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Identification
NamePitavastatin
Accession NumberDB08860  (DB06514)
TypeSmall Molecule
GroupsApproved
DescriptionPitavastatin 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 Identifiers
  • NK 104
  • NK-104
  • NKS-104
  • NKS104
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
LivaloTablet, film coated1 mg/1OralEli Lilly and Company2010-05-152016-10-13Us
LivaloTablet, film coated2.09 mg/1OralKowa Pharmaceuticals America, Inc.2010-05-15Not applicableUs
LivaloTablet, film coated2 mg/1OralEli Lilly and Company2010-05-152016-10-13Us
LivaloTablet, film coated4.18 mg/1OralKowa Pharmaceuticals America, Inc.2010-05-15Not applicableUs
LivaloTablet, film coated4 mg/1OralEli Lilly and Company2010-05-152016-10-13Us
LivaloTablet, film coated1.045 mg/1OralKowa Pharmaceuticals America, Inc.2010-05-15Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Pitavastatin Calcium
147526-32-7
Thumb
  • InChI Key: RHGYHLPFVJEAOC-FFNUKLMVSA-L
  • Monoisotopic Mass: 880.284814023
  • Average Mass: 880.984
DBSALT000140
Categories
UNIIM5681Q5F9P
CAS number147511-69-1
WeightAverage: 421.4608
Monoisotopic: 421.168936466
Chemical FormulaC25H24FNO4
InChI KeyVGYFMXBACGZSIL-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[[email protected]](C[[email protected]](O)\C=C\C1=C(N=C2C=CC=CC2=C1C1=CC=C(F)C=C1)C1CC1)CC(O)=O
Pharmacology
IndicationPitavastatin 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.
Structured Indications
PharmacodynamicsThe 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 actionPitavastatin 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.
TargetKindPharmacological actionActionsOrganismUniProt ID
3-hydroxy-3-methylglutaryl-coenzyme A reductaseProteinyes
inhibitor
HumanP04035 details
Related Articles
AbsorptionBioavailability = 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 elimination79% in feces and 15% excreted in urine.
Half lifePlasma elimination half-lfie = 12 hours
Clearance

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

ToxicityThe 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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbirateroneThe serum concentration of Pitavastatin can be increased when it is combined with Abiraterone.Approved
AcenocoumarolPitavastatin may increase the anticoagulant activities of Acenocoumarol.Approved
AcetaminophenThe serum concentration of Pitavastatin can be increased when it is combined with Acetaminophen.Approved
AcipimoxAcipimox may increase the myopathic rhabdomyolysis activities of Pitavastatin.Approved
AfatinibThe serum concentration of Pitavastatin can be increased when it is combined with Afatinib.Approved
AlbendazoleThe serum concentration of Pitavastatin can be increased when it is combined with Albendazole.Approved, Vet Approved
AldosteroneThe serum concentration of Pitavastatin can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Pitavastatin can be increased when it is combined with Alectinib.Approved
AlfentanilThe serum concentration of Pitavastatin can be increased when it is combined with Alfentanil.Approved, Illicit
Aluminum hydroxideThe serum concentration of Pitavastatin can be decreased when it is combined with Aluminum hydroxide.Approved
Aluminum phosphateThe serum concentration of Pitavastatin can be decreased when it is combined with Aluminum phosphate.Approved
AmantadineThe serum concentration of Pitavastatin can be increased when it is combined with Amantadine.Approved
Aminohippuric acidThe serum concentration of Pitavastatin can be increased when it is combined with Aminohippuric acid.Approved
AmiodaroneThe metabolism of Pitavastatin can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Pitavastatin can be increased when it is combined with Amitriptyline.Approved
AmlodipineThe serum concentration of Pitavastatin can be increased when it is combined with Amlodipine.Approved
AmprenavirThe serum concentration of Pitavastatin can be decreased when it is combined with Amprenavir.Approved
AmsacrineThe serum concentration of Pitavastatin can be increased when it is combined with Amsacrine.Approved
AprepitantThe metabolism of Pitavastatin can be increased when combined with Aprepitant.Approved, Investigational
AstemizoleThe serum concentration of Pitavastatin can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe serum concentration of Pitavastatin can be increased when it is combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Pitavastatin can be increased when it is combined with Atenolol.Approved
AtorvastatinThe serum concentration of Pitavastatin can be increased when it is combined with Atorvastatin.Approved
AzelastineThe serum concentration of Pitavastatin can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Pitavastatin can be increased when it is combined with Azithromycin.Approved
BenzocaineThe serum concentration of Pitavastatin can be increased when it is combined with Benzocaine.Approved
BepridilThe serum concentration of Pitavastatin can be increased when it is combined with Bepridil.Approved, Withdrawn
