore R, Lee C, Chen Y, Schneck D: Rosuvastatin pharmacokinetics and pharmacogenetics in white and Asian subjects residing in the same environment. Clin Pharmacol Ther. 2005 Oct;78(4):330-41. doi: 10.1016/j.clpt.2005.06.013. [PubMed:16198652]
  34. Cooper KJ, Martin PD, Dane AL, Warwick MJ, Schneck DW, Cantarini MV: The effect of fluconazole on the pharmacokinetics of rosuvastatin. Eur J Clin Pharmacol. 2002 Nov;58(8):527-31. doi: 10.1007/s00228-002-0508-8. Epub 2002 Oct 3. [PubMed:12451430]
  35. Windass AS, Lowes S, Wang Y, Brown CD: The contribution of organic anion transporters OAT1 and OAT3 to the renal uptake of rosuvastatin. J Pharmacol Exp Ther. 2007 Sep;322(3):1221-7. doi: 10.1124/jpet.107.125831. Epub 2007 Jun 21. [PubMed:17585018]
  36. Pasanen MK, Fredrikson H, Neuvonen PJ, Niemi M: Different effects of SLCO1B1 polymorphism on the pharmacokinetics of atorvastatin and rosuvastatin. Clin Pharmacol Ther. 2007 Dec;82(6):726-33. doi: 10.1038/sj.clpt.6100220. Epub 2007 May 2. [PubMed:17473846]
  37. Kostapanos MS, Milionis HJ, Elisaf MS: Rosuvastatin-associated adverse effects and drug-drug interactions in the clinical setting of dyslipidemia. Am J Cardiovasc Drugs. 2010;10(1):11-28. doi: 10.2165/13168600-000000000-00000. [PubMed:20104931]
  38. Kannel WB, Castelli WP, Gordon T, McNamara PM: Serum cholesterol, lipoproteins, and the risk of coronary heart disease. The Framingham study. Ann Intern Med. 1971 Jan;74(1):1-12. doi: 10.7326/0003-4819-74-1-1. [PubMed:5539274]
  39. Weitz-Schmidt G, Welzenbach K, Brinkmann V, Kamata T, Kallen J, Bruns C, Cottens S, Takada Y, Hommel U: Statins selectively inhibit leukocyte function antigen-1 by binding to a novel regulatory integrin site. Nat Med. 2001 Jun;7(6):687-92. doi: 10.1038/89058. [PubMed:11385505]
  40. Zhao W, Zhao SP: Different effects of statins on induction of diabetes mellitus: an experimental study. Drug Des Devel Ther. 2015 Nov 24;9:6211-23. doi: 10.2147/DDDT.S87979. eCollection 2015. [PubMed:26648697]
  41. Harper CR, Jacobson TA: The broad spectrum of statin myopathy: from myalgia to rhabdomyolysis. Curr Opin Lipidol. 2007 Aug;18(4):401-8. doi: 10.1097/MOL.0b013e32825a6773. [PubMed:17620856]
  42. FDA Label - Rosuvastatin [File]
  43. Health Canada Monograph - Rosuvastatin [File]
External Links
Human Metabolome Database
HMDB0015230
KEGG Drug
D08492
PubChem Compound
446157
PubChem Substance
46509022
ChemSpider
393589
BindingDB
18372
ChEBI
38545
ChEMBL
CHEMBL1496
Therapeutic Targets Database
DAP000555
PharmGKB
PA134308647
HET
FBI
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Rosuvastatin
ATC Codes
C10BX10 — Rosuvastatin and valsartanC10BX05 — Rosuvastatin and acetylsalicylic acidC10BX07 — Rosuvastatin, amlodipine and lisinoprilC10AA07 — RosuvastatinA10BH52 — Gemigliptin and rosuvastatinG01AE10 — Combinations of sulfonamidesC10BX13 — Rosuvastatin, perindopril and indapamideC10BX09 — Rosuvastatin and amlodipineC10BX14 — Rosuvastatin, amlodipine and perindoprilC10BA06 — Rosuvastatin and ezetimibe
AHFS Codes
  • 24:06.08 — Hmg-coa Reductase Inhibitors
MSDS
Download (57.8 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedBasic ScienceAtherosclerosis / Inflammatory Activity in Carotid Arteries1
0CompletedBasic ScienceAtherosclerosis / Inflammatory Activity in Coronary Arteries1
0CompletedTreatmentFriedreich's Ataxia1
0CompletedTreatmentHIV Seropositivity1
0RecruitingBasic ScienceInteraction Drug Food1
0Unknown StatusPreventionPatients With Coronary Artery Disease Scheduled for by Pass Surgery1
1Active Not RecruitingNot AvailableHealthy Volunteers1
1Active Not RecruitingBasic ScienceNash1
1Active Not RecruitingTreatmentHealthy Volunteers1
1Active Not RecruitingTreatmentParkinson's Disease (PD)1
1Active Not RecruitingTreatmentProstatic Neoplasms, Castration-Resistant1
1CompletedNot AvailableAcute Coronary Syndromes (ACS)1
1CompletedNot AvailableDrug Drug Interaction (DDI) / Healthy Volunteers / Pharmacokinetics1
1CompletedNot AvailableDyslipidemia & Hypertension1
1CompletedNot AvailableHealthy Volunteers7
1CompletedNot AvailableHealthy Volunteers / Pharmacokinetics of ASP015K1
1CompletedNot AvailableHepatitis C Viral Infection1
1CompletedNot AvailableHigh Blood Pressure (Hypertension)3
1CompletedNot AvailableHuman Immunodeficiency Virus (HIV) Infections1
