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Name
Pitavastatin
Accession Number
DB08860  (DB06514)
Type
Small Molecule
Groups
Approved
Description

Pitavastatin, also known as the brand name product Livalo, 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,3 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.4,5

Pitavastatin and other drugs from the statin class of medications including atorvastatin, pravastatin, rosuvastatin, fluvastatin, and lovastatin are considered first-line options for the treatment of dyslipidemia.4,5 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.6 Elevated cholesterol levels, and in particular, elevated low-density lipoprotein (LDL) levels, are an important risk factor for the development of CVD.4 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.8,9,10,11,12,13 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.4,5 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.15,14

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.16,17,13,18 Study data has confirmed that pitavastatin's potency in lowering LDL-C is comparable to that of other statins but also has increased efficacy in increasing HDL-C (also known as "good cholesterol").21,22,23 Despite these differences in potency, several trials have demonstrated only minimal differences in terms of clinical outcomes between statins.11

Structure
Thumb
Synonyms
  • Pitavastatia
  • Pitavastatin
  • Pitavastatina
  • Pitavastatine
  • Pitavastatinum
External IDs
NK 104 / NK-104 / NKS-104 / NKS104
Product Ingredients
IngredientUNIICASInChI Key
Pitavastatin calciumIYD54XEG3W147526-32-7RHGYHLPFVJEAOC-WUVPNHNWSA-L
Pitavastatin magnesiumBDS8LUQ384956116-90-8MPAZKXHCZWDZDY-FFNUKLMVSA-L
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
LivaloTablet, film coated2.09 mg/1OralKowa Pharmaceuticals America, Inc.2019-05-16Not applicableUs66869 0204 90 nlmimage10 293c1490
LivaloTablet, film coated4 mg/1OralEli Lilly & Co. Ltd.2010-05-152016-01-31Us00002 4772 90 nlmimage10 8c16c656
LivaloTablet, film coated1.045 mg/1OralKowa Pharmaceuticals America, Inc.2019-05-16Not applicableUs66869 0104 90 nlmimage10 323c1910
LivaloTablet, film coated2 mg/1OralEli Lilly & Co. Ltd.2010-05-152016-01-31Us00002 4771 90 nlmimage10 8f16c7a6
LivaloTablet, film coated1 mg/1OralEli Lilly & Co. Ltd.2010-05-152016-01-31Us00002 4770 90 nlmimage10 9516caa6
LivaloTablet, film coated4.18 mg/1OralKowa Pharmaceuticals America, Inc.2019-05-16Not applicableUs66869 0404 90 nlmimage10 d93c6ce3
ZypitamagTablet, film coated4 mg/1OralMedicure International Inc2018-03-09Not applicableUs
ZypitamagTablet, film coated2 mg/1OralMedicure International Inc2018-03-09Not applicableUs
ZypitamagTablet, film coated4 mg/1OralCadila Healthcare Limited2018-03-09Not applicableUs
ZypitamagTablet, film coated1 mg/1OralMedicure International Inc2018-03-09Not applicableUs
Additional Data Available
  • Application Number
    Application Number

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

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  • Product Code
    Product Code

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

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
PitavastatinTablet, film coated4.18 mg/1OralOrient Pharma Co., Ltd.2018-07-252018-07-25Us
PitavastatinTablet, film coated4 mg/1OralQuinn Pharmaceuticals, Llc2017-03-312017-03-31Us
PitavastatinTablet, film coated2.09 mg/1OralOrient Pharma Co., Ltd.2018-07-252018-07-25Us
PitavastatinTablet, film coated2 mg/1OralQuinn Pharmaceuticals, Llc2017-03-312017-03-31Us
PitavastatinTablet, film coated4 mg/1OralStason Pharmaceuticals, Inc.2017-12-252018-01-19Us
PitavastatinTablet, film coated1 mg/1OralQuinn Pharmaceuticals, Llc2017-03-312017-03-31Us
PitavastatinTablet, film coated2 mg/1OralStason Pharmaceuticals, Inc.2017-12-252018-01-19Us
PitavastatinTablet, film coated1.045 mg/1OralOrient Pharma Co., Ltd.2018-07-252018-07-25Us
PitavastatinTablet, film coated1 mg/1OralStason Pharmaceuticals, Inc.2017-12-252018-01-19Us
Additional Data Available
  • Application Number
    Application Number

