Identification

Logo pink
Are you a
new drug developer?
Contact us to learn more about our customized products and solutions.
Name
Atorvastatin
Accession Number
DB01076  (APRD00055)
Type
Small Molecule
Groups
Approved
Description

Atorvastatin, also known as the brand name product Lipitor, is a lipid-lowering drug belonging to the statin class of medications. By inhibiting the endogenous production of cholesterol within the liver, statins lower abnormal cholesterol and lipid levels and ultimately reduce the risk of cardiovascular disease. More specifically, statin medications competitively inhibit the enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) Reductase,8 which catalyzes the conversion of HMG-CoA to mevalonic acid. This 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.9,10

Atorvastatin and other drugs from the statin class of medications including lovastatin, pravastatin, rosuvastatin, fluvastatin, and simvastatin are considered first-line options for the treatment of dyslipidemia.9,10 Increasing use of the statin class of drugs 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.11 Elevated cholesterol levels, and in particular, elevated low-density lipoprotein (LDL) levels, are an important risk factor for the development of CVD.9,12 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.13,14,15,16,17,18 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.9,10 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% decrease in LDL cholesterol levels, while atorvastatin has been found to have about one-third of that potency.21,22,23,18,24 Potency is thought to correlate to tissue permeability as the more lipophilic statins such as atorvastatin are thought to enter endothelial cells by passive diffusion, as opposed to hydrophilic statins such as pravastatin and rosuvastatin which are taken up into hepatocytes through OATP1B1 (organic anion transporter protein 1B1)-mediated transport.25,26 Despite these differences in potency, several trials have demonstrated only minimal differences in terms of clinical outcomes between statins.16

Atorvastatin was first synthesized in 1985 by Dr. Bruce Roth and approved by the FDA in 1996.33 It is a pentasubstituted pyrrole3 formed by two contrasting moieties with an achiral heterocyclic core unit and a 3,5-dihydroxypentanoyl side chain identical to its parent compound.34 Unlike other members of the statin group, atorvastatin is an active compound and therefore does not require activation.4

Structure
Thumb
Synonyms
  • Atorvastatin
  • atorvastatina
  • atorvastatine
  • atorvastatinum
Product Ingredients
IngredientUNIICASInChI Key
Atorvastatin calciumC0GEJ5QCSO134523-03-8FQCKMBLVYCEXJB-MNSAWQCASA-L
Atorvastatin calcium trihydrate48A5M73Z4Q344423-98-9SHZPNDRIDUBNMH-NIJVSVLQSA-L
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AtorvastatinTablet10 mgOralRanbaxy Inc.Not applicableNot applicableCanada
AtorvastatinTablet80 mgOralActavis Pharma CompanyNot applicableNot applicableCanada
AtorvastatinTablet40 mgOralRatiopharm Inc Division Of Teva Canada Limited2010-05-192013-06-27Canada
AtorvastatinTablet20 mgOralPro Doc Limitee2010-05-21Not applicableCanada
AtorvastatinTablet20 mgOralApotex Corporation2013-01-07Not applicableCanada
AtorvastatinTablet20 mgOralLaboratoire Riva IncNot applicableNot applicableCanada
AtorvastatinTablet80 mgOralSivem Pharmaceuticals Ulc2012-06-26Not applicableCanada
AtorvastatinTablet80 mgOralSanis Health Inc2010-05-27Not applicableCanada
AtorvastatinTablet40 mgOralActavis Pharma CompanyNot applicableNot applicableCanada
AtorvastatinTablet80 mgOralAltamed PharmaNot applicableNot 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
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ach-atorvastatin CalciumTablet80 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ach-atorvastatin CalciumTablet40 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ach-atorvastatin CalciumTablet20 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ach-atorvastatin CalciumTablet10 mgOralAccord Healthcare LimitedNot applicableNot applicableCanada
Ag-atorvastatinTablet10 mgOralAngita Pharma Inc.2018-09-27Not applicableCanada
Ag-atorvastatinTablet80 mgOralAngita Pharma Inc.2018-09-25Not applicableCanada
Ag-atorvastatinTablet40 mgOralAngita Pharma Inc.2018-09-25Not applicableCanada
Ag-atorvastatinTablet20 mgOralAngita Pharma Inc.2018-09-25Not applicableCanada
Apo-atorvastatinTablet20 mgOralApotex Corporation2010-05-19Not applicableCanada
Apo-atorvastatinTablet10 mgOralApotex Corporation2010-05-19Not 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
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Amlodipine and atorvastatinAtorvastatin calcium trihydrate (20 mg/1) + Amlodipine besylate (10 mg/1)Tablet, film coatedOralCadila Healthcare Limited2019-05-30Not applicableUs
Amlodipine and atorvastatinAtorvastatin calcium trihydrate (10 mg/1) + Amlodipine besylate (5 mg/1)Tablet, film coatedOralCadila Healthcare Limited2019-05-30Not applicableUs
Amlodipine and atorvastatinAtorvastatin calcium trihydrate (20 mg/1) + Amlodipine besylate (10 mg/1)Tablet, film coatedOralMylan Pharmaceuticals Inc.2014-02-11Not applicableUs
Amlodipine and atorvastatinAtorvastatin calcium trihydrate (10 mg/1) + Amlodipine besylate (5 mg/1)Tablet, film coatedOralMylan Pharmaceuticals Inc.2015-04-02Not applicableUs
Amlodipine and atorvastatinAtorvastatin calcium trihydrate (80 mg/1) + Amlodipine besylate (5 mg/1)Tablet, film coatedOralZydus Pharmaceuticals (USA) Inc.2019-05-30Not applicableUs
Amlodipine and atorvastatinAtorvastatin calcium trihydrate (20 mg/1) + Amlodipine besylate (2.5 mg/1)Tablet, film coatedOralZydus Pharmaceuticals (USA) Inc.2019-05-30Not applicableUs
Amlodipine and atorvastatinAtorvastatin calcium trihydrate (10 mg/1) + Amlodipine besylate (10 mg/1)Tablet, film coatedOralCadila Healthcare Limited2019-05-30Not applicableUs
Amlodipine and atorvastatinAtorvastatin calcium trihydrate (40 mg/1) + Amlodipine besylate (2.5 mg/1)Tablet, film coatedOralCadila Healthcare Limited2019-05-30Not applicableUs
Amlodipine and atorvastatinAtorvastatin calcium trihydrate (10 mg/1) + Amlodipine besylate (10 mg/1)Tablet, film coatedOralMylan Pharmaceuticals Inc.2014-11-06Not applicableUs
Amlodipine and atorvastatinAtorvastatin calcium trihydrate (40 mg/1) + Amlodipine besylate (2.5 mg/1)Tablet, film coatedOralMylan Pharmaceuticals Inc.2013-02-14Not applicableUs
International/Other Brands
Atogal (Ingers (Czech Republic)) / Cardyl (Pfizer (Spain)) / Faboxim (Fabop (Argentina)) / Hipolixan (Pasteur (Chile)) / Lipotropic (Drugtech (Chile)) / Liprimar (Pfizer (Hungary, Ukraine), Goedecke (Russia)) / Lowden (Saval (Chile)) / Normalip (Quesada (Argentina)) / Sincol (Indeco (Argentina)) / Sortis (Pfizer (Austria, Czech Republic, Germany, Hungary, Poland, Portugal, Switzerland), Godecke (Germany), Parke, Davis (Germany)) / Torvacard (Zentiva (Czech Republic, Hungary, Poland, Russia, Ukraine)) / Torvast (Pfizer (Italy)) / Totalip (Guidotti (Italy)) / Tulip (Lek (Czech Republic, Russia), Wermar (Mexico), Sandoz (Poland, Ukraine), Pharmacia (Spain)) / Vastina (Penn (Argentina)) / Xanator (Sieger (Greece)) / Xarator (Parke, Davis (Italy)) / Zurinel (Prater (Chile))
Categories
UNII
A0JWA85V8F
CAS number
134523-00-5
Weight
Average: 558.6398
Monoisotopic: 558.253000445
Chemical Formula
C33H35FN2O5
InChI Key
XUKUURHRXDUEBC-KAYWLYCHSA-N
InChI
InChI=1S/C33H35FN2O5/c1-21(2)31-30(33(41)35-25-11-7-4-8-12-25)29(22-9-5-3-6-10-22)32(23-13-15-24(34)16-14-23)36(31)18-17-26(37)19-27(38)20-28(39)40/h3-16,21,26-27,37-38H,17-20H2,1-2H3,(H,35,41)(H,39,40)/t26-,27-/m1/s1
IUPAC Name
(3R,5R)-7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-(propan-2-yl)-1H-pyrrol-1-yl]-3,5-dihydroxyheptanoic acid
SMILES
CC(C)C1=C(C(=O)NC2=CC=CC=C2)C(=C(N1CC[C@@H](O)C[C@@H](O)CC(O)=O)C1=CC=C(F)C=C1)C1=CC=CC=C1

Pharmacology

Indication

Atorvastatin is approved for the treatment of several types of dyslipidemias including:

  • Primary hyperlipidemia and mixed dyslipidemia in adults.
  • Hypertriglyceridemia.
  • Primary dysbetalipoproteinemia.
  • Homozygous familial hypercholesterolemia.
  • Heterozygous familial hypercholesterolemia in adolescent patients with failed dietary modifications.2

Dyslipidemia is defined as an elevation of plasma cholesterol, triglycerides or both as well as to the presence of low levels of high-density lipoprotein. This condition represents an increased risk for the development of atherosclerosis.35

Atorvastatin is indicated, in combination with dietary modifications, to prevent cardiovascular events in patients with cardiac risk factors and/or abnormal lipid profiles.2

Atorvastatin can be used as a preventive agent for myocardial infarction, stroke, revascularization, and angina, in patients without coronary heart disease but with multiple risk factors, and in patients with type 2 diabetes without coronary heart disease but multiple risk factors.2

Atorvastatin can also be used as a preventive agent for non-fatal myocardial infarction, fatal and non-fatal stroke, revascularization procedures, hospitalization for congestive heart failure and angina in patients with coronary heart disease.2

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.9,10

Associated Conditions
Pharmacodynamics

Atorvastatin is an oral antilipemic agent which reversibly inhibits HMG-CoA reductase. 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, atorvastatin reduces the risk of cardiovascular morbidity and mortality.21,9,10,27

Elevated cholesterol levels, and in particular, elevated low-density lipoprotein (LDL) levels, are an important risk factor for the development of CVD.9 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.13,14,15,16,17 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.9,10 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.21,19,20 Clinical studies have shown that atorvastatin reduces LDL-C and total cholesterol by 36-53%.3

In patients with dysbetalipoproteinemia, atorvastatin has been shown to reduce the intermediate-density lipoprotein cholesterol.2 It has also been suggested that atorvastatin can reduce angiogenesis which can be useful in the treatment of chronic subdural hematoma.1

Myopathy/Rhabdomyolysis

Atorvastatin, like other inhibitors of HMG-CoA reductase, occasionally causes myopathy manifested as muscle pain, tenderness or weakness with creatine kinase (CK) above ten times the upper limit of normal (ULN). Myopathy sometimes takes the form of rhabdomyolysis with or without acute renal failure secondary to myoglobinuria, and rare fatalities have occurred. The risk of myopathy is dose-related and is increased by high levels of HMG-CoA reductase inhibitory activity in plasma.

Predisposing factors for myopathy include advanced age (≥65 years), female gender, uncontrolled hypothyroidism, and renal impairment. Chinese patients may also be at increased risk for myopathy. In most cases, muscle symptoms and CK increases resolved when treatment was promptly discontinued.