1CompletedNot AvailableImmunosuppression For Disease1
1CompletedNot AvailablePharmacokinetics and Drug Interaction of Crestor and Glucodown SR1
1CompletedBasic ScienceCYP2C19 Poor / Extensive Metabolizers1
1CompletedBasic ScienceDrug Drug Interaction (DDI)1
1CompletedBasic ScienceDrug Drug Interaction (DDI) / Healthy Volunteers / Intestinal Absorption / Pharmacokinetics of Fidaxomicin / Pharmacokinetics of Rosuvastatin1
1CompletedBasic ScienceDrug Interaction Potentiation2
1CompletedBasic ScienceDrug Pharmacokinetics in Healthy Volunteers1
1CompletedBasic ScienceHealthy Volunteers6
1CompletedBasic SciencePharmacokinetic Variables1
1CompletedBasic ScienceRheumatoid Arthritis1
1CompletedOtherHealthy Volunteers3
1CompletedOtherHigh Blood Pressure (Hypertension)1
1CompletedOtherHigh Cholesterol1
1CompletedOtherHigh Risk Coronary Artery Disease1
1CompletedOtherHuman Immunodeficiency Virus (HIV) Infections / Human Immunodeficiency Virus Infection(HIV)/Acquired Immunodeficiency Syndrome (AIDS)1
1CompletedOtherType 2 Diabetes Mellitus1
1CompletedScreeningDyslipidemias1
1CompletedSupportive CareHealthy Male Volunteers1
1CompletedTreatmentAcute Coronary Syndromes (ACS) / Angioplasty, Transluminal, Percutaneous Coronary / Blood Platelets / Hydroxymethylglutaryl-CoA Reductase Inhibitors1
1CompletedTreatmentAdverse Events / Pharmacokinetic Variables1
1CompletedTreatmentAdverse Events / Pharmacokinetics1
1CompletedTreatmentAnemias1
1CompletedTreatmentAsthma1
1CompletedTreatmentAtherosclerosis1
1CompletedTreatmentAtherosclerosis / High Cholesterol1
1CompletedTreatmentCrohn's Disease (CD)1
1CompletedTreatmentDiabetes Mellitus (DM)4
1CompletedTreatmentDiabetes Mellitus (DM) / Healthy Volunteers1
1CompletedTreatmentDiabetes Mellitus (DM) / Hyperlipidemias2
1CompletedTreatmentDyslipidemia, Renal Insufficiency1
1CompletedTreatmentDyslipidemias2
1CompletedTreatmentElderly1
1CompletedTreatmentEndotoxaemia1
1CompletedTreatmentHealthy Male Subjects1
1CompletedTreatmentHealthy Male Volunteers1
1CompletedTreatmentHealthy Volunteers26
1CompletedTreatmentHeathy Volunteer1
1CompletedTreatmentHepatitis C Virus (HCV) Infection1
1CompletedTreatmentHereditary Angioedema1
1CompletedTreatmentHigh Blood Pressure (Hypertension)1
1CompletedTreatmentHigh Blood Pressure (Hypertension) / Hyperlipidemias8
1CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections1
1CompletedTreatmentHypertension With Dyslipidemia2
1CompletedTreatmentHypertension and Dyslipidemia1
1CompletedTreatmentHypertension, Hyperlipidemia2
1CompletedTreatmentHypertriglyceridemias1
1CompletedTreatmentImpaired Renal Function1
1CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC) / Squamous Cell Carcinoma (SCC)1
1CompletedTreatmentMetabolic Diseases1
1CompletedTreatmentNeoplasms1
1CompletedTreatmentSkin Diseases, Bacterial1
1CompletedTreatmentSystemic Lupus Erythematosus (SLE)1
1CompletedTreatmentCMET-dysregulated Advanced Solid Tumors1
1Enrolling by InvitationNot AvailableHealthy Volunteers1
1Enrolling by InvitationTreatmentHealthy Volunteers2
1Not Yet RecruitingBasic ScienceHealthy Volunteers1
1Not Yet RecruitingTreatmentHealthy Volunteers1
1Not Yet RecruitingTreatmentProstate Cancer1
1RecruitingBasic ScienceAutoimmune Diseases / Inflammatory Diseases1
1RecruitingBasic ScienceHealthy Volunteers1
1RecruitingBasic ScienceStatin Pharmacokinetics Pre and Post Gastric Bypass Surgery1
1RecruitingDiagnosticHealthy Volunteers1
1RecruitingOtherNeoplasms1
1RecruitingTreatmentAdvanced Solid Tumors / Metastatic Melanoma1
1RecruitingTreatmentBreast Cancer1
1RecruitingTreatmentDiabetes Mellitus (DM) / Hyperlipidemias2
1RecruitingTreatmentHealthy Adult Subjects1
1RecruitingTreatmentHigh Blood Pressure (Hypertension) / Hyperlipidemias1
1TerminatedTreatmentCardiovascular Complications / Recurrent Breast Cancer / Stage I Breast Carcinoma / Stage II Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer1
1TerminatedTreatmentHigh Blood Pressure (Hypertension) / Hyperlipidemias1
1TerminatedTreatmentPlasmodium Infections1
1Unknown StatusTreatmentHealthy Volunteers1
1WithdrawnBasic ScienceHealthy Volunteers1
1, 2CompletedTreatmentCraniocerebral Injuries1
1, 2Unknown StatusTreatmentHuman Immunodeficiency Virus (HIV) Infections1
1, 2Unknown StatusTreatmentPre-Eclampsia, Severe1
2Active Not RecruitingSupportive CareBreast Cancer1