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  • Product Code
    Product Code

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Categories
UNII
M5681Q5F9P
CAS number
147511-69-1
Weight
Average: 421.4608
Monoisotopic: 421.168936466
Chemical Formula
C25H24FNO4
InChI Key
VGYFMXBACGZSIL-MCBHFWOFSA-N
InChI
InChI=1S/C25H24FNO4/c26-17-9-7-15(8-10-17)24-20-3-1-2-4-22(20)27-25(16-5-6-16)21(24)12-11-18(28)13-19(29)14-23(30)31/h1-4,7-12,16,18-19,28-29H,5-6,13-14H2,(H,30,31)/b12-11+/t18-,19-/m1/s1
IUPAC Name
(3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxyhept-6-enoic acid
SMILES
O[C@H](C[C@H](O)\C=C\C1=C(N=C2C=CC=CC2=C1C1=CC=C(F)C=C1)C1CC1)CC(O)=O

Pharmacology

Indication

Pitavastatin is indicated for the treatment of adult patients with primary hyperlipidemia or mixed dyslipidemia to reduce elevated total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), triglycerides (TG), and to increase high-density lipoprotein cholesterol (HDL-C). It is also indicated for the treatment of pediatric patients aged 8 years and older with heterozygous familial hypercholesterolemia (HeFH) to reduce elevated TC, LDL-C, and Apo B.29

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.4,5

Associated Conditions
Pharmacodynamics

Pitavastatin is an oral antilipemic agent which 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, rosuvastatin reduces the risk of cardiovascular morbidity and mortality.4,5

Elevated cholesterol levels, and in particular, elevated low-density lipoprotein (LDL) levels, are an important risk factor for the development of CVD.4 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.8,9,10,11,12 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.4,5 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.15,14

Skeletal Muscle Effects

Pitavastatin may cause myopathy (muscle pain, tenderness, or weakness with creatine kinase (CK) above ten times the upper limit of normal) and rhabdomyolysis (with or without acute renal failure secondary to myoglobinuria). Rare fatalities have occurred as a result of rhabdomyolysis with statin use, including pitavastatin. Predisposing factors for myopathy include advanced age (≥65 years), female gender, uncontrolled hypothyroidism, and renal impairment. In most cases, muscle symptoms and CK increases resolved when treatment was promptly discontinued. As dosages of pitavastatin greater than 4mg per day were associated with an increased risk of severe myopathy, the product monograph recommends a maximum daily dose of 4mg once daily.29

The risk of myopathy during treatment with pitavstatin may be increased with concurrent administration of interacting drugs such as fenofibrate, niacin, gemfibrozil, an d cyclosporine. 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.29

Real-world data from observational studies has suggested that 10-15% of people taking statins may experience muscle aches at some point during treatment.28

Hepatic Dysfunction

Increases in serum transaminases have been reported with pitavastatin. In most cases, the elevations were transient and either resolved or improved on continued therapy or after a brief interruption in therapy. There have been rare postmarketing reports of fatal and non-fatal hepatic failure in patients taking statins, including pitavastatin.29

Patients who consume substantial quantities of alcohol and/or have a history of liver disease may be at increased risk for hepatic injury.29

Increases in HbA1c and Fasting Serum Glucose Levels

Increases in HbA1c and fasting serum glucose levels have been reported with statins, including pitavastatin. Optimize lifestyle measures, including regular exercise, maintaining a healthy body weight, and making healthy food choices.29

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.24

Mechanism of action

Pitavastatin 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.3 Pitavastatin acts primarily in the liver, where decreased hepatic cholesterol concentrations stimulate the upregulation of hepatic low density lipoprotein (LDL) receptors which increase hepatic uptake of LDL, thereby reducing circulating LDL-C levels.