The risk of myopathy during treatment with lovastatin may be increased with concurrent administration of interacting drugs such as fenofibrate, niacin, gemfibrozil, cyclosporine, and strong inhibitors of the CYP3A4 enzyme. Cases of myopathy, including rhabdomyolysis, have been reported with HMG-CoA reductase inhibitors coadministered with colchicine, and caution should therefore be exercised when prescribing these two medications together.38,39

Real-world data from observational studies has suggested that 10-15% of people taking statins may experience muscle aches at some point during treatment.30

Liver Dysfunction

Statins, like some other lipid-lowering therapies, have been associated with biochemical abnormalities of liver function. Persistent elevations (> 3 times the upper limit of normal [ULN] occurring on two or more occasions) in serum transaminases occurred in 0.7% of patients who received atorvastatin in clinical trials. This effect appears to be dose-related.38,39

Endocrine Effects

Increases in HbA1c and fasting serum glucose levels have been reported with HMG-CoA reductase inhibitors, including atorvastatin.

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.7

HMG-CoA reductase inhibitors interfere with cholesterol synthesis and as such might theoretically blunt adrenal and/or gonadal steroid production. Clinical studies with atorvastatin and other HMG-CoA reductase inhibitors have suggested that these agents do not reduce plasma cortisol concentration or impair adrenal reserve and do not reduce basal plasma testosterone concentration. However, the effects of HMG-CoA reductase inhibitors on male fertility have not been studied in adequate numbers of patients. The effects, if any, on the pituitary-gonadal axis in premenopausal women are unknown.39

Cardiovascular

Significant decreases in circulating ubiquinone levels in patients treated with atorvastatin and 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.39

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 Lp(a) lipoprotein concentrations. Present knowledge suggests the importance of high Lp(a) levels as an emerging risk factor for coronary heart disease.39 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.28

Mechanism of action

Atorvastatin 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.1,8 Atorvastatin 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. Atorvastatin also reduces Very Low Density Lipoprotein-Cholesterol (VLDL-C), serum triglycerides (TG) and Intermediate Density Lipoproteins (IDL), as well as the number of apolipoprotein B (apo B) containing particles, but increases High Density Lipoprotein Cholesterol (HDL-C).

In vitro and in vivo animal studies also demonstrate that atorvastatin 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.29

TargetActionsOrganism
A3-hydroxy-3-methylglutaryl-coenzyme A reductase
inhibitor
Humans
UDipeptidyl peptidase 4
inhibitor
Humans
UAryl hydrocarbon receptor
agonist
Humans
UHistone deacetylase 2
inhibitor
Humans
UNuclear receptor subfamily 1 group I member 3
ligand
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

Atorvastatin presents a dose-dependent and non-linear pharmacokinetic profile.4 It is very rapidly absorbed after oral administration. After the administration of a dose of 40 mg, its peak plasma concentration of 28 ng/ml is reached 1-2 hours after initial administration with an AUC of about 200 ng∙h/ml.6 Atorvastatin undergoes extensive first-pass metabolism in the wall of the gut and the liver, resulting in an absolute oral bioavailability of 14%.2 Plasma atorvastatin concentrations are lower (approximately 30% for Cmax and AUC) following evening drug administration compared with morning. However, LDL-C reduction is the same regardless of the time of day of drug administration.38

Administration of atorvastatin with food results in prolonged Tmax and a reduction in Cmax and AUC.3

Breast Cancer Resistance Protein (BCRP) is a membrane-bound protein that plays an important role in the absorption of atorvastatin.26 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 1.72-fold higher AUC for atorvastatin 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.31,32 Other statin drugs impacted by this polymorphism include fluvastatin, simvastatin, and rosuvastatin.31

Genetic differences in the OATP1B1 (organic-anion-transporting polypeptide 1B1) hepatic transporter encoded by the SCLCO1B1 gene (Solute Carrier Organic Anion Transporter family member 1B1) have been shown to impact atorvastatin pharmacokinetics. Evidence from pharmacogenetic studies of the c.521T>C single nucleotide polymorphism (SNP) in the gene encoding OATP1B1 (SLCO1B1) demonstrated that atorvastatin AUC was increased 2.45-fold for individuals homozygous for 521CC compared to homozygous 521TT individuals.[A181493] Other statin drugs impacted by this polymorphism include simvastatin, pitavastatin, rosuvastatin, and pravastatin.26

Volume of distribution

The reported volume of distribution of atorvastatin is of 380 L.38,39

Protein binding

Atorvastatin is highly bound to plasma proteins and over 98% of the administered dose is found in a bound form.38,39

Metabolism

Atorvastatin is highly metabolized to ortho- and parahydroxylated derivatives and various beta-oxidation products, primarily by Cytochrome P450 3A4 in the intestine and liver.38,39 Atorvastatin's metabolites undergo further lactonization via the formation of acyl glucuronide intermediates by the enzymes UGT1A1 and UGT1A3. These lactones can be hydrolyzed back to their corresponding acid forms and exist in equilibirum.5,26

In vitro inhibition of HMG-CoA reductase by ortho- and parahydroxylated metabolites is equivalent to that of atorvastatin. Approximately 70% of circulating inhibitory activity for HMG-CoA reductase is attributed to active metabolites.38,39

Route of elimination

Atorvastatin and its metabolites are mainly eliminated in the bile without enterohepatic recirculation. The renal elimination of atorvastatin is very minimal and represents less than 1% of the eliminated dose.38,39

Half life

The half-life of atorvastatin is 14 hours while the half-life of its metabolites can reach up to 30 hours.38,39

Clearance

The registered total plasma clearance of atorvastatin is of 625 ml/min.5

Toxicity

The reported LD50 of oral atorvastatin in mice is higher than 5000 mg/kg.MSDS In cases of overdose with atorvastatin, there is reported symptoms of complicated breathing, jaundice, liver damage, dark urine, muscle pain, and seizures.37 In case of overdose, symptomatic treatment is recommended and due to the high plasma protein binding, hemodialysis is not expected to generate significant improvement.Label

In carcinogenic studies with high doses of atorvastatin, evidence of rhabdomyosarcoma, fibrosarcoma, liver adenoma, and liver carcinoma were observed.Label

In fertility studies with high doses of atorvastatin, there were events of aplasia, aspermia, low testis and epididymal weight, decreased sperm motility, decreased spermatid head concentration and increased abnormal sperm.Label

Atorvastatin was shown to not be mutagenic in diverse mutagenic assays.Label

Affected organisms
  • Humans and other mammals
Pathways
Not Available
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 atorvastatin.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 atorvastatin.Details
Cytochrome P450 3A4CYP3A4*1B(A;G) / (G;G)A > GEffect Directly StudiedPatients with this genotype have an greater reduction in LDL cholesterol with atorvastatin.Details

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Atorvastatin.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Atorvastatin.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Atorvastatin.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Atorvastatin.
4-MethoxyamphetamineThe metabolism of 4-Methoxyamphetamine can be decreased when combined with Atorvastatin.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Atorvastatin.
6-Deoxyerythronolide BThe risk or severity of adverse effects can be increased when 6-Deoxyerythronolide B is combined with Atorvastatin.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Atorvastatin.
7-ethyl-10-hydroxycamptothecinThe metabolism of Atorvastatin can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
9-aminocamptothecinThe metabolism of 9-aminocamptothecin can be decreased when combined with Atorvastatin.
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
  • Avoid alcohol.
  • Avoid drastic changes in dietary habit.
  • Avoid taking grapefruit or grapefruit juice throughout treatment. Grapefruit can significantly increase serum levels of this product.
  • Food may decrease maximum plasma levels and area under the curve, but this is clinically inconsequential according to the manufacturer.
  • Take with low fat meal.