2CompletedPreventionDeep Vein Thrombosis / Neoplasms / Venous Thromboembolism (VTE)1
2CompletedPreventionHeart Diseases / Human Immunodeficiency Virus (HIV) Infections1
2CompletedPreventionHigh Cholesterol1
2CompletedPreventionMinor burns1
2CompletedTreatmentArteriovenous Fistulas / Diabetes Mellitus (DM) / End-Stage Kidney Disease1
2CompletedTreatmentAtherosclerosis / Systemic Lupus Erythematosus (SLE)1
2CompletedTreatmentCardiovascular Disease (CVD) / Endothelial Dysfunction1
2CompletedTreatmentCerebral Hemorrhage / Stroke1
2CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD)1
2CompletedTreatmentCoronary Artery Disease / Obstructive Coronary Artery Disease1
2CompletedTreatmentCraniocerebral Injuries1
2CompletedTreatmentDiabetes Mellitus (DM)1
2CompletedTreatmentDiabetic Polyneuropathy1
2CompletedTreatmentDiabetic Polyneuropathy / Oxidative Stress1
2CompletedTreatmentDyslipidemias2
2CompletedTreatmentHeart Failure1
2CompletedTreatmentHepatitis C Viral Infection1
2CompletedTreatmentHigh Cholesterol1
2CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Hyperlipidemias1
2CompletedTreatmentHyperlipidemias1
2CompletedTreatmentIschaemia1
2CompletedTreatmentPlatelets Dysfunction1
2CompletedTreatmentRheumatoid Arthritis1
2Not Yet RecruitingTreatmentCoronary Syndrome1
2Not Yet RecruitingTreatmentDyslipidemias1
2RecruitingPreventionOvarian Cancer1
2RecruitingPreventionVenous Thromboembolism (VTE)1
2RecruitingTreatmentCoronary Heart Disease (CHD) / Human Immunodeficiency Virus (HIV) Infections1
2RecruitingTreatmentMetabolic Syndromes / Osteoporosis / Osteoporosis and Cardio-Metabolic Syndrome Following Spinal Cord Injury / Spinal Cord Injuries (SCI)1
2RecruitingTreatmentRectal Carcinoma1
2RecruitingTreatmentVenous Thromboembolism (VTE) / Wounds and Injuries1
2TerminatedBasic ScienceCoronary Artery Disease / Dyslipidemias1
2TerminatedTreatmentCritically-ill Patients / H1N1/Influenza Infection1
2TerminatedTreatmentInfluenza A Virus Infection1
2Unknown StatusNot AvailableHuman Immunodeficiency Virus Type 1 (HIV-1) Infection1
2Unknown StatusTreatmentAcute Myocardial Infarction (AMI)1
2Unknown StatusTreatmentDepression1
2Unknown StatusTreatmentSepsis1
2, 3CompletedTreatmentBlood Pressures / Glomerular Filtration Rate (GFR) / Lipids / Renal Artery Obstruction / Stents1
2, 3CompletedTreatmentPeriodontitis, Chronic5
2, 3CompletedTreatmentPeriodontitis, Chronic / Type2 Diabetes1
2, 3CompletedTreatmentRheumatoid Arthritis1
2, 3RecruitingTreatmentGastroesophageal variceal hemorrhage prophylaxis / Liver Cirrhosis / Portal Hypertension1
2, 3RecruitingTreatmentHyperlipidemias1
2, 3TerminatedTreatmentCardiovascular Disease (CVD) / Human Immunodeficiency Virus (HIV) Infections1
3Active Not RecruitingPreventionANCA-associated Primary Necrotizing Vasculitides1
3Active Not RecruitingPreventionCardiovascular Disease (CVD) / Coronary Artery Disease / Type 2 Diabetes Mellitus1
3Active Not RecruitingTreatmentHigh Blood Pressure (Hypertension) / High Cholesterol1
3Active Not RecruitingTreatmentHigh Cholesterol1
3CompletedNot AvailableHigh Cholesterol1
3CompletedPreventionAtherosclerotic Disease / Postoperative Hemorrhages1
3CompletedPreventionHeart Failure1
3CompletedPreventionRenal Failure1
3CompletedTreatmentAcute Coronary Syndromes (ACS)2
3CompletedTreatmentAortic Valve Stenosis1
3CompletedTreatmentAssess the Periprocedural Myocardial Necrosis1
3CompletedTreatmentAtherosclerosis3
3CompletedTreatmentAtherosclerosis / Cardiovascular Disease (CVD)1
3CompletedTreatmentAtherosclerosis / Coronary Heart Disease (CHD) / High Cholesterol2
3CompletedTreatmentCardiovascular Disorders / Diabetes Mellitus (DM)1
3CompletedTreatmentCarotid Artery Stenosis / High Cholesterol1
3CompletedTreatmentCholesterolemia / High Blood Pressure (Hypertension)1
3CompletedTreatmentCongestive Cardiomyopathy1
3CompletedTreatmentCongestive Heart Failure1
3CompletedTreatmentCoronary Arteriosclerosis1
3CompletedTreatmentCoronary Artery Atherosclerosis1
3CompletedTreatmentCoronary Artery Disease / Myocardial Ischemia1
3CompletedTreatmentCoronary Heart Disease (CHD) / Dyslipidemias / Mixed hypercholesterolemia2
3CompletedTreatmentCoronary Heart Disease (CHD) / High Cholesterol1
3CompletedTreatmentDiabetic Dyslipidemia / Type 2 Diabetes Mellitus1
3CompletedTreatmentDyslipidemia (Fredrickson Type Ⅱa)4
