Identification

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

Pitavastatin a lipid-lowering agent that belongs to the statin class of medications for treatment of dyslipidemia. It is also used for primary and secondary prevention of cardiovascular disease. FDA approved in Aug 3, 2009.

Structure
Thumb
Synonyms
  • Pitavastatia
  • Pitavastatine
  • Pitavastatinum
External IDs
NK 104 / NK-104 / NKS-104 / NKS104
Product Ingredients
IngredientUNIICASInChI Key
Pitavastatin calciumIYD54XEG3W147526-32-7RHGYHLPFVJEAOC-WUVPNHNWSA-L
Pitavastatin magnesiumNot Available956116-90-8MPAZKXHCZWDZDY-FFNUKLMVSA-L
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
LivaloTablet, film coated1.045 mg/1OralKowa Company, Ltd.2010-05-15Not applicableUs66869 0104 90 nlmimage10 323c1910
LivaloTablet, film coated1 mg/1OralEli Lilly & Co. Ltd.2010-05-152016-01-31Us00002 4770 90 nlmimage10 9516caa6
LivaloTablet, film coated4.18 mg/1OralKowa Company, Ltd.2010-05-15Not applicableUs66869 0404 90 nlmimage10 d93c6ce3
LivaloTablet, film coated4 mg/1OralEli Lilly & Co. Ltd.2010-05-152016-01-31Us00002 4772 90 nlmimage10 8c16c656
LivaloTablet, film coated2.09 mg/1OralKowa Company, Ltd.2010-05-15Not applicableUs66869 0204 90 nlmimage10 293c1490
LivaloTablet, film coated2 mg/1OralEli Lilly & Co. Ltd.2010-05-152016-01-31Us00002 4771 90 nlmimage10 8f16c7a6
ZypitamagTablet, film coated4 mg/1OralCadila Healthcare Limited2018-03-09Not applicableUs
ZypitamagTablet, film coated4 mg/1OralMedicure International Inc2018-03-09Not applicableUs
ZypitamagTablet, film coated2 mg/1OralCadila Healthcare Limited2018-03-09Not applicableUs
ZypitamagTablet, film coated2 mg/1OralMedicure International Inc2018-03-09Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
PitavastatinTablet, film coated1 mg/1OralStason Pharmaceuticals, Inc.2017-12-252018-01-19Us
PitavastatinTablet, film coated1 mg/1OralQuinn Pharmaceuticals, Llc2017-03-312017-03-31Us
PitavastatinTablet, film coated1.045 mg/1OralOrient Pharma Co., Ltd.2018-07-252018-07-25Us
PitavastatinTablet, film coated4 mg/1OralStason Pharmaceuticals, Inc.2017-12-252018-01-19Us
PitavastatinTablet, film coated4 mg/1OralQuinn Pharmaceuticals, Llc2017-03-312017-03-31Us
PitavastatinTablet, film coated4.18 mg/1OralOrient Pharma Co., Ltd.2018-07-252018-07-25Us
PitavastatinTablet, film coated2 mg/1OralStason Pharmaceuticals, Inc.2017-12-252018-01-19Us
PitavastatinTablet, film coated2 mg/1OralQuinn Pharmaceuticals, Llc2017-03-312017-03-31Us
PitavastatinTablet, film coated2.09 mg/1OralOrient Pharma Co., Ltd.2018-07-252018-07-25Us
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 used to lower serum levels of total cholesterol, LDL-C, apolipoprotein B, and triglycerides, and raise levels of HDL-C for the treatment of dyslipidemia.

Associated Conditions
Pharmacodynamics

The magnitude of LDL-C reduction by pitavastatin (2 mg and 4 mg) is comparable to atorvastatin (10 mg and 20 mg) and simvastatin (20 mg and 40 mg). It also does not prolong the QTc interval to a clinically significant degree.

Mechanism of action

Pitavastatin is lipid-lowering agent that works to control the synthesis of cholesterol via competitive inhibition of the liver enzyme, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. As a result, a compensatory increase in LDL-receptor expression can be observed which facilitates an increase LDL catabolism.