References

Synthesis Reference
US20020183527
General References
  1. Qiu S, Zhuo W, Sun C, Su Z, Yan A, Shen L: Effects of atorvastatin on chronic subdural hematoma: A systematic review. Medicine (Baltimore). 2017 Jun;96(26):e7290. doi: 10.1097/MD.0000000000007290. [PubMed:28658127]
  2. McIver LA, Siddique MS: Atorvastatin . [PubMed:28613530]
  3. Ye YC, Zhao XL, Zhang SY: Use of atorvastatin in lipid disorders and cardiovascular disease in Chinese patients. Chin Med J (Engl). 2015 Jan 20;128(2):259-66. doi: 10.4103/0366-6999.149226. [PubMed:25591572]
  4. Ray SK, Rege NN: Atorvastatin: in the management of hyperlipidaemia. J Postgrad Med. 2000 Jul-Sep;46(3):242-3. [PubMed:11298482]
  5. Lennernas H: Clinical pharmacokinetics of atorvastatin. Clin Pharmacokinet. 2003;42(13):1141-60. [PubMed:14531725]
  6. Lins RL, Matthys KE, Verpooten GA, Peeters PC, Dratwa M, Stolear JC, Lameire NH: Pharmacokinetics of atorvastatin and its metabolites after single and multiple dosing in hypercholesterolaemic haemodialysis patients. Nephrol Dial Transplant. 2003 May;18(5):967-76. [PubMed:12686673]
  7. 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]
  8. 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]
  9. 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]
  10. 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]
  11. 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]
  12. 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]
  13. 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]
  14. 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]
  15. 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]
  16. 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]
  17. 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]
  18. Authors unspecified: Randomised trial of cholesterol lowering in 4444 patients with coronary heart disease: the Scandinavian Simvastatin Survival Study (4S) Lancet. 1994 Nov 19;344(8934):1383-9. [PubMed:7968073]
  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. Henwood JM, Heel RC: Lovastatin. A preliminary review of its pharmacodynamic properties and therapeutic use in hyperlipidaemia. Drugs. 1988 Oct;36(4):429-54. doi: 10.2165/00003495-198836040-00003. [PubMed:3069436]
  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. Pedersen TR, Faergeman O, Kastelein JJ, Olsson AG, Tikkanen MJ, Holme I, Larsen ML, Bendiksen FS, Lindahl C, Szarek M, Tsai J: High-dose atorvastatin vs usual-dose simvastatin for secondary prevention after myocardial infarction: the IDEAL study: a randomized controlled trial. JAMA. 2005 Nov 16;294(19):2437-45. doi: 10.1001/jama.294.19.2437. [PubMed:16287954]
  24. 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]
  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. 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]
  27. Bradford RH, Shear CL, Chremos AN, Dujovne CA, Franklin FA, Grillo RB, Higgins J, Langendorfer A, Nash DT, Pool JL, et al.: Expanded Clinical Evaluation of Lovastatin (EXCEL) study results: two-year efficacy and safety follow-up. Am J Cardiol. 1994 Oct 1;74(7):667-73. doi: 10.1016/0002-9149(94)90307-7. [PubMed:7942524]
  28. 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]
  29. 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]
  30. 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]
  31. 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]
  32. 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]
  33. Corey E., Czako B. and Kurti L. (2007). Molecules and medicine. John Wiley & Sons, Inc. [ISBN:978-0-470-26096-8]
  34. Kumar R. and Bandichhor R. (2018). Hazardous reagent substitution. A pharmaceutical perspective. The Royal Society of Chemistry. [ISBN:978-1-78262-050-1]
  35. Merck Manuals [Link]
  36. Chemocare [Link]
  37. Laguna Treatment [Link]
  38. FDA Label - Atorvastatin [File]
  39. Health Canada Monograph - Atorvastatin [File]
External Links
Human Metabolome Database
HMDB0005006
KEGG Drug
D07474
KEGG Compound
C06834
PubChem Compound
60823
PubChem Substance
46506188
ChemSpider
54810
BindingDB
22164
ChEBI
39548
ChEMBL
CHEMBL1487
Therapeutic Targets Database
DAP000553
PharmGKB
PA448500
HET
117
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Atorvastatin
ATC Codes
C10BX15 — Atorvastatin and perindoprilC10AA05 — AtorvastatinC10BX03 — Atorvastatin and amlodipineC10BA05 — Atorvastatin and ezetimibeC10BX11 — Atorvastatin, amlodipine and perindoprilC10BX08 — Atorvastatin and acetylsalicylic acidC10BX06 — Atorvastatin, acetylsalicylic acid and ramiprilC10BX12 — Atorvastatin, acetylsalicylic acid and perindopril
AHFS Codes
  • 24:06.08 — Hmg-coa Reductase Inhibitors
PDB Entries
1hwk
FDA label
Download (387 KB)
MSDS
Download (56.5 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingBasic ScienceObstructive Sleep Apnea of Adult1
0RecruitingTreatmentCancer of the Breast / Cancer, Breast / Tumors, Breast1
0RecruitingTreatmentEndometrial Cancers1
0Unknown StatusPreventionStroke, Ischemic / Ventilator-Associated Pneumonia (VAP)1
1Active Not RecruitingTreatmentHealthy Male Subjects1
1CompletedNot AvailableAcute Coronary Syndromes (ACS)1
1CompletedNot AvailableEffect of Atorvastatin on the Pharmacokinetics of Lomitapide1
1CompletedNot AvailableHealthy Volunteers5
1CompletedNot AvailableHealthy Volunteers / Pharmacokinetics of Atorvastatin1
1CompletedNot AvailableHealthy Volunteers / Pharmacokinetics of Atorvastatin / Pharmacokinetics of Isavuconazole1
1CompletedNot AvailableHigh Blood Pressure (Hypertension)1
1CompletedNot AvailableHigh Cholesterol3
1CompletedNot AvailableHigh Cholesterol / Human Immunodeficiency Virus (HIV)1
1CompletedNot AvailableHuman Immunodeficiency Virus (HIV) Infections1
1CompletedNot AvailableHypertension,Essential1
1CompletedNot AvailablePediatric Heterozygous Hypercholesterolemia1
1CompletedBasic ScienceCoronary Heart Disease (CHD)1
1CompletedBasic ScienceDiabetes Mellitus (DM) / Healthy Volunteers1
1CompletedBasic ScienceDrug Interaction Potentiation1
1CompletedBasic ScienceDyslipidemias1
1CompletedBasic ScienceHealthy Volunteers4
1CompletedBasic ScienceHealthy Volunteers / Pharmacokinetics1
1CompletedBasic ScienceHigh Cholesterol1
1CompletedDiagnosticOsteoarthritis (OA) / Osteoporosis1
1CompletedHealth Services ResearchHealthy Controls1
1CompletedOtherDiabete Mellitus1
1CompletedOtherHealthy Volunteers2
1CompletedPreventionAtypical Ductal Breast Hyperplasia / Cancer, Breast / Ductal Breast Carcinoma In Situ / Lobular Breast Carcinoma In Situ1
1CompletedTreatmentAcute Coronary Syndromes (ACS) / Inflammatory Reaction / Myocardial Infarction / Reperfusion Injury1
1CompletedTreatmentAcute and Chronic Inflammation / Autoimmune Diseases / Disorder of Pleura and Pleural Cavity / Disorder of Synovium / Felty's Syndrome / Rheumatoid Arthritis / Rheumatoid Nodules / Sjögren's Syndrome1
1CompletedTreatmentAtherosclerotic Vascular Diseases1
1CompletedTreatmentAutoimmune Diseases / Disseminated or Multiple Sclerosis Nos / Disseminated Sclerosis / Multiple Sclerosis, Acute Relapsing / Multiple Sclerosis, Chronic Progressive / Multiple Sclerosis, Primary Progressive1
1CompletedTreatmentCholesterol, LDL / High Cholesterol1
1CompletedTreatmentDiabetes Mellitus (DM) / Healthy Volunteers1
1CompletedTreatmentDiseases of the Circulatory System / Hypertension,Essential1
1CompletedTreatmentDyslipidemia (Fredrickson Type Ⅱa) / Dyslipidemia (Fredrickson Type Ⅱb)1
1CompletedTreatmentDyslipidemias2
1CompletedTreatmentEnd-Stage Kidney Disease1
1CompletedTreatmentEndometriosis / Prostate Cancer1
1CompletedTreatmentEpilepsies1
1CompletedTreatmentHIV Seronegativity / Human Immunodeficiency Virus (HIV) Infections / Lipodystrophies1
1CompletedTreatmentHealthy Participants1
1CompletedTreatmentHealthy Volunteers18
1CompletedTreatmentHealthy Volunteers / Normocholesterolaemic Men / Normozoospermic Men1
1CompletedTreatmentHigh Blood Pressure (Hypertension) / Hyperlipidemias2
1CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections1
1CompletedTreatmentHyperlipidemias1
1CompletedTreatmentHyperlipidemias / Hypertension,Essential2
1CompletedTreatmentHypertension With Hyperlipidemia / Hypertention With Hyperlipidemia1
1CompletedTreatmentHypertension, Hyperlipidemia1
1CompletedTreatmentImpaired Renal Function1
1CompletedTreatmentPharmacokinetics1
1CompletedTreatmentSleep disorders and disturbances1
1Not Yet RecruitingNot AvailableHealthy Male Subjects1
1Not Yet RecruitingTreatmentHIV-1-infection1
1RecruitingTreatmentLeukemia Acute Myeloid Leukemia (AML) / Malignant Diseases / Tumors, Solid1
1TerminatedDiagnosticPeripheral Arterial Disease (PAD)1
1TerminatedTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
1Unknown StatusTreatmentHealthy Volunteers1
1Unknown StatusTreatmentPlasma Cell Myeloma1
1Unknown StatusTreatmentStrokes1
1WithdrawnBasic ScienceAdvanced Adenocarcinoma of the Colon or Rectum1
1, 2CompletedTreatmentMetabolic Syndromes1
1, 2CompletedTreatmentMucocutaneous Lymph Node Syndrome1
1, 2CompletedTreatmentSystemic Lupus Erythematosus (SLE)1
1, 2Enrolling by InvitationBasic ScienceSleep Apnea, Obstructive1
1, 2Not Yet RecruitingTreatmentEbola Virus Disease1
1, 2Not Yet RecruitingTreatmentImmune Thrombocytopenia1
1, 2RecruitingPreventionPrimary Arteriovenous Fistula Failure1
1, 2RecruitingTreatmentCerebral Cavernous Malformations1
1, 2RecruitingTreatmentNon-segmental Vitiligo1
1, 2RecruitingTreatmentVenous Thromboembolism (VTE)1
1, 2TerminatedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Hyperlipidemias1
1, 2Unknown StatusTreatmentMetabolic Syndromes1
1, 2Unknown StatusTreatmentStenosis1