In vitro and in vivo animal studies also demonstrate that statins exert vasculoprotective effects independent of their lipid-lowering properties, also known as the pleiotropic effects of statins.19 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.26

TargetActionsOrganism
A3-hydroxy-3-methylglutaryl-coenzyme A reductase
inhibitor
Humans
UIntegrin alpha-LNot AvailableHumans
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Contraindications

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Absorption

Pitavastatin peak plasma concentrations are achieved about 1 hour after oral administration. Both Cmax and AUC0-inf increased in an approximately dose-proportional manner for single pitavastatin doses from 1 mg to 24 mg once daily. The absolute bioavailability of pitavastatin oral solution is 51%. The Cmax and AUC of pitavastatin did not differ following evening or morning drug administration. In healthy volunteers receiving 4 mg pitavastatin, the percent change from baseline for LDL-C following evening dosing was slightly greater than that following morning dosing. Pitavastatin was absorbed in the small intestine but very little in the colon.29

Compared to other statins, pitavastatin has a relatively high bioavailability, which has been suggested to occur due to enterohepatic reabsorption in the intestine following intestinal absorption.25

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 pitavastatin pharmacokinetics. Evidence from pharmacogenetic studies of the c.521T>C single nucleotide polymorphism (SNP) in the gene encoding OATP1B1 (SLCO1B1) demonstrated that pitavastatin AUC was increased 3.08-fold for individuals homozygous for 521CC compared to homozygous 521TT individuals.27 Other statin drugs impacted by this polymorphism include simvastatin, pitavastatin, atorvastatin, and rosuvastatin.20 Individuals with the 521CC genotype may be at increased risk of dose-related adverse effects including myopathy and rhabdomyolysis due to increased exposure to the drug.

Volume of distribution

148 L29

Protein binding

Pitavstatin is more than 99% protein bound in human plasma, mainly to albumin and alpha 1-acid glycoprotein.29

Metabolism

The principal route of pitavastatin metabolism is glucuronidation via liver uridine 5'-diphosphate glucuronosyltransferase (UGT) with subsequent formation of pitavastatin lactone. There is only minimal metabolism by the cytochrome P450 system. Pitavastatin is marginally metabolized by CYP2C9 and to a lesser extent by CYP2C8. The major metabolite in human plasma is the lactone, which is formed via an ester-type pitavastatin glucuronide conjugate by UGTs (UGT1A3 and UGT2B7).29,25

Route of elimination

A mean of 15% of radioactivity of orally administered, single 32 mg 14C-labeled pitavastatin dose was excreted in urine, whereas a mean of 79% of the dose was excreted in feces within 7 days.29

Half life

The mean plasma elimination half-life is approximately 12 hours.29

Clearance

Following a single dose, the apparent mean oral clearance of pitavastatin is 43.4 L/h.25

Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
(R)-warfarinThe metabolism of Pitavastatin can be decreased when combined with (R)-warfarin.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Pitavastatin.
4-hydroxycoumarinThe risk or severity of bleeding can be increased when Pitavastatin is combined with 4-hydroxycoumarin.
AbataceptThe metabolism of Pitavastatin can be increased when combined with Abatacept.
AbemaciclibThe serum concentration of Pitavastatin can be increased when it is combined with Abemaciclib.
AbirateroneThe metabolism of Pitavastatin can be decreased when combined with Abiraterone.
AcebutololThe serum concentration of Pitavastatin can be increased when it is combined with Acebutolol.
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Pitavastatin.
AcetaminophenThe serum concentration of Pitavastatin can be increased when it is combined with Acetaminophen.
AcetohexamideThe metabolism of Pitavastatin can be decreased when combined with Acetohexamide.
Additional Data Available
  • Extended Description
    Extended Description

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  • Severity
    Severity

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Food Interactions
  • Avoid taking pitavastatin with red yeast rice. May increase risk of myopathy of pitavastatin via pharmacodynamic synergism. Red yeast rice contain monocolin K (similar to lovastatin)
  • Take with or without food

References

Synthesis Reference

Shriprakash Dhar DWIVEDI, Dhimant Jasubhai PATEL, Alpesh Pravinchandra SHAH, "METHOD FOR PREPARATION OF PITAVASTATIN AND ITS PHARMACEUTICAL ACCEPTABLE SALTS THEREOF." U.S. Patent US20120022102, issued January 26, 2012.