TargetActionsOrganism
A3-hydroxy-3-methylglutaryl-coenzyme A reductase
inhibitor
Human
Absorption

Bioavailability = 51%; Time to peak, plasma = 1 hour; Pitavastatin was absorbed in the small intestine but very little in the colon. Cmax decreases by 43% if pitavastatin is taken with a fatty meal but there are no significant changes to AUC or baseline LDL levels compared to fasting state. The Cmax and AUC of pitavastatin did not differ following evening or morning drug administration.

Volume of distribution

148 L

Protein binding

>99% protein bound in human plasma, mainly to albumin and alpha 1-acid glycoprotein.

Metabolism

Pitavastatin is mainly metabolized by liver. It undergoes glucuronidation by uridine 5-diphosphate glucuronosyl transferases (UGT1A3 and UGT2B7) to form the major circulating metabolite, pitavastatin lactone.

The cytochrome P450 system has little involvement with the metabolism of pitavastatin. There is some metabolism by CYP2C9 and to a lesser extent, CYP2C8. Studies suggest that concomitant therapy with drugs that are involved with the cytochrome P450 system will not effect the pharmacokinetics of pitavastatin.

Route of elimination

79% in feces and 15% excreted in urine.

Half life

Plasma elimination half-lfie = 12 hours

Clearance

CL/F (apparent clearance), 4 mg, healthy male Korean subjects = 23.6 L/h

Toxicity

The most frequent adverse reactions (rate ≥2.0% in at least one marketed dose) were myalgia, back pain, diarrhea, constipation and pain in extremity.