2Active Not RecruitingPreventionAdult Acute Lymphoblastic Leukemia / Adult Acute Myeloid Leukemia / Adult Diffuse Large B-Cell Lymphoma / Aggressive Non-Hodgkin Lymphoma / Aggressive, recurrent Adult Non-Hodgkin Lymphoma / Blasts Under 5 Percent of Bone Marrow Nucleated Cells / Childhood Acute Lymphoblastic Leukemia / Childhood Acute Myeloid Leukemia / Childhood Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Childhood Diffuse Large B -Cell Lymphoma / Chronic Lymphocytic Leukaemia (CLL) / Chronic Lymphocytic Leukemia (CLL) - Refractory / Chronic, recurrent Lymphocytic Leukemia / DS Stage I Plasma Cell Myeloma / DS Stage II Plasma Cell Myeloma / DS Stage III Plasma Cell Myeloma / Leukemia, Prolymphocytic / Loss of Chromosome 17p / Myelodysplastic/Myeloproliferative Neoplasms / Non-Hodgkin's Lymphoma (NHL) / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent Adult Acute Myeloid Leukemia / Recurrent Childhood Acute Lymphoblastic Leukemia / Recurrent Childhood Acute Myeloid Leukemia / Recurrent Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Recurrent Diffuse Large B-Cell Lymphoma / Recurrent Hodgkin Lymphoma / Recurrent Mantle Cell Lymphoma / Recurrent Non-Hodgkin Lymphoma / Recurrent Plasma Cell Myeloma / Recurrent Small Lymphocytic Lymphoma / Refractory Childhood Hodgkin Lymphoma / Refractory Chronic Myelogenous Leukemia, BCR-ABL1 Positive / Stage I Adult Hodgkin Lymphoma / Stage I Aggressive Adult Non-Hodgkin Lymphoma / Stage I Childhood Hodgkin Lymphoma / Stage I Chronic Lymphocytic Leukemia / Stage I Diffuse Large B-Cell Lymphoma / Stage I Mantle Cell Lymphoma / Stage I Small Lymphocytic Lymphoma / Stage II Adult Hodgkin Lymphoma / Stage II Childhood Hodgkin Lymphoma / Stage II Chronic Lymphocytic Leukemia / Stage II Contiguous Adult Aggressive Non-Hodgkin Lymphoma / Stage II Contiguous Mantle Cell Lymphoma / Stage II Diffuse Large B-Cell Lymphoma / Stage II Non-Contiguous Aggressive Adult Non-Hodgkin Lymphoma / Stage II Non-Contiguous Mantle Cell Lymphoma / Stage II Small Lymphocytic Lymphoma / Stage III Adult Hodgkin Lymphoma / Stage III Aggressive Adult Non-Hodgkin Lymphoma / Stage III Childhood Hodgkin Lymphoma / Stage III Chronic Lymphocytic Leukemia / Stage III Diffuse Large B-Cell Lymphoma / Stage III Mantle Cell Lymphoma / Stage III Small Lymphocytic Lymphoma / Stage IV Adult Hodgkin Lymphoma / Stage IV Aggressive Adult Non-Hodgkin Lymphoma / Stage IV Childhood Hodgkin Lymphoma / Stage IV Chronic Lymphocytic Leukemia / Stage IV Diffuse Large B-Cell Lymphoma / Stage IV Mantle Cell Lymphoma / Stage IV Small Lymphocytic Lymphoma / T-cell chronic lymphocytic leukaemia / T-Cell Prolymphocytic Leukemia / Waldenström's Macroglobulinemia (WM)1
2Active Not RecruitingPreventionCancer, Breast1
2Active Not RecruitingPreventionGraft Versus Host Disease (GVHD)1
2Active Not RecruitingTreatmentHuman Immunodeficiency Virus (HIV) / Human Immunodeficiency Virus (HIV) Infections1
2Active Not RecruitingTreatmentScleroderma1
2Active Not RecruitingTreatmentSpastic Paraplegia, Hereditary1
2CompletedBasic ScienceHuman Immunodeficiency Virus (HIV)1
2CompletedDiagnosticHealthy Volunteers1
2CompletedPreventionAlzheimer's Disease (AD)1
2CompletedPreventionDisseminated Sclerosis1
2CompletedPreventionHigh Blood Pressure (Hypertension) / Hyperlipidemias1
2CompletedPreventionHip Fractures / Inflammatory Reaction / Myocardial Ischemia1
2CompletedPreventionMalignant Neoplasm of Colon / Precancerous Conditions / Rectal Carcinoma1
2CompletedPreventionMetabolic Syndromes1
2CompletedPreventionProstatic Neoplasms1
2CompletedPreventionProphylaxis of Contrast-induced nephropathy1
2CompletedSupportive CareAcute Lymphocytic Leukemia (ALL) / Acute Myelogenous Leukaemia (AML) / Myelodysplastic Syndrome1
2CompletedSupportive CareNeoplasms, Malignant1
2CompletedTreatmentALL, Childhood / Cardiovascular Disease (CVD) / Childhood NHL1
2CompletedTreatmentAcute Coronary Syndromes (ACS)1
2CompletedTreatmentAlzheimer's Disease (AD)1
2CompletedTreatmentAngioplasty, Transluminal, Percutaneous Coronary / Myocardial Infarction / Transplantation, Stem Cell1
2CompletedTreatmentAsthma Bronchial / Chronic Obstructive Pulmonary Disease (COPD) / Smoking1
2CompletedTreatmentCancer, Breast / One to five years postmenopausal1
2CompletedTreatmentCardiovascular Disease (CVD)1
2CompletedTreatmentCardiovascular Disease (CVD) / Diabetes Mellitus (DM) / Renal Dysfunction1
2CompletedTreatmentCardiovascular Disease (CVD) / Renal Dysfunction2
2CompletedTreatmentCarotid Atherosclerosis1
2CompletedTreatmentChronic Subdural Hematomas1
2CompletedTreatmentCrohns Disease1
2CompletedTreatmentDiabetes Mellitus (DM)1
2CompletedTreatmentDiabetes Mellitus (DM) / High Cholesterol / Metabolic Syndromes1
2CompletedTreatmentDiabetes Mellitus (DM) / Ulcus Cruris1
2CompletedTreatmentDisseminated Sclerosis1
2CompletedTreatmentDyslipidemias8
2CompletedTreatmentFlu caused by Influenza1
2CompletedTreatmentGlioblastoma Multiforme (GBM)1
2CompletedTreatmentGlomerulosclerosis, Focal Segmental1
2CompletedTreatmentHepatitis C Viral Infection1
2CompletedTreatmentHigh Cholesterol12
2CompletedTreatmentHigh Cholesterol / Hyperlipidemias / Muscle Soreness1
2CompletedTreatmentHuman Immunodeficiency Virus Type 1 (HIV-1) Infection1
2CompletedTreatmentHyperlipidemias5
2CompletedTreatmentKnee Osteoarthritis (Knee OA)1
2CompletedTreatmentLeukemias / Non-Hodgkin's Lymphoma (NHL)1
2CompletedTreatmentNonalcoholic Steatohepatitis1
2CompletedTreatmentPlatelets Dysfunction1
2CompletedTreatmentPolycystic Ovaries Syndrome1
2CompletedTreatmentProstate Cancer1
2CompletedTreatmentPsoriasis1
2CompletedTreatmentPulmonary Hypertension (PH)1
2CompletedTreatmentRenal Cancers / Renal Cell Adenocarcinoma1
2CompletedTreatmentRheumatoid Arthritis1
2CompletedTreatmentSarcoidosis, Pulmonary1
2CompletedTreatmentSickle Cell Disorders / Sickle Cell Nephropathy1
2CompletedTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
2CompletedTreatmentVascular Diseases1
2CompletedTreatmentVitiligo1
2Not Yet RecruitingTreatmentAdenocarcinoma, Prostate / Erectile Dysfunction (ED) / Erectile Dysfunction, CTCAE1
2Not Yet RecruitingTreatmentAngioplasty, Transluminal, Percutaneous Coronary / Myocardial Infarction / Transplantation, Stem Cell1
2Not Yet RecruitingTreatmentChronic Subdural Hematomas1
2Not Yet RecruitingTreatmentDyslipidemias1
2Not Yet RecruitingTreatmentHigh Cholesterol / Thyroid Associated Ophthalmopathy1
2Not Yet RecruitingTreatmentNeoplasms, Breast1
2Not Yet RecruitingTreatmentProstate Cancer1
2RecruitingPreventionCardiotoxicity / Heart Failure / Malignancies1
2RecruitingPreventionCoronary Artery Disease1
2RecruitingPreventionHigh Cholesterol1
2RecruitingTreatmentAnatomic Stage IIB Breast Cancer AJCC v8 / Anatomic Stage III Breast Cancer AJCC v8 / Anatomic Stage IIIA Breast Cancer AJCC v8 / Anatomic Stage IIIB Breast Cancer AJCC v8 / Anatomic Stage IIIC Breast Cancer AJCC v8 / Estrogen Receptor Negative / HER2/Neu Negative / Inflammatory Breast Carcinoma / Progesterone Receptor Negative / Prognostic Stage IIB Breast Cancer AJCC v8 / Prognostic Stage III Breast Cancer AJCC v8 / Prognostic Stage IIIA Breast Cancer AJCC v8 / Prognostic Stage IIIB Breast Cancer AJCC v8 / Prognostic Stage IIIC Breast Cancer AJCC v8 / Stage IIB Breast Cancer AJCC v6 and v7 / Stage III Breast Cancer AJCC V7 / Stage IIIA Breast Cancer AJCC v7 / Stage IIIB Breast Cancer AJCC v7 / Stage IIIC Breast Cancer AJCC v7 / Triple-Negative Breast Carcinoma1
2RecruitingTreatmentBipolar Disorder (BD) / Lithium Use, Nephrogenic Diabetes Insipidus1
2RecruitingTreatmentCancer, Breast1
2RecruitingTreatmentClinical Outcome Improvement / Overall Survival / Tumor Responses1
2RecruitingTreatmentDyslipidemias / High Cholesterol1
2RecruitingTreatmentHeart Failure1
2RecruitingTreatmentHigh Blood Pressure (Hypertension)1
2RecruitingTreatmentNon-Alcoholic Steatohepatitis1
2RecruitingTreatmentTriple Negative Breast Cancer (TNBC)1
2SuspendedPreventionNasopharyngeal Carcinoma / Radiation Therapy Complication1
2TerminatedBasic ScienceCoronary Artery Disease / Dyslipidemias1
2TerminatedPreventionAvascular Necrosis1
2TerminatedTreatmentAsthma Bronchial1
2TerminatedTreatmentCancer, Breast / Cardiotoxicity / Heart Diseases / Myocardial Dysfunction1
2TerminatedTreatmentGlomerulonephritis minimal lesion / Hyperlipidemias1
2TerminatedTreatmentHigh Cholesterol / Venous Thromboembolism (VTE)1
2TerminatedTreatmentMild Traumatic Brain Injury (MTBI) / Post Traumatic Stress Disorder (PTSD) / Traumatic Brain Injury (TBI)1
2TerminatedTreatmentObstructive Sleep Apnea Syndrome (OSAS)1
2Unknown StatusPreventionAcute Non-ST-segment Elevation Myocardial Infarction / Stable Angina (SA) / Unstable Angina Pectoris1
2Unknown StatusPreventionCancer, Breast1
2Unknown StatusPreventionGraft Versus Host Disease (GVHD)1
2Unknown StatusPreventionProstatic Neoplasms1
2Unknown StatusTreatmentAneurysm, Coronary / Mucocutaneous Lymph Node Syndrome1
2Unknown StatusTreatmentSepsis1
2, 3CompletedPreventionMyocardial Infarction / Renal Failure / Strokes1
2, 3CompletedPreventionProphylaxis of Contrast-induced nephropathy1
2, 3CompletedTreatmentAcute Kidney Dysfunction1
2, 3CompletedTreatmentArterial Occlusive Diseases / Insulin Resistance / Intermittent Claudication1
2, 3CompletedTreatmentAsthma Bronchial1
2, 3CompletedTreatmentChronic Periodontitis Wth Diabetes Mellitus1
2, 3CompletedTreatmentDyslipidemias1
2, 3CompletedTreatmentPeriodontitis, Chronic4
2, 3RecruitingPreventionCognitively Normal Older Adults / Family History of Alzheimer's Disease / High Blood Pressure (Hypertension) / Subjective Cognitive Decline1
2, 3RecruitingTreatmentHyperlipidemias1
2, 3TerminatedTreatmentAdvanced Cancers1
2, 3Unknown StatusTreatmentSystemic Lupus Erythematosus (SLE)1
2, 3WithdrawnTreatmentHuman Immunodeficiency Virus Infection(HIV)/Acquired Immunodeficiency Syndrome (AIDS) / Immune Reconstitution Inflammatory Syndrome / Immune Reconstitution Syndrome / Tuberculosis Infection1
3Active Not RecruitingPreventionCardiovascular Disease (CVD) / Coronary Artery Disease / Type 2 Diabetes Mellitus1
3Active Not RecruitingTreatmentBicuspid Aortic Valve (BAV)1
3Active Not RecruitingTreatmentCardiovascular Risk Factors / Dyslipidemias1