3CompletedTreatmentDyslipidemia (Fredrickson Type Ⅱa) / High Cholesterol1
3CompletedTreatmentDyslipidemia With Hypertension1
3CompletedTreatmentDyslipidemias2
3CompletedTreatmentDyslipidemias / High Blood Pressure (Hypertension)2
3CompletedTreatmentDyslipidemias / High Cholesterol5
3CompletedTreatmentDyslipidemias / Hypertension,Essential1
3CompletedTreatmentDyslipidemias / Kidney Diseases1
3CompletedTreatmentDyslipidemias / Metabolic Syndromes2
3CompletedTreatmentDyslipidemias / Type 2 Diabetes Mellitus3
3CompletedTreatmentEssential Hypertension, Dyslipidemia1
3CompletedTreatmentFredrickson Type IIa & Type IIb Dyslipidaemia1
3CompletedTreatmentHeart Failure1
3CompletedTreatmentHeart Failure / Positron Emission Tomography (PET) / Rosuvastatin1
3CompletedTreatmentHeterozygous Familial Hypercholesterolemia1
3CompletedTreatmentHigh Blood Pressure (Hypertension) / Hyperlipidemias3
3CompletedTreatmentHigh Cholesterol25
3CompletedTreatmentHomozygous Familial Hypercholesterolemia (HoFH)2
3CompletedTreatmentHyperlipidemias1
3CompletedTreatmentHyperlipoproteinemia Type III1
3CompletedTreatmentHypertension With Hyperlipidemia1
3CompletedTreatmentMetabolic Syndromes1
3CompletedTreatmentObesity, Abdominal1
3CompletedTreatmentPeriprocedural Myocardial Necrosis1
3CompletedTreatmentSclerosis, Progressive Systemic1
3CompletedTreatmentType 2 Diabetes Mellitus1
3CompletedTreatmentMixed hypercholesterolemia2
3Enrolling by InvitationTreatmentHypertension With Hyperlipidemia1
3Not Yet RecruitingTreatmentDyslipidemias1
3Not Yet RecruitingTreatmentDyslipidemias / High Blood Pressure (Hypertension)1
3Not Yet RecruitingTreatmentDyslipidemias / Hypertriglyceridemias1
3Not Yet RecruitingTreatmentHigh Blood Pressure (Hypertension) / High Cholesterol1
3Not Yet RecruitingTreatmentHuman Immunodeficiency Virus (HIV) Infections1
3RecruitingTreatmentDyslipidemias / High Blood Pressure (Hypertension)1
3RecruitingTreatmentHigh Blood Pressure (Hypertension) / Hyperlipidemias1
3RecruitingTreatmentHigh Cholesterol1
3TerminatedPreventionElevated High-sensitivity C-Reactive Protein (hsCRP)1
3TerminatedTreatmentAcute Lung Injury (ALI) / Sepsis1
3TerminatedTreatmentColorectal Cancers / Precancerous Conditions1
3TerminatedTreatmentHigh Cholesterol3
3TerminatedTreatmentHip Fractures1
3TerminatedTreatmentStable Coronary Artery Disease Undergoing PCI1
3TerminatedTreatmentStroke1
3Unknown StatusPreventionCoronary Heart Disease (CHD)1
3Unknown StatusTreatmentCoronary Artery Disease1
3Unknown StatusTreatmentHigh Blood Pressure (Hypertension) / Hyperlipidemias1
3Unknown StatusTreatmentHigh Cholesterol1
3Unknown StatusTreatmentValvular Cardiac Surgery1
3WithdrawnTreatmentPulmonary Embolism / Thrombosis, Venous1
4Active Not RecruitingTreatment22q Telomere Deletion Syndrome / Telomere Length, Mean Leukocyte / Telomere Shortening1
4Active Not RecruitingTreatmentDyslipidemias1
4Active Not RecruitingTreatmentHigh Blood Pressure (Hypertension)1
4Active Not RecruitingTreatmentHyperlipidemias / Sexual Dysfunctions1
4CompletedNot AvailableAtherosclerosis / High Cholesterol1
4CompletedNot AvailableCoronary Heart Disease (CHD)1
4CompletedNot AvailableHealthy Volunteers1
4CompletedNot AvailableSexual Dysfunctions1
4CompletedBasic ScienceHigh Cholesterol / Type 2 Diabetes Mellitus1
4CompletedDiagnosticCardiovascular Disease (CVD) / Human Immunodeficiency Virus (HIV)1
4CompletedHealth Services ResearchDiabetes Mellitus (DM) / Dyslipidemias1
4CompletedOtherDyslipidemias / High Blood Pressure (Hypertension)1
4CompletedPreventionAcute Coronary Syndromes (ACS)2
4CompletedPreventionAdverse Effects / Coronary Artery Atherosclerosis / Insulin resistance syndrome1
4CompletedPreventionAtherosclerosis / Cardiovascular Disease (CVD)1
4CompletedPreventionAtherosclerosis / Systemic Lupus Erythematosus (SLE) / Thromboembolism1
4CompletedPreventionAtrial Fibrillation (AF) / Myocardium; Injury1
4CompletedPreventionCardiovascular Disease (CVD) / Stroke1
4CompletedPreventionChronic Kidney Disease (CKD) / Diabetes Mellitus (DM)1
4CompletedPreventionEndothelial Dysfunction / Ischemia Reperfusion Injury1
4CompletedPreventionIschemia Reperfusion Injury1
4CompletedPreventionRenal Dysfunction1
4CompletedPreventionType 2 Diabetes Mellitus1
4CompletedSupportive CareA Total of 234 Patients With Acute Coronary Syndrome Who Will Undergo OPCAB1