US20120022102
General References
  1. Morgan RE, Campbell SE, Yu CY, Sponseller CA, Muster HA: Comparison of the safety, tolerability, and pharmacokinetic profile of a single oral dose of pitavastatin 4 mg in adult subjects with severe renal impairment not on hemodialysis versus healthy adult subjects. J Cardiovasc Pharmacol. 2012 Jul;60(1):42-8. doi: 10.1097/FJC.0b013e318256cdf0. [PubMed:22472908]
  2. Jung JA, Noh YH, Jin S, Kim MJ, Kim YH, Jung JA, Lim HS, Bae KS: Pharmacokinetic interaction between pitavastatin and valsartan: a randomized, open-labeled crossover study in healthy male Korean volunteers. Clin Ther. 2012 Apr;34(4):958-65. doi: 10.1016/j.clinthera.2012.01.026. Epub 2012 Mar 10. [PubMed:22410289]
  3. 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]
  4. 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]
  5. 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]
  6. 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]
  7. Tardy B, Lecompte T, Boelhen F, Tardy-Poncet B, Elalamy I, Morange P, Gruel Y, Wolf M, Francois D, Racadot E, Camarasa P, Blouch MT, Nguyen F, Doubine S, Dutrillaux F, Alhenc-Gelas M, Martin-Toutain I, Bauters A, Ffrench P, de Maistre E, Grunebaum L, Mouton C, Huisse MG, Gouault-Heilmann M, Lucke V: Predictive factors for thrombosis and major bleeding in an observational study in 181 patients with heparin-induced thrombocytopenia treated with lepirudin. Blood. 2006 Sep 1;108(5):1492-6. Epub 2006 May 11. [PubMed:16690967]
  8. 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]
  9. 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]
  10. 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]
  11. 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]
  12. 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]
  13. 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]
  14. 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]
  15. 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]
  16. 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]
  17. 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]
  18. 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]
  19. 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]
  20. 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]
  21. Saku K, Zhang B, Noda K: Randomized head-to-head comparison of pitavastatin, atorvastatin, and rosuvastatin for safety and efficacy (quantity and quality of LDL): the PATROL trial. Circ J. 2011;75(6):1493-505. Epub 2011 Apr 15. [PubMed:21498906]
  22. Teramoto T: The clinical impact of pitavastatin: comparative studies with other statins on LDL-C and HDL-C. Expert Opin Pharmacother. 2012 Apr;13(6):859-65. doi: 10.1517/14656566.2012.660525. Epub 2012 Feb 15. [PubMed:22332608]
  23. Teramoto T, Shimano H, Yokote K, Urashima M: Effects of pitavastatin (LIVALO Tablet) on high density lipoprotein cholesterol (HDL-C) in hypercholesterolemia. J Atheroscler Thromb. 2009 Oct;16(5):654-61. doi: 10.5551/jat.1719. [PubMed:19907105]
  24. 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]
  25. Hoy SM: Pitavastatin: A Review in Hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168. doi: 10.1007/s40256-017-0213-8. [PubMed:28130659]
  26. 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]
  27. Ieiri I, Suwannakul S, Maeda K, Uchimaru H, Hashimoto K, Kimura M, Fujino H, Hirano M, Kusuhara H, Irie S, Higuchi S, Sugiyama Y: SLCO1B1 (OATP1B1, an uptake transporter) and ABCG2 (BCRP, an efflux transporter) variant alleles and pharmacokinetics of pitavastatin in healthy volunteers. Clin Pharmacol Ther. 2007 Nov;82(5):541-7. doi: 10.1038/sj.clpt.6100190. Epub 2007 Apr 25. [PubMed:17460607]
  28. 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]
  29. FDA Label - Pitavastatin [File]
External Links
Human Metabolome Database
HMDB0041991
KEGG Drug
D01862
KEGG Compound
C13334
PubChem Compound
5282452
PubChem Substance
175427122
ChemSpider
4445604
BindingDB
86707
ChEBI
32020
ChEMBL
CHEMBL1201753
PharmGKB
PA142650384
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Pitavastatin
ATC Codes
C10AA08 — Pitavastatin
MSDS
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Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableHealthy Volunteers1