3Active Not RecruitingTreatmentCoronary Artery Disease1
3Active Not RecruitingTreatmentDyslipidemia (Fredrickson Type Ⅱa)1
3Active Not RecruitingTreatmentEssential Hypertension, Dyslipidemia1
3Active Not RecruitingTreatmentHigh Cholesterol2
3CompletedPreventionAortic Aneurism / Myocardial Infarction / Peripheral Vascular Disease (PVD)1
3CompletedPreventionCoronary Artery Disease1
3CompletedPreventionHeart Valve Diseases1
3CompletedPreventionMyocardial Oedema1
3CompletedPreventionType 1 Insulin-Dependent Diabetes Mellitus1
3CompletedPreventionProphylaxis of preeclampsia1
3CompletedTreatmentAcute Coronary Syndromes (ACS)2
3CompletedTreatmentAlzheimer's Disease (AD)1
3CompletedTreatmentAssess the Periprocedural Myocardial Necrosis1
3CompletedTreatmentAtherosclerosis3
3CompletedTreatmentAtherosclerosis / Calcifications, Vascular / Dyslipidemias / Inflammatory Reaction1
3CompletedTreatmentAtherosclerosis / Cardiovascular Disease (CVD)1
3CompletedTreatmentAtherosclerosis / Coronary Artery Disease / High Cholesterol1
3CompletedTreatmentAtherosclerotic Disease / Coronary Heart Disease (CHD) / High Cholesterol1
3CompletedTreatmentBMI >30 kg/m2 / Dyslipidemias1
3CompletedTreatmentBMI >30 kg/m2 / Dyslipidemias / Insulin Resistance1
3CompletedTreatmentCardiovascular Disorders / Diabetes Mellitus (DM)1
3CompletedTreatmentChronic Kidney Disease (CKD)1
3CompletedTreatmentCombined (Atherogenic) Dyslipidemia / Coronary Heart Disease (CHD) / Dyslipidemias / Mixed hypercholesterolemia1
3CompletedTreatmentCombined Dyslipidemia1
3CompletedTreatmentCoronary Arteriosclerosis / Coronary Heart Disease (CHD) / Hyperlipidemias1
3CompletedTreatmentCoronary Artery Atherosclerosis1
3CompletedTreatmentCoronary Heart Disease (CHD) / Dyslipidemias / Mixed hypercholesterolemia2
3CompletedTreatmentCoronary Heart Disease (CHD) / High Cholesterol1
3CompletedTreatmentDiabetes Mellitus, Insulin-Dependent / High Cholesterol1
3CompletedTreatmentDiabetes, Hyperlipidemia, Mixed Dyslipidemia1
3CompletedTreatmentDyslipidemia (Fredrickson Type Ⅱa)3
3CompletedTreatmentDyslipidemia (Fredrickson Type Ⅱa) / Dyslipidemias1
3CompletedTreatmentDyslipidemia (Fredrickson Type Ⅱa) / Hyperlipidemias2
3CompletedTreatmentDyslipidemia (Fredrickson Type Ⅱa) / Mixed hypercholesterolemia1
3CompletedTreatmentDyslipidemias1
3CompletedTreatmentDyslipidemias / High Blood Pressure (Hypertension)1
3CompletedTreatmentDyslipidemias / High Cholesterol3
3CompletedTreatmentDyslipidemias / High Cholesterol / Hyperlipidemias1
3CompletedTreatmentDyslipidemias / Type 2 Diabetes Mellitus2
3CompletedTreatmentHeterozygous Familial Hypercholesterolemia1
3CompletedTreatmentHigh Cholesterol32
3CompletedTreatmentHigh Cholesterol / Metabolic Syndromes1
3CompletedTreatmentHigh Cholesterol / Primary Biliary Cholangitis1
3CompletedTreatmentHigh Cholesterol / Type 2 Diabetes Mellitus1
3CompletedTreatmentHypercholesterolemia in Coronaory Heart Disease1
3CompletedTreatmentHyperlipidemia or Mixed Dyslipidemia at High Risk for Cardiovascular Events1
3CompletedTreatmentHyperlipidemias10
3CompletedTreatmentHyperlipidemias / Hypertension,Essential1
3CompletedTreatmentHyperlipidemias / Mixed hypercholesterolemia1
3CompletedTreatmentHyperlipoproteinemia Type iv / Hypertriglyceridemias1
3CompletedTreatmentHypertriglyceridemias1
3CompletedTreatmentHypertrophic Cardiomyopathy1
3CompletedTreatmentImpaired Renal Function2
3CompletedTreatmentMetabolic Syndromes1
3CompletedTreatmentPrimary Hyperlipidemia and Mixed Dyslipidemia1
3CompletedTreatmentSystemic Lupus Erythematosus (SLE)1
3CompletedTreatmentType 2 Diabetes Mellitus2
3CompletedTreatmentMixed hypercholesterolemia2
3Not Yet RecruitingPreventionAcute Chest Syndrome1
3Not Yet RecruitingTreatmentAcute Coronary Syndromes (ACS) / Ischaemic Heart Diseases / Revascularization1
3Not Yet RecruitingTreatmentChronic Subdural Hematomas1
3Not Yet RecruitingTreatmentCoronary Artery Disease Progression1
3Not Yet RecruitingTreatmentHuman Immunodeficiency Virus (HIV) Infections1
3Not Yet RecruitingTreatmentMetastatic Hormone Refractory Prostate Cancer / Recurrent Prostate Cancer1
3Not Yet RecruitingTreatmentProstate Cancer1
3Not Yet RecruitingTreatmentStroke, Acute / Transient Ischaemic Attack (TIA)1
3RecruitingPreventionAcute Lymphocytic Leukemia (ALL) / Leukemia Acute Myeloid Leukemia (AML) / Myelodysplastic Syndrome1
3RecruitingPreventionCarotid Artery Stenosis / Strokes1
3RecruitingTreatmentAortic Valve Stenosis / Ventricular Hypertrophy1
3RecruitingTreatmentAtherosclerosis / Dyslipidemias1
3RecruitingTreatmentAtopic Dermatitis (AD)1
3RecruitingTreatmentCardiovascular Disease (CVD)1
3RecruitingTreatmentDyslipidemias / Type 2 Diabetes Mellitus1
3RecruitingTreatmentHigh Cholesterol2
3RecruitingTreatmentMalignancies / Overall Survival / Quality of Life1
3TerminatedPreventionInflammatory Reaction / Nonvalvular Atrial Fibrillation1
3TerminatedTreatmentAcute Coronary Syndromes (ACS) / Coronary Artery Disease1
3TerminatedTreatmentCardiovascular Disease (CVD)1
3TerminatedTreatmentCoronary Artery Disease / High Cholesterol1
3TerminatedTreatmentCoronary Heart Disease (CHD) / Diabetes Mellitus (DM)1
3TerminatedTreatmentDyslipidemias / High Cholesterol / Hyperlipidemias1
3TerminatedTreatmentDyslipidemias / Hyperlipidemias1
3TerminatedTreatmentHigh Cholesterol5
3TerminatedTreatmentHyperlipidemias1
3TerminatedTreatmentHyperlipoproteinemia Type III1
3TerminatedTreatmentStable Coronary Artery Disease Undergoing PCI1
3TerminatedTreatmentType 2 Diabetes Mellitus1
3TerminatedTreatmentMixed hypercholesterolemia1
3Unknown StatusPreventionContrast Induced Nephropathy (CIN)1
3Unknown StatusTreatmentAbdominal Surgeries1
3Unknown StatusTreatmentBranch Retinal Vein Occlusion / Central Retinal Vein Occlusion (CRVO) / Retinal Vein Occlusions(RVO) / Retinal Vein Thrombosis / Thrombotic events1
3Unknown StatusTreatmentCoronary Angioplasty / Coronary Artery Disease1
3Unknown StatusTreatmentHyperlipidemia, Familial Combined1
3Unknown StatusTreatmentHyperlipidemias1
3Unknown StatusTreatmentST Elevation Myocardial Infarction (STEMI)1
3Unknown StatusTreatmentStable Coronary Artery Disease1
3Unknown StatusTreatmentMixed hypercholesterolemia1
3WithdrawnTreatmentHypertriglyceridemias1
3WithdrawnTreatmentPsoriasis1
4Active Not RecruitingOtherAtherosclerosis / Carotid Artery Diseases / Coronary Artery Disease1
4Active Not RecruitingTreatmentChronic Kidney Disease (CKD)1
4Active Not RecruitingTreatmentDyslipidemias1
4Active Not RecruitingTreatmentHigh Cholesterol / Type 2 Diabetes Mellitus1
4CompletedNot AvailableAbdominal Aortic Aneurysms (AAA)1
4CompletedNot AvailableCardiovascular Disease (CVD) / Cholesterol, LDL / Cognition / Type 2 Diabetes Mellitus1
4CompletedNot AvailableDyslipidemias / Vascular Diseases1
4CompletedNot AvailableHealthy Volunteers3
4CompletedNot AvailableHigh Cholesterol4
4CompletedNot AvailablePrediabetic State1
4CompletedBasic ScienceAtherosclerosis / Coronary Artery Disease / Endothelial Dysfunction / HMG-CoA Reductase Inhibitor Toxicity / Oxidative Stress1
4CompletedBasic ScienceDrug intolerance1
4CompletedBasic ScienceHigh Cholesterol / Osteoporosis1
4CompletedBasic ScienceHyperlipidemias / Metabolic Syndromes / Renal Failure Chronic Requiring Hemodialysis / Type 2 Diabetes Mellitus1
4CompletedBasic SciencePeripheral Arterial Disease (PAD)1
4CompletedDiagnosticMuscular Diseases1
4CompletedDiagnosticMyopathies1
4CompletedDiagnosticMyotoxicity of Atorvastatin Treatment1
4CompletedPreventionAcute Coronary Syndromes (ACS)3
4CompletedPreventionAcute Kidney Injury (AKI) / Aortic Surgery1
4CompletedPreventionAging / Alzheimer's Disease (AD)1
4CompletedPreventionCardiac Insufficiency Following Cardiac Surgery / Disorder; Heart, Functional, Postoperative, Cardiac Surgery / Ischaemia-reperfusion Injury / Nonvalvular Atrial Fibrillation1
4CompletedPreventionCardiovascular Disease (CVD) / Cerebrovascular Accidents / Coronary Heart Disease (CHD)1
4CompletedPreventionCerebrovascular Accidents / Coronary Artery Bypass Graft Surgery Patients / Major Coronary Event / Revascularization / Unstable Angina Pectoris1
4CompletedPreventionContrast Induced Nephropathy (CIN)1
4CompletedPreventionCoronary Artery Bypass Graft Surgery Patients1
4CompletedPreventionEndothelial Dysfunction / Ischemia Reperfusion Injury1
4CompletedPreventionHemostasis / Inflammatory Reaction / Magnetic Resonance Imaging (MRI) / Neuropsychology / Nonvalvular Atrial Fibrillation1
4CompletedPreventionMyocardial Infarction1
4CompletedPreventionSystemic Lupus Erythematosus (SLE)1
4CompletedPreventionType 2 Diabetes Mellitus1
4CompletedScreeningInflammatory Reaction1
4CompletedTreatmentAcute Coronary Syndromes (ACS)1
4CompletedTreatmentAcute Coronary Syndromes (ACS) / Dyslipidemias1
4CompletedTreatmentAcute Coronary Syndromes (ACS) / High Cholesterol1
4CompletedTreatmentAcute Ischemic Stroke (AIS)1
4CompletedTreatmentAcute Myocardial Infarction (AMI)2
4CompletedTreatmentAging-related Inflammation in HIV-infected Patients1
4CompletedTreatmentAngina Pectoris / High Blood Pressure (Hypertension) / High Cholesterol1
4CompletedTreatmentAnginal Pain1
4CompletedTreatmentAngioplasty / Myocardial Infarction / Percutaneous Coronary1
4CompletedTreatmentArrythmias1
4CompletedTreatmentArrythmias / Endothelial Dysfunction / Inflammatory Reaction / Nonvalvular Atrial Fibrillation1
4CompletedTreatmentArteriosclerosis / Calcinosis / Hyperparathyroidism, Secondary1
4CompletedTreatmentAtherosclerosis1
4CompletedTreatmentAtherosclerosis / Coronary Artery Disease1
4CompletedTreatmentAtherosclerosis / Coronary Heart Disease (CHD) / Diabetes Mellitus (DM) / Dyslipidemias / Strokes1
4CompletedTreatmentAtherosclerosis / High Cholesterol1
4CompletedTreatmentBMI >30 kg/m2 / Cardiovascular Disease (CVD) / Hypertriglyceridemias / Lipid Disorders1
4CompletedTreatmentBronchiectasis2
4CompletedTreatmentCVD1
4CompletedTreatmentCardiovascular Disease (CVD)2
4CompletedTreatmentCardiovascular Disease (CVD) / Dyslipidemias / High Cholesterol1