4CompletedTreatmentAcute Coronary Syndromes (ACS) / Carotid Atherosclerotic Plaque With Inflammation1
4CompletedTreatmentAcute Coronary Syndromes (ACS) / Dyslipidemias1
4CompletedTreatmentAcute Coronary Syndromes (ACS) / High Cholesterol1
4CompletedTreatmentAdult Periodontitis1
4CompletedTreatmentAngina Pectoris1
4CompletedTreatmentAtherosclerosis / Coronary Heart Disease (CHD) / Diabetes Mellitus (DM) / Dyslipidemias / Stroke1
4CompletedTreatmentAtherosclerosis / Endothelial Dysfunction1
4CompletedTreatmentCardiovascular Risk Factors / High Blood Pressure (Hypertension)1
4CompletedTreatmentComplete Occlusion of Coronary Artery / Hibernation, Myocardial1
4CompletedTreatmentCoronary Artery Disease3
4CompletedTreatmentCoronary Artery Disease Progression1
4CompletedTreatmentCoronary Artery Disease / Hyperlipidemias1
4CompletedTreatmentDiabetes Mellitus (DM)2
4CompletedTreatmentDiabetes Mellitus and Hypercholesterolemia1
4CompletedTreatmentDisorder Related to Renal Transplantation / High Cholesterol1
4CompletedTreatmentDyslipidemia (Fredrickson Type Ⅱa)1
4CompletedTreatmentDyslipidemias / High Cholesterol1
4CompletedTreatmentFurcation Defects1
4CompletedTreatmentHealthy Volunteers1
4CompletedTreatmentHigh Cholesterol6
4CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Hyperlipidemias1
4CompletedTreatmentHyperlipidemias2
4CompletedTreatmentHyperlipidemias / Hyperlipoproteinemia Type IIb / Hyperlipoproteinemia Type iv / Hyperlipoproteinemia Type V / Hypertriglyceridemias1
4CompletedTreatmentHypertriglycemia / Type 2 Diabetes Mellitus1
4CompletedTreatmentMetabolic Syndromes2
4CompletedTreatmentMyocardial Infarction [C14.907.585.500]1
4CompletedTreatmentOSAS (Obstructive Sleep Apneas Syndrome)1
4CompletedTreatmentOrganic Anion Transporting Polypeptide1B1 (OATP1B1) / Rosuvastatin1
4CompletedTreatmentST Segment Elevation Myocardial Infarction (STEMI) / Subclinical Carotid Atherosclerosis1
4CompletedTreatmentST-segment Elevation AMI1
4CompletedTreatmentStroke, Ischemic1
4CompletedTreatmentType 2 Diabetes Mellitus2
4CompletedTreatmentType IIa and IIb Hypercholesterolaemia1
4Enrolling by InvitationTreatmentCerebral Infarctions / CLOPIDOGREL, POOR METABOLISM of (Disorder)1
4Enrolling by InvitationTreatmentChronic Total Occlusion of Coronary Artery / Coronary Artery Disease / Percutaneous Coronary Intervention / Viable Myocardium1
4Not Yet RecruitingPreventionAtherosclerosis / Cardiovascular Disease (CVD) / Molecular Imaging1
4Not Yet RecruitingPreventionCoronary Artery Disease1
4Not Yet RecruitingPreventionCoronary Heart Disease (CHD) / Hyperlipidemias1
4Not Yet RecruitingSupportive CareStroke, Ischemic1
4Not Yet RecruitingTreatmentAngina Pectoris / Coronary Artery Disease1
4Not Yet RecruitingTreatmentArterial Hypertension1
4Not Yet RecruitingTreatmentInfarction, Anterior Cerebral Artery1
4Not Yet RecruitingTreatmentIntracranial Arterial Stenosis1
4Not Yet RecruitingTreatmentIschemic1
4Not Yet RecruitingTreatmentParoxysmal Atrial Fibrillation (PAF)1
4RecruitingBasic ScienceHealthy Volunteers1
4RecruitingHealth Services ResearchDiabetes Mellitus (DM)1
4RecruitingPreventionAdverse Effects / Cardiovascular Disease (CVD) / Cardiovascular Risk Factors1
4RecruitingPreventionHigh Blood Pressure (Hypertension) / Stroke / Transient Ischaemic Attack (TIA)1
4RecruitingTreatmentAcute Coronary Syndromes (ACS)1
4RecruitingTreatmentAngina Pectoris / Coronary Artery Disease1
4RecruitingTreatmentAtherosclerosis1
4RecruitingTreatmentCardiovascular Disease (CVD)1
4RecruitingTreatmentCardiovascular Disease (CVD) / Coronary Artery Disease / Coronary Heart Disease (CHD)1
4RecruitingTreatmentCarotid Atherosclerosis1
4RecruitingTreatmentChronic Kidney Disease (CKD) / Proteinuria1
4RecruitingTreatmentCoronary Artery Disease3
4RecruitingTreatmentCoronary Artery Dissection, Spontaneous1
4RecruitingTreatmentDyslipidemias / Nonalcoholic Fatty Liver Disease1
4RecruitingTreatmentDyslipidemias / Venous Thromboembolism (VTE)1
4RecruitingTreatmentHigh Cholesterol1
4RecruitingTreatmentHypertension, Hyperlipidemia1
4RecruitingTreatmentIntracranial Atherosclerosis / Stroke1
4RecruitingTreatmentMyocardial Fibrosis1
4RecruitingTreatmentST Elevation Myocardial Infarction (STEMI)1
4TerminatedNot AvailableDyslipidemias1