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

Interactions

Drug Interactions
DrugInteraction
6-Deoxyerythronolide BThe risk or severity of rhabdomyolysis can be increased when 6-Deoxyerythronolide B is combined with Pitavastatin.
AbirateroneThe serum concentration of Pitavastatin can be increased when it is combined with Abiraterone.
AcenocoumarolThe risk or severity of bleeding can be increased when Pitavastatin is combined with Acenocoumarol.
AcetaminophenThe serum concentration of Pitavastatin can be increased when it is combined with Acetaminophen.
AcetazolamideThe serum concentration of Pitavastatin can be increased when it is combined with Acetazolamide.
Acetyl sulfisoxazoleThe serum concentration of Pitavastatin can be increased when it is combined with Acetyl sulfisoxazole.
AcipimoxAcipimox may increase the myopathic rhabdomyolysis activities of Pitavastatin.
AlmasilateThe serum concentration of Pitavastatin can be decreased when it is combined with Almasilate.
AloglutamolThe serum concentration of Pitavastatin can be decreased when it is combined with Aloglutamol.
AluminiumThe serum concentration of Pitavastatin can be decreased when it is combined with Aluminium.
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]
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
FDA label
Download (460 KB)
MSDS
Download (116 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableHealthy Volunteers1
1CompletedNot AvailableHigh Blood Pressure (Hypertension) / Hyperlipidemias1
1CompletedOtherHigh Blood Pressure (Hypertension) / Hyperlipidemias1
1CompletedSupportive CareHealthy Volunteers1
1CompletedTreatmentHigh Blood Cholesterol Level1
1CompletedTreatmentImpaired Renal Function1
1CompletedTreatmentInfluenza in Humans1
1CompletedTreatmentMetabolic Syndromes1
1Unknown StatusNot AvailableHuman Immunodeficiency Virus (HIV) / Hyperlipidemias1
3CompletedTreatmentCoronary Heart Disease (CHD) / Dyslipidemias / High Blood Cholesterol Level1
3CompletedTreatmentDyslipidemia (Fredrickson Type Ⅱa) / Dyslipidemias1
3CompletedTreatmentDyslipidemias / High Blood Cholesterol Level4
3CompletedTreatmentDyslipidemias / High Blood Pressure (Hypertension)1
3CompletedTreatmentDyslipidemias / Type 2 Diabetes Mellitus2
3CompletedTreatmentHigh Blood Cholesterol Level1
3CompletedTreatmentHypercholesterolemia or Combined Dyslipidemia1
3RecruitingPreventionCardiovascular Disease (CVD) / Human Immunodeficiency Virus (HIV) Infections1
3RecruitingTreatmentBMI >30 kg/m2 / Dyslipidemias1
3TerminatedTreatmentDyslipidemias / Hyperlipidemias2
3Unknown StatusTreatmentHyperlipidemias1
4Active Not RecruitingBasic ScienceHealthy Volunteers1
4Active Not RecruitingTreatmentAnginal Pain / Atherosclerosis / Neointima1
4Active Not RecruitingTreatmentChronic Kidney Disease (CKD)1
4Active Not RecruitingTreatmentDyslipidemias1
4CompletedNot AvailableHealthy Volunteers3
4CompletedNot AvailableSevere Renal Impairment1
4CompletedTreatmentCardiovascular Risks / High Blood Pressure (Hypertension)1
4CompletedTreatmentChronic Heart Failure (CHF)1
4CompletedTreatmentCoronary Artery Disease / High Blood Cholesterol Level1
4CompletedTreatmentCoronary Heart Disease (CHD) / High Blood Cholesterol Level2
4CompletedTreatmentDyslipidemias1
4CompletedTreatmentDyslipidemias / Human Immunodeficiency Virus (HIV)1
4CompletedTreatmentHbA1c Level Associated With Lipid Compositions1
4CompletedTreatmentHigh Blood Cholesterol Level2
4CompletedTreatmentHigh Blood Cholesterol Level / Metabolic Syndromes1
4CompletedTreatmentHypercholesterolemia With Type2DM1
4CompletedTreatmentInflammatory Reaction / Metabolic Syndromes / Oxidative Stress1
4CompletedTreatmentMixed hypercholesterolemia / Primary Dyslipidemia1
4Not Yet RecruitingDiagnosticCoronary Artery Disease1
4RecruitingTreatmentDyslipidemias / High Blood Pressure (Hypertension) / Prediabetic State1
4Unknown StatusPreventionProphylaxis of Contrast-induced nephropathy1
4WithdrawnPreventionPercutaneous Coronary Intervention1
Not AvailableActive Not RecruitingNot AvailableInfection, Human Immunodeficiency Virus I1
Not AvailableCompletedTreatmentBMI >30 kg/m2 / Fatty Liver, Nonalcoholic1
Not AvailableCompletedTreatmentHealthy Volunteers1
Not AvailableNot Yet RecruitingTreatmentDyslipidemias / Lipid-Lowering Therapy / Statin / Subclinical hypothyroïdism1
Not AvailableRecruitingPreventionCoronary Artery Disease1
Not AvailableTerminatedTreatmentAlzheimer's Disease (AD) / High Blood Cholesterol Level1
Not AvailableUnknown StatusPreventionCardiovascular Disease (CVD)1
Not AvailableUnknown StatusTreatmentCarotid Artery Diseases / Hyperlipidemias1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Tablet, film coatedOral1 mg/1
Tablet, film coatedOral1.045 mg/1
Tablet, film coatedOral2 mg/1
Tablet, film coatedOral2.09 mg/1
Tablet, film coatedOral4 mg/1
Tablet, film coatedOral4.18 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6465477No2009-08-032016-12-20Us
US5753675No2009-08-032015-05-19Us
US5856336No2009-08-032016-01-05Us
US7022713No2009-08-032024-02-19Us
US5854259No2009-08-032015-12-29Us
US8557993No2004-02-022024-02-02Us
US8829186No2011-01-192031-01-19Us

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
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Nadph binding
Specific Function
Transmembrane glycoprotein that is the rate-limiting enzyme in cholesterol biosynthesis as well as in the biosynthesis of nonsterol isoprenoids that are essential for normal cell function including...
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]

Enzymes

Kind
Protein
Organism
Human
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]
Kind
Protein
Organism
Human
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]
Kind
Protein
Organism
Human
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]
Kind
Protein
Organism
Human
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]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
Kind
Protein
Organism
Human
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

Transporters

Kind
Protein
Organism
Human
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]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as 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]
Kind
Protein
Organism
Human
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]
Kind
Protein
Organism
Human
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]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both 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
Human
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
Human
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
Human
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 August 15, 2018 09:55