1CompletedNot AvailableHigh Blood Pressure (Hypertension) / Hyperlipidemias1
1CompletedNot AvailableHyperlipidemias1
1CompletedBasic ScienceHealthy Male Volunteers1
1CompletedOtherHigh Blood Pressure (Hypertension) / Hyperlipidemias1
1CompletedSupportive CareHealthy Volunteers1
1CompletedTreatmentHealthy Volunteers1
1CompletedTreatmentHigh Cholesterol1
1CompletedTreatmentInfluenza in Humans1
1CompletedTreatmentMetabolic Syndromes1
1CompletedTreatmentImpaired kidney function1
1Unknown StatusNot AvailableHuman Immunodeficiency Virus (HIV) / Hyperlipidemias1
2CompletedTreatmentHigh Cholesterol1
3Active Not RecruitingPreventionCardiovascular Heart Disease / Human Immunodeficiency Virus (HIV) Infections1
3CompletedTreatmentComplex-dyslipidemia1
3CompletedTreatmentCoronary Heart Disease (CHD) / Dyslipidemias / High Cholesterol1
3CompletedTreatmentDyslipidemia (Fredrickson Type Ⅱa) / Dyslipidemias1
3CompletedTreatmentDyslipidemias / High Blood Pressure (Hypertension)1
3CompletedTreatmentDyslipidemias / High Cholesterol4
3CompletedTreatmentDyslipidemias / Type 2 Diabetes Mellitus2
3CompletedTreatmentHigh Cholesterol1
3CompletedTreatmentHypercholesterolemia or Combined Dyslipidemia1
3RecruitingTreatmentBMI >30 kg/m2 / Dyslipidemias1
3TerminatedTreatmentDyslipidemias / Hyperlipidemias2
3Unknown StatusTreatmentHyperlipidemias1
4Active Not RecruitingTreatmentAnginal Pain / Atherosclerosis / Neointima1
4Active Not RecruitingTreatmentChronic Kidney Disease (CKD)1
4Active Not RecruitingTreatmentDyslipidemias1
4CompletedNot AvailableHealthy Volunteers4
4CompletedNot AvailableSeverely impaired renal function1
4CompletedBasic ScienceHealthy Volunteers1
4CompletedPreventionDiabetes Mellitus (DM) / Impaired Glucose Tolerance1
4CompletedTreatmentCardiovascular Risk / High Blood Pressure (Hypertension)1
4CompletedTreatmentChronic Heart Failure (CHF)1
4CompletedTreatmentCoronary Artery Disease / High Cholesterol1
4CompletedTreatmentCoronary Heart Disease (CHD) / High Cholesterol2
4CompletedTreatmentDyslipidemias1
4CompletedTreatmentDyslipidemias / Human Immunodeficiency Virus (HIV)1
4CompletedTreatmentHbA1c Level Associated With Lipid Compositions1
4CompletedTreatmentHigh Cholesterol2
4CompletedTreatmentHigh Cholesterol / Metabolic Syndromes1
4CompletedTreatmentHypercholesterolemia With Type2DM1
4CompletedTreatmentInflammatory Reaction / Metabolic Syndromes / Oxidative Stress1
4CompletedTreatmentMixed hypercholesterolemia / Primary Dyslipidemia1
4CompletedTreatmentStable Angina or Acute Coronary Syndrome Considered for Percutaneous Coronary Intervention With Dyslipidemia or Hypertension1
4Not Yet RecruitingDiagnosticCoronary Artery Disease1
4RecruitingTreatmentDyslipidemias / High Blood Pressure (Hypertension) / Prediabetic State1
4RecruitingTreatmentMetabolic Syndromes1
4Unknown StatusPreventionProphylaxis of Contrast-induced nephropathy1
4WithdrawnPreventionPercutaneous Coronary Intervention1
Not AvailableActive Not RecruitingNot AvailableHuman Immunodeficiency Virus Type 1 (HIV-1) Infection1
Not AvailableCompletedPreventionBreast Cancer1
Not AvailableCompletedTreatmentBMI >30 kg/m2 / Fatty Liver, Nonalcoholic1
Not AvailableCompletedTreatmentHealthy Volunteers1
Not AvailableNot Yet RecruitingOtherDyslipidemias1
Not AvailableRecruitingPreventionCoronary Artery Disease1
Not AvailableRecruitingTreatmentASCVD / Dyslipidemias / Lipid-Lowering Therapy / Statin / Subclinical hypothyroïdism1
Not AvailableTerminatedTreatmentAlzheimer's Disease (AD) / High Cholesterol1
Not AvailableUnknown StatusPreventionCardiovascular Heart Disease1
Not AvailableUnknown StatusTreatmentCarotid Artery Diseases / Hyperlipidemias1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Tablet, film coatedOral1 mg/1
Tablet, film coatedOral2 mg/1
Tablet, film coatedOral4 mg/1
Tablet, film coatedOral1.045 mg/1
Tablet, film coatedOral2.09 mg/1
Tablet, film coatedOral4.18 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6465477No2002-10-152016-12-20Us
US5753675No1998-05-192015-05-19Us
US5856336Yes1999-01-052021-06-25Us
US7022713Yes2006-04-042024-08-19Us
US5854259No1998-12-292015-12-29Us
US8557993Yes2013-10-152024-08-02Us
US8829186No2014-09-092031-01-19Us
Additional Data Available
  • Filed On
    Filed On