4TerminatedNot AvailableStatin Adverse Reaction / Statin-Associated Myopathy1
4TerminatedTreatmentAtherosclerosis1
4TerminatedTreatmentAtherosclerosis / Coronary Artery Disease / High Cholesterol1
4TerminatedTreatmentAtherosclerosis / Human Immunodeficiency Virus (HIV) Infections1
4TerminatedTreatmentCoronary Arteriosclerosis1
4TerminatedTreatmentHigh Cholesterol1
4TerminatedTreatmentMetabolic Syndromes1
4TerminatedTreatmentStroke / Transient Ischaemic Attack (TIA)1
4Unknown StatusPreventionCardiovascular Disease (CVD) / Human Immunodeficiency Virus (HIV)1
4Unknown StatusPreventionDeep Vein Thrombosis / Prevention / Thrombotic events / Venous1
4Unknown StatusTreatmentAcute Coronary Syndromes (ACS)1
4Unknown StatusTreatmentAcute Coronary Syndromes (ACS) / Angioplasty1
4Unknown StatusTreatmentAtherosclerosis / Hyperlipidemias1
4Unknown StatusTreatmentCoronary Artery Disease4
4Unknown StatusTreatmentCoronary Artery Disease / Hyperlipidemias1
4Unknown StatusTreatmentCoronary Heart Disease (CHD) / High Cholesterol1
4Unknown StatusTreatmentDyslipidemias2
4Unknown StatusTreatmentFocus of Study1
4Unknown StatusTreatmentHigh Cholesterol1
4Unknown StatusTreatmentNon ST Segment Elevation Acute Coronary Syndrome1
4Unknown StatusTreatmentNon-familial hypercholesterolemia / Physical Inactivity1
4Unknown StatusTreatmentIncreases in serum total low-density lipoprotein (LDL) / Systemic Lupus Erythematosus (SLE)1
4WithdrawnBasic ScienceDiabetes Mellitus (DM) / Glaucoma1
4WithdrawnPreventionContrast-Induced Acute Kidney Injury / Hydration / Primary PCI / Rosuvastatin / ST Elevation Myocardial Infarction1
4WithdrawnTreatmentDyslipidemia (Fredrickson Type Ⅱa)1
Not AvailableActive Not RecruitingNot AvailableDyslipidemias1
Not AvailableAvailableNot AvailableCVD / Diabetes Mellitus (DM)1
Not AvailableAvailableNot AvailableHyperlipidemias1
Not AvailableCompletedNot AvailableAnkylosing Spondylitis (AS) / Carotid Artery Plaque / Rheumatoid Arthritis1
Not AvailableCompletedNot AvailableCardiovascular Disease (CVD) / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableCerebrovascular Accident / Coronary Heart Disease (CHD) / Diabetes Mellitus (DM) / High Cholesterol / Peripheral Vascular Disease Patient1
Not AvailableCompletedNot AvailableDyslipidemia (Fredrickson Type Ⅱa)1
Not AvailableCompletedNot AvailableHigh Cholesterol2
Not AvailableCompletedBasic ScienceAdenosine Metabolism1
Not AvailableCompletedBasic ScienceAtherosclerosis / Hyperlipidemias1
Not AvailableCompletedBasic ScienceDeep Vein Thrombosis / Pulmonary Embolism1
Not AvailableCompletedDiagnosticStatin Induced Proteinuria1
Not AvailableCompletedTreatmentAcute Coronary Syndromes (ACS)1
Not AvailableCompletedTreatmentCoronary Artery Occlusive Disease1
Not AvailableCompletedTreatmentHigh Cholesterol / Human Immunodeficiency Virus (HIV) Infections1
Not AvailableCompletedTreatmentHypercholesterolemia With Concomitant Type 2 Diabetes1
Not AvailableNot Yet RecruitingNot AvailableAcute Ischemic Stroke AIS / Intracranial Atherosclerosis ICAS1
Not AvailableRecruitingBasic ScienceAtherosclerosis / Cardiovascular Disease (CVD)1
Not AvailableRecruitingPreventionAcute Coronary Syndromes (ACS)1
Not AvailableRecruitingTreatmentArteriosclerosis / Diabetes Mellitus (DM) / Lipid Disorders1
Not AvailableRecruitingTreatmentCardiovascular Disease (CVD) / Cerebrovascular Diseases / Peripheral Atherosclerotic Disease1
Not AvailableRecruitingTreatmentCardiovascular Disease (CVD) / Prostate Cancer1
Not AvailableRecruitingTreatmentIntracranial Arterial Diseases1
Not AvailableRecruitingTreatmentType 2 Diabetes Mellitus1
Not AvailableTerminatedPreventionHigh Blood Pressure (Hypertension) / High Cholesterol / Type 2 Diabetes Mellitus1
Not AvailableTerminatedTreatmentAcute Respiratory Distress Syndrome (ARDS) / Flu caused by Influenza / Influenza A Virus Infection1
Not AvailableTerminatedTreatmentHCC1
Not AvailableUnknown StatusTreatmentAcute Coronary Syndromes (ACS) / Diabetes Mellitus (DM)1
Not AvailableUnknown StatusTreatmentAcute Respiratory Distress Syndrome (ARDS) / Blunt Chest Trauma1
Not AvailableUnknown StatusTreatmentHigh Cholesterol1
Not AvailableWithdrawnNot AvailablePCI Patients1
Not AvailableWithdrawnTreatmentHepatitis C Viral Infection1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • A-S Medication Solutions LLC
  • AstraZeneca Inc.