4CompletedTreatmentCardiovascular Disease (CVD) / Heart Diseases / Myocardial Diseases / Myocardial Ischemia / Prophylaxis of cardiomyopathy1
4CompletedTreatmentCardiovascular Disease (CVD) / Ischemia Reperfusion Injury1
4CompletedTreatmentCerebrovascular Accidents / Coronary Arteriosclerosis / Dyslipidemias / Peripheral Vascular Disease (PVD) / Type 2 Diabetes Mellitus2
4CompletedTreatmentCerebrovascular Accidents / High Cholesterol1
4CompletedTreatmentChronic Kidney Disease (CKD)1
4CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD)1
4CompletedTreatmentChronic Periaortitis / Intrabony Periodontal Defect1
4CompletedTreatmentChronic Stable Angina Pectoris / Non ST Segment Elevation Myocardial Infarction (NSTEMI) / Unstable Angina Pectoris1
4CompletedTreatmentComplete Occlusion of Coronary Artery / Hibernation, Myocardial1
4CompletedTreatmentCongestive Heart Failure (CHF)1
4CompletedTreatmentCoronary Arteriosclerosis1
4CompletedTreatmentCoronary Arteriosclerosis / High Cholesterol2
4CompletedTreatmentCoronary Artery Bypass Graft Surgery Patients / Elective Surgical Procedure1
4CompletedTreatmentCoronary Artery Disease1
4CompletedTreatmentCoronary Artery Disease / High Cholesterol3
4CompletedTreatmentCoronary Artery Disease / Hyperlipidemias1
4CompletedTreatmentCoronary Heart Disease (CHD) / High Cholesterol2
4CompletedTreatmentDiabetes Mellitus (DM)1
4CompletedTreatmentDyslipidemia (Fredrickson Type Ⅱa)1
4CompletedTreatmentDyslipidemia in Patients With Diabetes Mellitus1
4CompletedTreatmentDyslipidemias7
4CompletedTreatmentDyslipidemias / High Blood Pressure (Hypertension)3
4CompletedTreatmentDyslipidemias / Type 1 Insulin-Dependent Diabetes Mellitus1
4CompletedTreatmentHIV Dementia2
4CompletedTreatmentHealthy Volunteers2
4CompletedTreatmentHeart Failure1
4CompletedTreatmentHepatitis C Viral Infection1
4CompletedTreatmentHigh Blood Pressure (Hypertension) / High Cholesterol1
4CompletedTreatmentHigh Blood Pressure (Hypertension) / Hyperlipidemias1
4CompletedTreatmentChronic, stable Kidney Disease / High Blood Pressure (Hypertension)1
4CompletedTreatmentHigh Cholesterol10
4CompletedTreatmentHypercholesterolemia With Type2DM1
4CompletedTreatmentHyperlipidemias1
4CompletedTreatmentHypertriglycemia / Type 2 Diabetes Mellitus1
4CompletedTreatmentMetabolic Syndromes1
4CompletedTreatmentMulti-vessel Diseases, Angina1
4CompletedTreatmentMyocardial Infarction / Reperfusion Injury1
4CompletedTreatmentRheumatoid Arthritis1
4CompletedTreatmentSocket Preservation1
4CompletedTreatmentStable Angina (SA)1
4CompletedTreatmentStroke, Ischemic2
4CompletedTreatmentType 2 Diabetes Mellitus2
4CompletedTreatmentType IIa and IIb Hypercholesterolaemia1
4CompletedTreatmentVascular Surgery1
4CompletedTreatmentTransient ischemia attacks1
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 RecruitingDiagnosticCoronary Artery Disease1
4Not Yet RecruitingPreventionCardiovascular Disease (CVD)1
4Not Yet RecruitingTreatmentCarotid Artery Stenosis1
4Not Yet RecruitingTreatmentCoronary Artery Disease2
4Not Yet RecruitingTreatmentDyslipidemias / High Blood Pressure (Hypertension)1
4RecruitingDiagnosticHyperlipidemias1
4RecruitingDiagnosticStatin Adverse Reaction1
4RecruitingOtherCardiovascular Disease (CVD)1
4RecruitingOtherHigh Cholesterol1
4RecruitingPreventionAdverse Effects / Cardiovascular Disease (CVD) / Hyperlipidemias1
4RecruitingPreventionArrythmias1
4RecruitingPreventionCardiothoracic Surgery / Post-Operative Atrial Fibrillation1
4RecruitingPreventionCardiovascular Disease (CVD)1
4RecruitingPreventionCoronary Artery Disease1
4RecruitingPreventionDisability Free Survival / Elderly / Healthy Volunteers / Independent Living1
4RecruitingPreventionHepatocellular,Carcinoma1
4RecruitingPreventionHigh Blood Pressure (Hypertension) / Strokes / Transient Ischaemic Attack (TIA)1
4RecruitingPreventionMitochondrial Diseases1
4RecruitingTreatmentAtherosclerosis, Cerebral / Stroke, Ischemic1
4RecruitingTreatmentCardiovascular Disease (CVD)1
4RecruitingTreatmentCoronary Artery Disease1
4RecruitingTreatmentDental Plaque1
4RecruitingTreatmentDiabetes Mellitus (DM) / Dyslipidemias / Fatty Liver1
4RecruitingTreatmentDiabetes Mellitus Type 2 Platelets Reactivity Statin1
4RecruitingTreatmentDyslipidemias1
4RecruitingTreatmentDyslipidemias / High Blood Pressure (Hypertension)1
4RecruitingTreatmentDyslipidemias / High Blood Pressure (Hypertension) / Prediabetic State1
4RecruitingTreatmentHeart Failure1
4RecruitingTreatmentImmune Thrombocytopenia / Thrombocytopenic Purpura1
4RecruitingTreatmentMyocardial Infarction1
4RecruitingTreatmentPrinzmetal's variant angina1
4RecruitingTreatmentSevere Hypercholesterolemia1
4TerminatedNot AvailableStatin Adverse Reaction / Statin-Associated Myopathy1
4TerminatedDiagnosticMyopathic Conditions1
4TerminatedPreventionAtherosclerosis / Carotid Artery Stenosis / Strokes1
4TerminatedPreventionCardiovascular Disease (CVD) / Osteoarthritis (OA)1
4TerminatedPreventionCoarctation of the Aorta1
4TerminatedPreventionCoronary Heart Disease (CHD)1
4TerminatedPreventionHigh Blood Pressure (Hypertension)1
4TerminatedTreatmentAortic Valve Stenosis1
4TerminatedTreatmentAtherosclerosis / Coronary Artery Disease / High Cholesterol1
4TerminatedTreatmentChronic Kidney Disease (CKD) / High Cholesterol1
4TerminatedTreatmentHigh Cholesterol1
4TerminatedTreatmentHyperlipidemias / Non-Insulin Dependent Diabetes Mellitus / Type 2 Diabetes Mellitus1
4TerminatedTreatmentStable Angina (SA)1
4Unknown StatusNot AvailableCoronary Heart Disease (CHD) / Diabetes Mellitus (DM) / High Cholesterol / Non-Coronary Atherosclerotic Disease1
4Unknown StatusPreventionCarotid Stenosis1
4Unknown StatusPreventionCholesterol, HDL1
4Unknown StatusPreventionCoronary Heart Disease (CHD)1
4Unknown StatusPreventionEndothelium / Hydroxymethylglutaryl-CoA Reductase Inhibitors1
4Unknown StatusPreventionGeneral Surgery / Prevention / Thrombotic events1
4Unknown StatusPreventionVaccination Failure / Viral Hepatitis B1
4Unknown StatusTreatmentAcute Coronary Syndromes (ACS)1
4Unknown StatusTreatmentAngina Pectoris, Variant1
4Unknown StatusTreatmentAnterior Acute Myocardial Infarction1
4Unknown StatusTreatmentArterial and Arteriolar Disorders1
4Unknown StatusTreatmentAtherosclerosis1
4Unknown StatusTreatmentAtherosclerosis / Inflammatory Reaction1
4Unknown StatusTreatmentCoronary Artery Disease3
4Unknown StatusTreatmentDiabetes Mellitus (DM) / High Blood Pressure (Hypertension)1
4Unknown StatusTreatmentDiabetes Mellitus, Hypercholessterolemia1
4Unknown StatusTreatmentDrug-eluting Stent (DES)1
4Unknown StatusTreatmentFocus of Study1
4Unknown StatusTreatmentHigh Blood Pressure (Hypertension)1
4Unknown StatusTreatmentMyocardial Infarction / Unstable Angina Pectoris1
4Unknown StatusTreatmentST Elevation Myocardial Infarction (STEMI)1
4Unknown StatusTreatmentType 2 Diabetes Mellitus Without Insulin Treatment1
4WithdrawnTreatmentAngina Pectoris, Variant / Statins, HMG-CoA1
4WithdrawnTreatmentArterial Hypertension / Blood Pressures / Dyslipidemias / Lipid Metabolism Disorders1
4WithdrawnTreatmentAtherosclerosis1
4WithdrawnTreatmentDyslipidemias / Myocardial Infarction1
Not AvailableActive Not RecruitingTreatmentRheumatoid Arthritis1
Not AvailableCompletedNot AvailableAnesthesia; Adverse Effect / Delirium1
Not AvailableCompletedNot AvailableAngina Pectoris / Dyslipidemia (Fredrickson Type Ⅱa) / High Blood Pressure (Hypertension) / High Cholesterol1
Not AvailableCompletedNot AvailableAtheroma / Atherosclerosis / Atherosclerotic Carotid Disease1
Not AvailableCompletedNot AvailableCardiovascular Disease (CVD) / Coronary Artery Disease1
Not AvailableCompletedNot AvailableCardiovascular Disease (CVD) / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableCarotid Atherosclerosis / Metabolic Syndromes / Strokes / Type 2 Diabetes Mellitus1
Not AvailableCompletedNot AvailableCongestive Cardiomyopathy1
Not AvailableCompletedNot AvailableEndothelial Function / Infection NOS / Inflammatory Reaction1
Not AvailableCompletedNot AvailableGynecologic Oncological Pelvic/Abdominal Surgery1
Not AvailableCompletedNot AvailableHigh Blood Pressure (Hypertension)1
Not AvailableCompletedNot AvailableHigh Cholesterol3
Not AvailableCompletedNot AvailableHydroxymethylglutaryl-CoA Reductase Inhibitors / Muscular Diseases1
Not AvailableCompletedBasic ScienceDifference of 12-hour AUC1
Not AvailableCompletedBasic ScienceHydroxymethylglutaryl-CoA Reductase Inhibitors / Type 2 Diabetes Mellitus1
Not AvailableCompletedBasic ScienceHyperlipidemias1
Not AvailableCompletedDiagnosticCoronary Artery Disease / High Cholesterol / Monocyte Function1
Not AvailableCompletedPreventionAcute Kidney Injury (AKI)1
Not AvailableCompletedPreventionAcute Kidney Injury (AKI) / Acute Renal Failure (ARF) / Delirium / Icu Delirium / Post-Operative Delirium1
Not AvailableCompletedPreventionArrythmias1
Not AvailableCompletedPreventionCoronary Artery Bypass Graft Surgery Patients1
Not AvailableCompletedPreventionInflammatory Reaction / Myocardial Infarction / Myocardial Ischemia1
Not AvailableCompletedPreventionOsteoporosis1
Not AvailableCompletedPreventionType 1 Insulin-Dependent Diabetes Mellitus1
Not AvailableCompletedTreatmentAngioplasty, Transluminal, Percutaneous Coronary1
Not AvailableCompletedTreatmentAtherosclerosis1
Not AvailableCompletedTreatmentAtherosclerosis / Cardiovascular Disease (CVD) / Human Immunodeficiency Virus (HIV) / Human Immunodeficiency Virus (HIV) Infections / Inflammatory Reaction / Statins, HMG-CoA1
Not AvailableCompletedTreatmentCardiovascular Disease (CVD)1
Not AvailableCompletedTreatmentChronic Kidney Disease (CKD)1
Not AvailableCompletedTreatmentChronic Kidney Disease (CKD) / Proteinuria1
Not AvailableCompletedTreatmentCoronary Arteriosclerosis / Genetic Diseases, Inborn / Hypoalphalipoproteinemias1
Not AvailableCompletedTreatmentCoronary Artery1
Not AvailableCompletedTreatmentCoronary Artery Disease1