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

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityVery slightly soluble FDA label
Predicted Properties
PropertyValueSource
Water Solubility0.00394 mg/mLALOGPS
logP3.75ALOGPS
logP2.92ChemAxon
logS-5ALOGPS
pKa (Strongest Acidic)4.13ChemAxon
pKa (Strongest Basic)4.86ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area90.65 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity115.74 m3·mol-1ChemAxon
Polarizability43.76 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9735
Blood Brain Barrier+0.9296
Caco-2 permeable+0.5135
P-glycoprotein substrateSubstrate0.5
P-glycoprotein inhibitor INon-inhibitor0.9015
P-glycoprotein inhibitor IINon-inhibitor0.9672
Renal organic cation transporterNon-inhibitor0.9101
CYP450 2C9 substrateNon-substrate0.7757
CYP450 2D6 substrateNon-substrate0.7668
CYP450 3A4 substrateNon-substrate0.5634
CYP450 1A2 substrateNon-inhibitor0.6867
CYP450 2C9 inhibitorNon-inhibitor0.7168
CYP450 2D6 inhibitorNon-inhibitor0.8695
CYP450 2C19 inhibitorNon-inhibitor0.8563
CYP450 3A4 inhibitorNon-inhibitor0.6855
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6481
Ames testNon AMES toxic0.837
CarcinogenicityNon-carcinogens0.9038
BiodegradationNot ready biodegradable0.997
Rat acute toxicity3.1821 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.987
hERG inhibition (predictor II)Non-inhibitor0.926
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
MS/MS Spectrum - DI-ESI-qTof , NegativeLC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as phenylquinolines. These are heterocyclic compounds containing a quinoline moiety substituted with a phenyl group.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Quinolines and derivatives
Sub Class
Phenylquinolines
Direct Parent
Phenylquinolines
Alternative Parents
Phenylpyridines / Medium-chain hydroxy acids and derivatives / Medium-chain fatty acids / Beta hydroxy acids and derivatives / Fluorobenzenes / Halogenated fatty acids / Heterocyclic fatty acids / Hydroxy fatty acids / Unsaturated fatty acids / Aryl fluorides
show 11 more
Substituents
Phenylquinoline / 4-phenylpyridine / Medium-chain hydroxy acid / Medium-chain fatty acid / Beta-hydroxy acid / Fluorobenzene / Halobenzene / Halogenated fatty acid / Heterocyclic fatty acid / Hydroxy fatty acid
show 27 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
quinolines, statin (synthetic), cyclopropanes, dihydroxy monocarboxylic acid, monofluorobenzenes (CHEBI:32020)