  • Bryant Ranch Prepack
  • Cardinal Health
  • Corden Pharma GmbH
  • IPR Pharmaceuticals Inc.
  • Lake Erie Medical and Surgical Supply
  • Murfreesboro Pharmaceutical Nursing Supply
  • Nucare Pharmaceuticals Inc.
  • PD-Rx Pharmaceuticals Inc.
  • Physicians Total Care Inc.
  • Prepak Systems Inc.
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • Southwood Pharmaceuticals
Dosage forms
FormRouteStrength
Tablet, film coatedOral10 mg/1
Tablet, film coatedOral20 mg/1
Tablet, film coatedOral40 mg/1
Tablet, film coatedOral5 mg/1
TabletOral
CapsuleOral10 mg/1
CapsuleOral20 mg/1
CapsuleOral40 mg/1
CapsuleOral5 mg/1
TabletOral10 mg
TabletOral10.0 mg
TabletOral20 mg
TabletOral20.0 mg
TabletOral40 mg
TabletOral40.0 mg
TabletOral5 mg
TabletOral5.0 mg
TabletOral10 mg/1
TabletOral20 mg/1
TabletOral40 mg/1
TabletOral5 mg/1
Tablet, coatedOral10 mg/1
Tablet, coatedOral20 mg/1
Tablet, coatedOral40 mg/1
Tablet, coatedOral5 mg/1
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)
CA2315141No2009-08-182020-08-04Canada
CA2072945No2001-07-312012-07-02Canada
US6858618Yes2005-02-222022-06-17Us
US7030152Yes2006-04-182018-10-02Us
US7964614Yes2011-06-212018-10-02Us
US6316460Yes2001-11-132021-02-04Us
USRE37314Yes2001-08-072016-07-08Us
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
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 FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This 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.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazines
Sub Class
Pyrimidines and pyrimidine derivatives
Direct Parent
Phenylpyrimidines
Alternative Parents
Medium-chain hydroxy acids and derivatives / Medium-chain fatty acids / Beta hydroxy acids and derivatives / Fluorobenzenes / Halogenated fatty acids / Heterocyclic fatty acids / Hydroxy fatty acids / Aryl fluorides / Unsaturated fatty acids / Organosulfonamides
show 13 more
Substituents
4-phenylpyrimidine / 5-phenylpyrimidine / Medium-chain hydroxy acid / Medium-chain fatty acid / Beta-hydroxy acid / Fluorobenzene / Halobenzene / Halogenated fatty acid / Heterocyclic fatty acid / Hydroxy fatty acid
show 33 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
statin (synthetic), sulfonamide, pyrimidines, dihydroxy monocarboxylic acid, monofluorobenzenes (CHEBI:38545)

Targets

Kind
Protein
Organism
Humans
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...
Gene Name
HMGCR
Uniprot ID
P04035
Uniprot Name
3-hydroxy-3-methylglutaryl-coenzyme A reductase
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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitory allosteric modulator
General Function
Metal ion binding
Specific Function
Integrin alpha-L/beta-2 is a receptor for ICAM1, ICAM2, ICAM3 and ICAM4. It is involved in a variety of immune phenomena including leukocyte-endothelial cell interaction, cytotoxic T-cell mediated ...
Gene Name
ITGAL
Uniprot ID
P20701
Uniprot Name
Integrin alpha-L
Molecular Weight
128768.495 Da
References
  1. Weitz-Schmidt G, Welzenbach K, Brinkmann V, Kamata T, Kallen J, Bruns C, Cottens S, Takada Y, Hommel U: Statins selectively inhibit leukocyte function antigen-1 by binding to a novel regulatory integrin site. Nat Med. 2001 Jun;7(6):687-92. doi: 10.1038/89058. [PubMed:11385505]
  2. Katano H, Pesnicak L, Cohen JI: 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. 2004 Apr 6;101(14):4960-5. Epub 2004 Mar 23. [PubMed:15041742]
  3. Liao JK, Laufs U: Pleiotropic effects of statins. Annu Rev Pharmacol Toxicol. 2005;45:89-118. doi: 10.1146/annurev.pharmtox.45.120403.095748. [PubMed:15822172]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
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 un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Sakaeda T, Fujino H, Komoto C, Kakumoto M, Jin JS, Iwaki K, Nishiguchi K, Nakamura T, Okamura N, Okumura K: Effects of acid and lactone forms of eight HMG-CoA reductase inhibitors on CYP-mediated metabolism and MDR1-mediated transport. Pharm Res. 2006 Mar;23(3):506-12. doi: 10.1007/s11095-005-9371-5. Epub 2006 Jan 1. [PubMed:16388406]
  2. Cooper KJ, Martin PD, Dane AL, Warwick MJ, Schneck DW, Cantarini MV: The effect of fluconazole on the pharmacokinetics of rosuvastatin. Eur J Clin Pharmacol. 2002 Nov;58(8):527-31. doi: 10.1007/s00228-002-0508-8. Epub 2002 Oct 3. [PubMed:12451430]
  3. Health Canada Monograph - Rosuvastatin [File]

Carriers

Kind
Protein
Organism
Humans
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 colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da

Transporters

Kind
Protein
Organism
Humans
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
Uniprot Name
Multidrug resistance-associated protein 4
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
Humans
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 inhibit...