Not AvailableCompletedTreatmentDiastolic Heart Failure1
Not AvailableCompletedTreatmentEnd-Stage Renal Disease (ESRD)1
Not AvailableCompletedTreatmentHealthy Volunteers2
Not AvailableCompletedTreatmentHigh Blood Pressure (Hypertension) / High Cholesterol1
Not AvailableCompletedTreatmentHypercholesterolemia With Concomitant Type 2 Diabetes1
Not AvailableCompletedTreatmentHyperlipidemias1
Not AvailableCompletedTreatmentPolycystic Ovaries Syndrome1
Not AvailableCompletedTreatmentShock, Septic1
Not AvailableCompletedTreatmentThoracic Surgery1
Not AvailableRecruitingNot AvailableCoronary Arteriosclerosis / Coronary Artery Disease / Hydroxymethylglutaryl-CoA Reductase Inhibitors1
Not AvailableRecruitingBasic ScienceAtherosclerosis / Cardiovascular Disease (CVD)1
Not AvailableRecruitingBasic ScienceHealthy Volunteers1
Not AvailableRecruitingTreatmentGlomerulonephritis minimal lesion1
Not AvailableRecruitingTreatmentSleep Deprivation1
Not AvailableTerminatedNot AvailableHypertension and Cardiovascular Risk Factors1
Not AvailableTerminatedBasic ScienceDiabetes Mellitus (DM) / Metabolic Syndromes1
Not AvailableTerminatedPreventionRenal Dysfunction1
Not AvailableTerminatedTreatmentCoronary Artery Disease1
Not AvailableTerminatedTreatmentDiastolic Heart Failure1
Not AvailableUnknown StatusNot AvailableDisseminated Sclerosis1
Not AvailableUnknown StatusBasic ScienceAutonomic Changes of Cardiomyocytes Repolarisation / Heterogeneity of Cardiomyocytes Repolarisation1
Not AvailableUnknown StatusDiagnosticDiabetes Mellitus (DM)1
Not AvailableUnknown StatusPreventionAtherosclerosis1
Not AvailableUnknown StatusTreatmentAcute Coronary Syndromes (ACS)2
Not AvailableUnknown StatusTreatmentBlood Pressure Variability / Intracranial Artery Stenosis1
Not AvailableUnknown StatusTreatmentCongestive Heart Failure (CHF)1
Not AvailableUnknown StatusTreatmentEndometriosis / Pain NOS1
Not AvailableUnknown StatusTreatmentHigh Cholesterol / Thrombotic events1
Not AvailableUnknown StatusTreatmentNonalcoholic Fatty Liver Disease (NAFLD)1
Not AvailableUnknown StatusTreatmentMixed hypercholesterolemia1
Not AvailableWithdrawnBasic ScienceNeurocognitive Dysfunction1
Not AvailableWithdrawnPreventionPsoriatic Arthritis / Rheumatoid Arthritis1
Not AvailableWithdrawnTreatmentAtherosclerosis / Type 2 Diabetes Mellitus1
Not AvailableWithdrawnTreatmentComplication of Renal Dialysis1
Not AvailableWithdrawnTreatmentEndothelial Dysfunction1
Not AvailableWithdrawnTreatmentNon Alcoholic Fatty Liver Diseases (NAFLD)1
Not AvailableWithdrawnTreatmentRecurrent Prostate Cancer / Stage I Prostate Cancer / Stage IIA Prostate Cancer / Stage IIB Prostate Cancer / Stage III Prostate Cancer / Stage IV Prostate Cancer1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Advanced Pharmaceutical Services Inc.
  • Apotheca Inc.
  • A-S Medication Solutions LLC
  • Atlantic Biologicals Corporation
  • Bryant Ranch Prepack
  • Cardinal Health
  • Direct Pharmaceuticals Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Goedecke GmbH
  • Healthcare Pharmacy
  • Heartland Repack Services LLC
  • Kaiser Foundation Hospital
  • Lake Erie Medical and Surgical Supply
  • Murfreesboro Pharmaceutical Nursing Supply
  • Nucare Pharmaceuticals Inc.
  • Orifice Medical AB
  • PCA LLC
  • PD-Rx Pharmaceuticals Inc.
  • Pfizer Inc.
  • Pharmaceutical Utilization Management Program VA Inc.
  • Physicians Total Care Inc.
  • Prepackage Specialists
  • Prepak Systems Inc.
  • Resource Optimization and Innovation LLC
  • Sandhills Packaging Inc.
  • Southwood Pharmaceuticals
  • Tya Pharmaceuticals
  • US Pharmaceutical Group
  • Vangard Labs Inc.
  • Vitrum Ab
  • Warner Lambert Company LLC
Dosage forms
FormRouteStrength
PowderNot applicable1 kg/1kg
TabletOral10 mg/1
TabletOral20 mg/1
TabletOral40 mg/1
TabletOral80 mg/1
Tablet, film coatedOral10 mg/301
Tablet, film coatedOral20 mg/301
Tablet, film coatedOral80 mg/301
PowderNot applicable20 kg/20kg
TabletOral
Tablet, film coatedOral
TabletOral10 mg
TabletOral20 mg
TabletOral40 mg
TabletOral80 mg
Tablet, film coatedOral10 mg/1
Tablet, film coatedOral20 mg/1
Tablet, film coatedOral40 mg/1
Tablet, film coatedOral80 mg/1
Prices
Unit descriptionCostUnit
Lipitor 20 mg tablet5.0USD tablet
Lipitor 40 mg tablet5.0USD tablet
Lipitor 80 mg tablet5.0USD tablet
Lipitor 10 mg tablet3.5USD tablet
Lipitor 40 mg Tablet2.52USD tablet
Lipitor 80 mg Tablet2.52USD tablet
Lipitor 20 mg Tablet2.34USD tablet
Lipitor 10 mg Tablet1.87USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US4681893No1987-07-212009-09-24Us
CA2521776No2006-04-252022-05-21Canada
CA2220018No2001-04-172016-07-08Canada
US5969156Yes1999-10-192017-01-08Us
USRE42461Yes2011-06-142017-04-25Us
US6455574No2002-09-242018-08-11Us
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
melting point (°C)176 °C'MSDS'
boiling point (°C)722 ºC at 760 mmHg'MSDS'
water solubilityPractically insoluble'MSDS'
logP6.36'MSDS'
pKa4.46'MSDS'
Predicted Properties
PropertyValueSource
Water Solubility0.00063 mg/mLALOGPS
logP4.24ALOGPS
logP5.39ChemAxon
logS-6ALOGPS
pKa (Strongest Acidic)4.33ChemAxon
pKa (Strongest Basic)-2.7ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area111.79 Å2ChemAxon
Rotatable Bond Count12ChemAxon
Refractivity158.2 m3·mol-1ChemAxon
Polarizability59.39 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.8947
Blood Brain Barrier-0.7825
Caco-2 permeable-0.8956
P-glycoprotein substrateSubstrate0.5246
P-glycoprotein inhibitor IInhibitor0.7164
P-glycoprotein inhibitor IIInhibitor0.8724
Renal organic cation transporterNon-inhibitor0.8131
CYP450 2C9 substrateNon-substrate0.7887
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.6841
CYP450 1A2 substrateNon-inhibitor0.8551
CYP450 2C9 inhibitorNon-inhibitor0.719
CYP450 2D6 inhibitorNon-inhibitor0.9042
CYP450 2C19 inhibitorNon-inhibitor0.6191
CYP450 3A4 inhibitorNon-inhibitor0.6675
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6894
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.7777
BiodegradationNot ready biodegradable0.9974
Rat acute toxicity2.5686 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9904
hERG inhibition (predictor II)Non-inhibitor0.5101
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
LC-MS/MS Spectrum - LC-ESI-QTOF , negativeLC-MS/MSsplash10-0a4i-0000090000-ae5c999b091a2bc93933
LC-MS/MS Spectrum - LC-ESI-QTOF , negativeLC-MS/MSsplash10-0a4i-0000190000-dd563e18b1f0f74aadd5
LC-MS/MS Spectrum - LC-ESI-QTOF , negativeLC-MS/MSsplash10-0zfs-0007960000-cb66a18d2f0a687261ba
LC-MS/MS Spectrum - LC-ESI-QTOF , negativeLC-MS/MSsplash10-002b-0059000000-0942bc1e35434cd7d0d3
LC-MS/MS Spectrum - LC-ESI-QTOF , negativeLC-MS/MSsplash10-004i-0093000000-f42ba46820a3cf3295c5
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0udj-0005910000-b09ba5f3b86948c7f3cb
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0a4i-0000090000-6f297ca79ae1761aac33
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0002-1009300000-9479520f395dcdd585e7
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-0092000000-9b561b8d35c3bdc5e46a
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-0090000000-3aad87273e7f9942a50f
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-01t9-1090000000-3f0efff41ebdb5320ce4
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-03di-2090000000-0227638704b90c4249d0
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0a4i-0000090000-65c729c6734f6533c431
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0002-1009300000-9122e4479d8c0c32bb0d
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-0092000000-22d639a8882509e1bcdb
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-0090000000-30a0198165bae85fa258
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-01t9-1090000000-cb3feea45f5280f05c37
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-03di-2090000000-8db2f70b373277f143c0
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0udj-0005910000-a63c845ca248d958068d
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0a6s-1085190000-9e43612012842effca5a
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0006-0031900000-4081fba1ae61b0d871cf
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-052f-0000980000-6751fefdee0a257e52f8
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0006-0000900000-4009a70e947dcceb6e0f
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0006-0085900000-e1a4447e4c9a4bda83b2
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0udi-0092100000-4a5517154ad5f7375ea2
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0a4i-0000090000-e741fcb91eb29d1032cb
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00kf-0000900000-fdd41dae94afd3f4d3c5
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0000490000-25199beeece682c7de9e
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0006-0020900000-71cacdfc979c4386762b
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0udi-0092000000-38374b1412250df34777
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0udi-0090000000-87710909ebad67c88f3b
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0udj-0190000000-60e7ef3dc3f76db11c5f
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0f72-0290000000-e8c2cda8588874b2aaa5
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0000490000-a5ee6b466e73e9e72383
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0006-0011900000-b8fc562d4be5ffb07f59
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0udi-0092000000-df78998b01951a3dd03a
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0udi-0090000000-19c391db652668c97d59
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0udj-0190000000-931a1911dcd7ec9dbbc8
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0f72-0290000000-6157ef91cb98aeef5cf7
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00kf-0000900000-cd6fb2c00146543cbb47
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0f6x-0092420000-fb2c084ecdd5af8f6f7b