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. Morgan RE, Campbell SE, Yu CY, Sponseller CA, Muster HA: Comparison of the safety, tolerability, and pharmacokinetic profile of a single oral dose of pitavastatin 4 mg in adult subjects with severe renal impairment not on hemodialysis versus healthy adult subjects. J Cardiovasc Pharmacol. 2012 Jul;60(1):42-8. doi: 10.1097/FJC.0b013e318256cdf0. [PubMed:22472908]
  2. Hoy SM: Pitavastatin: A Review in Hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168. doi: 10.1007/s40256-017-0213-8. [PubMed:28130659]
  3. FDA Label - Pitavastatin [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Metal ion binding
Specific Function
Integrin alpha-L/beta-2 is a receptor for ICAM1, ICAM2, ICAM3 and ICAM4. It is involved in a variety of immune phenomena including leukocyte-endothelial cell interaction, cytotoxic T-cell mediated ...
Gene Name
ITGAL
Uniprot ID
P20701
Uniprot Name
Integrin alpha-L
Molecular Weight
128768.495 Da
References
  1. Weitz-Schmidt G, Welzenbach K, Brinkmann V, Kamata T, Kallen J, Bruns C, Cottens S, Takada Y, Hommel U: Statins selectively inhibit leukocyte function antigen-1 by binding to a novel regulatory integrin site. Nat Med. 2001 Jun;7(6):687-92. doi: 10.1038/89058. [PubMed:11385505]
  2. Liao JK, Laufs U: Pleiotropic effects of statins. Annu Rev Pharmacol Toxicol. 2005;45:89-118. doi: 10.1146/annurev.pharmtox.45.120403.095748. [PubMed:15822172]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Glucuronosyltransferase activity
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.Its unique specificity for 3,4-catechol estrogens and estriol su...
Gene Name
UGT2B7
Uniprot ID
P16662
Uniprot Name
UDP-glucuronosyltransferase 2B7
Molecular Weight
60694.12 Da
References
  1. Morgan RE, Campbell SE, Yu CY, Sponseller CA, Muster HA: Comparison of the safety, tolerability, and pharmacokinetic profile of a single oral dose of pitavastatin 4 mg in adult subjects with severe renal impairment not on hemodialysis versus healthy adult subjects. J Cardiovasc Pharmacol. 2012 Jul;60(1):42-8. doi: 10.1097/FJC.0b013e318256cdf0. [PubMed:22472908]
  2. Hoy SM: Pitavastatin: A Review in Hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168. doi: 10.1007/s40256-017-0213-8. [PubMed:28130659]
  3. FDA Label - Pitavastatin [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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. Morgan RE, Campbell SE, Yu CY, Sponseller CA, Muster HA: Comparison of the safety, tolerability, and pharmacokinetic profile of a single oral dose of pitavastatin 4 mg in adult subjects with severe renal impairment not on hemodialysis versus healthy adult subjects. J Cardiovasc Pharmacol. 2012 Jul;60(1):42-8. doi: 10.1097/FJC.0b013e318256cdf0. [PubMed:22472908]
  2. Hoy SM: Pitavastatin: A Review in Hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168. doi: 10.1007/s40256-017-0213-8. [PubMed:28130659]
  3. FDA Label - Pitavastatin [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Morgan RE, Campbell SE, Yu CY, Sponseller CA, Muster HA: Comparison of the safety, tolerability, and pharmacokinetic profile of a single oral dose of pitavastatin 4 mg in adult subjects with severe renal impairment not on hemodialysis versus healthy adult subjects. J Cardiovasc Pharmacol. 2012 Jul;60(1):42-8. doi: 10.1097/FJC.0b013e318256cdf0. [PubMed:22472908]
  2. Hoy SM: Pitavastatin: A Review in Hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168. doi: 10.1007/s40256-017-0213-8. [PubMed:28130659]
  3. Pitavastatin FDA Label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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. Morgan RE, Campbell SE, Yu CY, Sponseller CA, Muster HA: Comparison of the safety, tolerability, and pharmacokinetic profile of a single oral dose of pitavastatin 4 mg in adult subjects with severe renal impairment not on hemodialysis versus healthy adult subjects. J Cardiovasc Pharmacol. 2012 Jul;60(1):42-8. doi: 10.1097/FJC.0b013e318256cdf0. [PubMed:22472908]
  2. FDA Label - Pitavastatin [File]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. FDA Label - Pitavastatin [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Not Available
Specific Function
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
Gene Name