Gene Name
SLCO1A2
Uniprot ID
P46721
Uniprot Name
Solute carrier organic anion transporter family member 1A2
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
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
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]
  2. Karlgren M, Ahlin G, Bergstrom CA, Svensson R, Palm J, Artursson P: In vitro and in silico strategies to identify OATP1B1 inhibitors and predict clinical drug-drug interactions. Pharm Res. 2012 Feb;29(2):411-26. doi: 10.1007/s11095-011-0564-9. Epub 2011 Aug 23. [PubMed:21861202]
  3. Elsby R, Hilgendorf C, Fenner K: Understanding the critical disposition pathways of statins to assess drug-drug interaction risk during drug development: it's not just about OATP1B1. Clin Pharmacol Ther. 2012 Nov;92(5):584-98. doi: 10.1038/clpt.2012.163. Epub 2012 Oct 10. [PubMed:23047648]
Kind
Protein
Organism
Humans
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), methotre...
Gene Name
SLCO1B3
Uniprot ID
Q9NPD5
Uniprot Name
Solute carrier organic anion transporter family member 1B3
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
Humans
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
Uniprot Name
Solute carrier organic anion transporter family member 2B1
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
Humans
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
Uniprot Name
Cystine/glutamate transporter
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
Humans
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
Uniprot Name
Bile salt export pump
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
Humans
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 fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. Elsby R, Hilgendorf C, Fenner K: Understanding the critical disposition pathways of statins to assess drug-drug interaction risk during drug development: it's not just about OATP1B1. Clin Pharmacol Ther. 2012 Nov;92(5):584-98. doi: 10.1038/clpt.2012.163. Epub 2012 Oct 10. [PubMed:23047648]
  2. Keskitalo JE, Zolk O, Fromm MF, Kurkinen KJ, Neuvonen PJ, Niemi M: ABCG2 polymorphism markedly affects the pharmacokinetics of atorvastatin and rosuvastatin. Clin Pharmacol Ther. 2009 Aug;86(2):197-203. doi: 10.1038/clpt.2009.79. Epub 2009 May 27. [PubMed:19474787]
  3. Lee E, Ryan S, Birmingham B, Zalikowski J, March R, Ambrose H, Moore R, Lee C, Chen Y, Schneck D: Rosuvastatin pharmacokinetics and pharmacogenetics in white and Asian subjects residing in the same environment. Clin Pharmacol Ther. 2005 Oct;78(4):330-41. doi: 10.1016/j.clpt.2005.06.013. [PubMed:16198652]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Organic anion transmembrane transporter activity
Specific Function
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name
ABCC2
Uniprot ID
Q92887
Uniprot Name
Canalicular multispecific organic anion transporter 1
Molecular Weight
174205.64 Da
References
  1. Ellis LC, Hawksworth GM, Weaver RJ: ATP-dependent transport of statins by human and rat MRP2/Mrp2. Toxicol Appl Pharmacol. 2013 Jun 1;269(2):187-94. doi: 10.1016/j.taap.2013.03.019. Epub 2013 Apr 2. [PubMed:23562342]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Curator comments
Substrate activity was demonstrated in vitro using human and rat OAT3 expressed on Xenopus Laevis.
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
Gene Name
SLC22A8
Uniprot ID
Q8TCC7
Uniprot Name
Solute carrier family 22 member 8
Molecular Weight
59855.585 Da
References
  1. VanWert AL, Gionfriddo MR, Sweet DH: Organic anion transporters: discovery, pharmacology, regulation and roles in pathophysiology. Biopharm Drug Dispos. 2010 Jan;31(1):1-71. doi: 10.1002/bdd.693. [PubMed:19953504]
  2. Windass AS, Lowes S, Wang Y, Brown CD: The contribution of organic anion transporters OAT1 and OAT3 to the renal uptake of rosuvastatin. J Pharmacol Exp Ther. 2007 Sep;322(3):1221-7. doi: 10.1124/jpet.107.125831. Epub 2007 Jun 21. [PubMed:17585018]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Virus receptor activity
Specific Function
The hepatic sodium/bile acid uptake system exhibits broad substrate specificity and transports various non-bile acid organic compounds as well. It is strictly dependent on the extracellular presenc...
Gene Name
SLC10A1
Uniprot ID
Q14973
Uniprot Name
Sodium/bile acid cotransporter
Molecular Weight
38118.64 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]

Drug created on June 13, 2005 07:24 / Updated on November 19, 2019 16:35