Taxonomy

Description
This compound belongs to the class of organic compounds known as diphenylpyrroles. These are aromatic heterocyclic compounds with a structure based on a pyrrole ring linked to exactly two phenyl groups.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Pyrroles
Sub Class
Substituted pyrroles
Direct Parent
Diphenylpyrroles
Alternative Parents
Aromatic anilides / Medium-chain hydroxy acids and derivatives / Pyrrole carboxamides / Medium-chain fatty acids / Beta hydroxy acids and derivatives / Fluorobenzenes / Halogenated fatty acids / Hydroxy fatty acids / Heterocyclic fatty acids / Aryl fluorides
show 13 more
Substituents
2,3-diphenylpyrrole / Aromatic anilide / Medium-chain hydroxy acid / Pyrrole-3-carboxamide / Pyrrole-3-carboxylic acid or derivatives / Medium-chain fatty acid / Beta-hydroxy acid / Fluorobenzene / Halobenzene / Halogenated fatty acid
show 30 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
statin (synthetic), aromatic amide, pyrroles, dihydroxy monocarboxylic acid, monofluorobenzenes (CHEBI:39548)

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. Davidson MH: Rosuvastatin: a highly efficacious statin for the treatment of dyslipidaemia. Expert Opin Investig Drugs. 2002 Mar;11(3):125-41. [PubMed:12769127]
  2. Jafari M, Ebrahimi R, Ahmadi-Kashani M, Balian H, Bashir M: Efficacy of alternate-day dosing versus daily dosing of atorvastatin. J Cardiovasc Pharmacol Ther. 2003 Jun;8(2):123-6. [PubMed:12808485]
  3. Baxter JD, Webb P, Grover G, Scanlan TS: Selective activation of thyroid hormone signaling pathways by GC-1: a new approach to controlling cholesterol and body weight. Trends Endocrinol Metab. 2004 May-Jun;15(4):154-7. [PubMed:15109613]
  4. Maejima T, Yamazaki H, Aoki T, Tamaki T, Sato F, Kitahara M, Saito Y: Effect of pitavastatin on apolipoprotein A-I production in HepG2 cell. Biochem Biophys Res Commun. 2004 Nov 12;324(2):835-9. [PubMed:15474503]
  5. Bosel J, Gandor F, Harms C, Synowitz M, Harms U, Djoufack PC, Megow D, Dirnagl U, Hortnagl H, Fink KB, Endres M: Neuroprotective effects of atorvastatin against glutamate-induced excitotoxicity in primary cortical neurones. J Neurochem. 2005 Mar;92(6):1386-98. [PubMed:15748157]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Virus receptor activity
Specific Function
Cell surface glycoprotein receptor involved in the costimulatory signal essential for T-cell receptor (TCR)-mediated T-cell activation. Acts as a positive regulator of T-cell coactivation, by bindi...
Gene Name
DPP4
Uniprot ID
P27487
Uniprot Name
Dipeptidyl peptidase 4
Molecular Weight
88277.935 Da
References
  1. Taldone T, Zito SW, Talele TT: Inhibition of dipeptidyl peptidase-IV (DPP-IV) by atorvastatin. Bioorg Med Chem Lett. 2008 Jan 15;18(2):479-84. Epub 2007 Dec 3. [PubMed:18068977]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Transcription regulatory region dna binding
Specific Function
Ligand-activated transcriptional activator. Binds to the XRE promoter region of genes it activates. Activates the expression of multiple phase I and II xenobiotic chemical metabolizing enzyme genes...
Gene Name
AHR
Uniprot ID
P35869
Uniprot Name
Aryl hydrocarbon receptor
Molecular Weight
96146.705 Da
References
  1. Hu W, Sorrentino C, Denison MS, Kolaja K, Fielden MR: Induction of cyp1a1 is a nonspecific biomarker of aryl hydrocarbon receptor activation: results of large scale screening of pharmaceuticals and toxicants in vivo and in vitro. Mol Pharmacol. 2007 Jun;71(6):1475-86. Epub 2007 Feb 27. [PubMed:17327465]
  2. Chauvin B, Drouot S, Barrail-Tran A, Taburet AM: Drug-drug interactions between HMG-CoA reductase inhibitors (statins) and antiviral protease inhibitors. Clin Pharmacokinet. 2013 Oct;52(10):815-31. doi: 10.1007/s40262-013-0075-4. [PubMed:23703578]
  3. Korhonova M, Doricakova A, Dvorak Z: Optical Isomers of Atorvastatin, Rosuvastatin and Fluvastatin Enantiospecifically Activate Pregnane X Receptor PXR and Induce CYP2A6, CYP2B6 and CYP3A4 in Human Hepatocytes. PLoS One. 2015 Sep 14;10(9):e0137720. doi: 10.1371/journal.pone.0137720. eCollection 2015. [PubMed:26366873]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Transcription factor binding
Specific Function
Responsible for the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4). Histone deacetylation gives a tag for epigenetic repression and plays an impo...
Gene Name
HDAC2
Uniprot ID
Q92769
Uniprot Name
Histone deacetylase 2
Molecular Weight
55363.855 Da
References
  1. Lin YC, Lin JH, Chou CW, Chang YF, Yeh SH, Chen CC: Statins increase p21 through inhibition of histone deacetylase activity and release of promoter-associated HDAC1/2. Cancer Res. 2008 Apr 1;68(7):2375-83. doi: 10.1158/0008-5472.CAN-07-5807. [PubMed:18381445]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Zinc ion binding
Specific Function
Binds and transactivates the retinoic acid response elements that control expression of the retinoic acid receptor beta 2 and alcohol dehydrogenase 3 genes. Transactivates both the phenobarbital re...
Gene Name
NR1I3
Uniprot ID
Q14994
Uniprot Name
Nuclear receptor subfamily 1 group I member 3
Molecular Weight
39942.145 Da
References
  1. Rezen T, Hafner M, Kortagere S, Ekins S, Hodnik V, Rozman D: Rosuvastatin and Atorvastatin Are Ligands of the Human Constitutive Androstane Receptor/Retinoid X Receptor alpha Complex. Drug Metab Dispos. 2017 Aug;45(8):974-976. doi: 10.1124/dmd.117.075523. Epub 2017 May 23. [PubMed:28536098]

Enzymes

Details
1. Cytochrome P450 3A4
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. 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. doi: 10.1016/j.clpt.2006.09.003. [PubMed:17178259]
  2. Cohen LH, van Leeuwen RE, van Thiel GC, van Pelt JF, Yap SH: Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64. [PubMed:11523064]
  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]
  5. Jacobsen W, Kuhn B, Soldner A, Kirchner G, Sewing KF, Kollman PA, Benet LZ, Christians U: Lactonization is the critical first step in the disposition of the 3-hydroxy-3-methylglutaryl-CoA reductase inhibitor atorvastatin. Drug Metab Dispos. 2000 Nov;28(11):1369-78. [PubMed:11038166]
  6. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
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 un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 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]
  2. 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]
  3. Jacobsen W, Kuhn B, Soldner A, Kirchner G, Sewing KF, Kollman PA, Benet LZ, Christians U: Lactonization is the critical first step in the disposition of the 3-hydroxy-3-methylglutaryl-CoA reductase inhibitor atorvastatin. Drug Metab Dispos. 2000 Nov;28(11):1369-78. [PubMed:11038166]
  4. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
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 un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
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
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 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]
  2. Jacobsen W, Kuhn B, Soldner A, Kirchner G, Sewing KF, Kollman PA, Benet LZ, Christians U: Lactonization is the critical first step in the disposition of the 3-hydroxy-3-methylglutaryl-CoA reductase inhibitor atorvastatin. Drug Metab Dispos. 2000 Nov;28(11):1369-78. [PubMed:11038166]
  3. Backman JT, Filppula AM, Niemi M, Neuvonen PJ: Role of Cytochrome P450 2C8 in Drug Metabolism and Interactions. Pharmacol Rev. 2016 Jan;68(1):168-241. doi: 10.1124/pr.115.011411. [PubMed:26721703]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Cohen LH, van Leeuwen RE, van Thiel GC, van Pelt JF, Yap SH: Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64. [PubMed:11523064]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
Curator comments
Supporting data are limited to findings of an in vitro study.
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. Cohen LH, van Leeuwen RE, van Thiel GC, van Pelt JF, Yap SH: Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64. [PubMed:11523064]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
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 im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Cohen LH, van Leeuwen RE, van Thiel GC, van Pelt JF, Yap SH: Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64. [PubMed:11523064]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inducer
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
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 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]
  2. Kobayashi K, Yamanaka Y, Iwazaki N, Nakajo I, Hosokawa M, Negishi M, Chiba K: Identification of HMG-CoA reductase inhibitors as activators for human, mouse and rat constitutive androstane receptor. Drug Metab Dispos. 2005 Jul;33(7):924-9. Epub 2005 Mar 31. [PubMed:15802384]
  3. Kocarek TA, Dahn MS, Cai H, Strom SC, Mercer-Haines NA: Regulation of CYP2B6 and CYP3A expression by hydroxymethylglutaryl coenzyme A inhibitors in primary cultured human hepatocytes. Drug Metab Dispos. 2002 Dec;30(12):1400-5. [PubMed:12433810]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Gene Name
UGT1A1
Uniprot ID
P22309
Uniprot Name
UDP-glucuronosyltransferase 1-1
Molecular Weight
59590.91 Da
References
  1. Stormo C, Bogsrud MP, Hermann M, Asberg A, Piehler AP, Retterstol K, Kringen MK: UGT1A1*28 is associated with decreased systemic exposure of atorvastatin lactone. Mol Diagn Ther. 2013 Aug;17(4):233-7. doi: 10.1007/s40291-013-0031-x. [PubMed:23580084]
  2. Lennernas H: Clinical pharmacokinetics of atorvastatin. Clin Pharmacokinet. 2003;42(13):1141-60. [PubMed:14531725]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Retinoic acid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
Gene Name
UGT1A3
Uniprot ID
P35503
Uniprot Name
UDP-glucuronosyltransferase 1-3
Molecular Weight
60337.835 Da
References
  1. Stormo C, Bogsrud MP, Hermann M, Asberg A, Piehler AP, Retterstol K, Kringen MK: UGT1A1*28 is associated with decreased systemic exposure of atorvastatin lactone. Mol Diagn Ther. 2013 Aug;17(4):233-7. doi: 10.1007/s40291-013-0031-x. [PubMed:23580084]
  2. Lennernas H: Clinical pharmacokinetics of atorvastatin. Clin Pharmacokinet. 2003;42(13):1141-60. [PubMed:14531725]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Binder
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
References
  1. McIver LA, Siddique MS: Atorvastatin . [PubMed:28613530]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Wang E, Casciano CN, Clement RP, Johnson WW: HMG-CoA reductase inhibitors (statins) characterized as direct inhibitors of P-glycoprotein. Pharm Res. 2001 Jun;18(6):800-6. [PubMed:11474784]
  2. Sieczkowski E, Lehner C, Ambros PF, Hohenegger M: Double impact on p-glycoprotein by statins enhances doxorubicin cytotoxicity in human neuroblastoma cells. Int J Cancer. 2010 May 1;126(9):2025-35. doi: 10.1002/ijc.24885. [PubMed:19739078]
  3. Lennernas H: Clinical pharmacokinetics of atorvastatin. Clin Pharmacokinet. 2003;42(13):1141-60. [PubMed:14531725]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
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. Hsiang B, Zhu Y, Wang Z, Wu Y, Sasseville V, Yang WP, Kirchgessner TG: A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters. J Biol Chem. 1999 Dec 24;274(52):37161-8. [PubMed:10601278]
Kind
Protein
Organism
Humans
Pharmacological action
No
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. Hsiang B, Zhu Y, Wang Z, Wu Y, Sasseville V, Yang WP, Kirchgessner TG: A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters. J Biol Chem. 1999 Dec 24;274(52):37161-8. [PubMed:10601278]
  2. Kameyama Y, Yamashita K, Kobayashi K, Hosokawa M, Chiba K: Functional characterization of SLCO1B1 (OATP-C) variants, SLCO1B1*5, SLCO1B1*15 and SLCO1B1*15+C1007G, by using transient expression systems of HeLa and HEK293 cells. Pharmacogenet Genomics. 2005 Jul;15(7):513-22. [PubMed:15970799]
  3. Lennernas H: Clinical pharmacokinetics of atorvastatin. Clin Pharmacokinet. 2003;42(13):1141-60. [PubMed:14531725]
Kind
Protein
Organism
Humans
Pharmacological action
No
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
No
Actions
Substrate
General Function
Organic anion transmembrane transporter activity
Specific Function
Acts as a multispecific organic anion pump which can transport nucleotide analogs.
Gene Name
ABCC5
Uniprot ID
O15440
Uniprot Name
Multidrug resistance-associated protein 5
Molecular Weight
160658.8 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
No
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, methotre...
Gene Name
ABCC1
Uniprot ID
P33527
Uniprot Name
Multidrug resistance-associated protein 1
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
Humans
Pharmacological action
No
Actions
Substrate
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. Grube M, Kock K, Oswald S, Draber K, Meissner K, Eckel L, Bohm M, Felix SB, Vogelgesang S, Jedlitschky G, Siegmund W, Warzok R, Kroemer HK: Organic anion transporting polypeptide 2B1 is a high-affinity transporter for atorvastatin and is expressed in the human heart. Clin Pharmacol Ther. 2006 Dec;80(6):607-20. [PubMed:17178262]
  2. 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
No
Actions
Substrate
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. Klatt S, Fromm MF, Konig J: The influence of oral antidiabetic drugs on cellular drug uptake mediated by hepatic OATP family members. Basic Clin Pharmacol Toxicol. 2013 Apr;112(4):244-50. doi: 10.1111/bcpt.12031. Epub 2012 Dec 6. [PubMed:23121773]
  2. Lennernas H: Clinical pharmacokinetics of atorvastatin. Clin Pharmacokinet. 2003;42(13):1141-60. [PubMed:14531725]
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. Becker ML, Elens LL, Visser LE, Hofman A, Uitterlinden AG, van Schaik RH, Stricker BH: Genetic variation in the ABCC2 gene is associated with dose decreases or switches to other cholesterol-lowering drugs during simvastatin and atorvastatin therapy. Pharmacogenomics J. 2013 Jun;13(3):251-6. doi: 10.1038/tpj.2011.59. Epub 2011 Dec 20. [PubMed:22186618]
Kind
Protein
Organism
Humans
Pharmacological action
No
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. Pedersen JM, Matsson P, Bergstrom CA, Hoogstraate J, Noren A, LeCluyse EL, Artursson P: Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Epub 2013 Sep 6. [PubMed:24014644]

Drug created on June 13, 2005 07:24 / Updated on August 16, 2019 09:57