ORM1
Uniprot ID
P02763
Uniprot Name
Alpha-1-acid glycoprotein 1
Molecular Weight
23511.38 Da
References
  1. FDA Label - Pitavastatin [File]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. Hirano M, Maeda K, Shitara Y, Sugiyama Y: Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans. J Pharmacol Exp Ther. 2004 Oct;311(1):139-46. Epub 2004 May 24. [PubMed:15159445]
  2. Karlgren M, Ahlin G, Bergstrom CA, Svensson R, Palm J, Artursson P: In vitro and in silico strategies to identify OATP1B1 inhibitors and predict clinical drug-drug interactions. Pharm Res. 2012 Feb;29(2):411-26. doi: 10.1007/s11095-011-0564-9. Epub 2011 Aug 23. [PubMed:21861202]
  3. Hoy SM: Pitavastatin: A Review in Hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168. doi: 10.1007/s40256-017-0213-8. [PubMed:28130659]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as 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. Hirano M, Maeda K, Shitara Y, Sugiyama Y: Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans. J Pharmacol Exp Ther. 2004 Oct;311(1):139-46. Epub 2004 May 24. [PubMed:15159445]
  2. Hoy SM: Pitavastatin: A Review in Hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168. doi: 10.1007/s40256-017-0213-8. [PubMed:28130659]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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. Morgan RE, Campbell SE, Yu CY, Sponseller CA, Muster HA: Comparison of the safety, tolerability, and pharmacokinetic profile of a single oral dose of pitavastatin 4 mg in adult subjects with severe renal impairment not on hemodialysis versus healthy adult subjects. J Cardiovasc Pharmacol. 2012 Jul;60(1):42-8. doi: 10.1097/FJC.0b013e318256cdf0. [PubMed:22472908]
  2. Hoy SM: Pitavastatin: A Review in Hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168. doi: 10.1007/s40256-017-0213-8. [PubMed:28130659]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Virus receptor activity
Specific Function
The hepatic sodium/bile acid uptake system exhibits broad substrate specificity and transports various non-bile acid organic compounds as well. It is strictly dependent on the extracellular presenc...
Gene Name
SLC10A1
Uniprot ID
Q14973
Uniprot Name
Sodium/bile acid cotransporter
Molecular Weight
38118.64 Da
References
  1. Morgan RE, Campbell SE, Yu CY, Sponseller CA, Muster HA: Comparison of the safety, tolerability, and pharmacokinetic profile of a single oral dose of pitavastatin 4 mg in adult subjects with severe renal impairment not on hemodialysis versus healthy adult subjects. J Cardiovasc Pharmacol. 2012 Jul;60(1):42-8. doi: 10.1097/FJC.0b013e318256cdf0. [PubMed:22472908]
  2. Hoy SM: Pitavastatin: A Review in Hypercholesterolemia. Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168. doi: 10.1007/s40256-017-0213-8. [PubMed:28130659]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. Morgan RE, Campbell SE, Yu CY, Sponseller CA, Muster HA: Comparison of the safety, tolerability, and pharmacokinetic profile of a single oral dose of pitavastatin 4 mg in adult subjects with severe renal impairment not on hemodialysis versus healthy adult subjects. J Cardiovasc Pharmacol. 2012 Jul;60(1):42-8. doi: 10.1097/FJC.0b013e318256cdf0. [PubMed:22472908]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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. Morgan RE, Campbell SE, Yu CY, Sponseller CA, Muster HA: Comparison of the safety, tolerability, and pharmacokinetic profile of a single oral dose of pitavastatin 4 mg in adult subjects with severe renal impairment not on hemodialysis versus healthy adult subjects. J Cardiovasc Pharmacol. 2012 Jul;60(1):42-8. doi: 10.1097/FJC.0b013e318256cdf0. [PubMed:22472908]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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. Morgan RE, Campbell SE, Yu CY, Sponseller CA, Muster HA: Comparison of the safety, tolerability, and pharmacokinetic profile of a single oral dose of pitavastatin 4 mg in adult subjects with severe renal impairment not on hemodialysis versus healthy adult subjects. J Cardiovasc Pharmacol. 2012 Jul;60(1):42-8. doi: 10.1097/FJC.0b013e318256cdf0. [PubMed:22472908]
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 March 03, 2013 16:50 / Updated on December 02, 2019 08:30