BezafibrateBezafibrate may increase the myopathic rhabdomyolysis activities of Pitavastatin.Approved
BiperidenThe serum concentration of Pitavastatin can be increased when it is combined with Biperiden.Approved
Bismuth SubcitrateThe serum concentration of Pitavastatin can be decreased when it is combined with Bismuth Subcitrate.Approved
BoceprevirThe serum concentration of Pitavastatin can be increased when it is combined with Boceprevir.Approved
BosentanThe metabolism of Pitavastatin can be increased when combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Pitavastatin can be increased when it is combined with Bosutinib.Approved
BromocriptineThe serum concentration of Pitavastatin can be increased when it is combined with Bromocriptine.Approved, Investigational
BuprenorphineThe serum concentration of Pitavastatin can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe serum concentration of Pitavastatin can be increased when it is combined with Buspirone.Approved, Investigational
CabazitaxelThe serum concentration of Pitavastatin can be increased when it is combined with Cabazitaxel.Approved
CaffeineThe serum concentration of Pitavastatin can be increased when it is combined with Caffeine.Approved
Calcium carbonateThe serum concentration of Pitavastatin can be decreased when it is combined with Calcium carbonate.Approved
CanagliflozinThe serum concentration of Pitavastatin can be increased when it is combined with Canagliflozin.Approved
CandesartanThe serum concentration of Pitavastatin can be increased when it is combined with Candesartan.Approved
CapecitabineThe metabolism of Pitavastatin can be decreased when combined with Capecitabine.Approved, Investigational
CaptoprilThe serum concentration of Pitavastatin can be increased when it is combined with Captopril.Approved
CarbamazepineThe metabolism of Pitavastatin can be increased when combined with Carbamazepine.Approved, Investigational
CarvedilolThe serum concentration of Pitavastatin can be increased when it is combined with Carvedilol.Approved, Investigational
CaspofunginThe serum concentration of Pitavastatin can be increased when it is combined with Caspofungin.Approved
CelecoxibThe metabolism of Pitavastatin can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Pitavastatin can be increased when it is combined with Ceritinib.Approved
ChloroquineThe serum concentration of Pitavastatin can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorpromazineThe serum concentration of Pitavastatin can be increased when it is combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe serum concentration of Pitavastatin can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Pitavastatin can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
CholecalciferolThe metabolism of Pitavastatin can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CholesterolThe serum concentration of Pitavastatin can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Pitavastatin can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe serum concentration of Pitavastatin can be increased when it is combined with Cilazapril.Approved
CimetidineThe serum concentration of Pitavastatin can be decreased when it is combined with Cimetidine.Approved
CiprofibrateThe risk or severity of adverse effects can be increased when Ciprofibrate is combined with Pitavastatin.Approved
CiprofloxacinThe serum concentration of Pitavastatin can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CitalopramThe serum concentration of Pitavastatin can be increased when it is combined with Citalopram.Approved
ClarithromycinThe serum concentration of Pitavastatin can be increased when it is combined with Clarithromycin.Approved
ClofazimineThe serum concentration of Pitavastatin can be increased when it is combined with Clofazimine.Approved, Investigational
ClomipramineThe serum concentration of Pitavastatin can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClopidogrelThe metabolism of Pitavastatin can be decreased when combined with Clopidogrel.Approved, Nutraceutical
ClotrimazoleThe serum concentration of Pitavastatin can be decreased when it is combined with Clotrimazole.Approved, Vet Approved
CobicistatThe serum concentration of Pitavastatin can be increased when it is combined with Cobicistat.Approved
ColchicineColchicine may increase the myopathic rhabdomyolysis activities of Pitavastatin.Approved
ColforsinThe serum concentration of Pitavastatin can be increased when it is combined with Colforsin.Experimental
CrizotinibThe serum concentration of Pitavastatin can be increased when it is combined with Crizotinib.Approved
CyclophosphamideThe serum concentration of Pitavastatin can be increased when it is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe serum concentration of Pitavastatin can be increased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
CyclosporineThe serum concentration of Pitavastatin can be decreased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Pitavastatin can be increased when it is combined with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Pitavastatin can be decreased when it is combined with Dabrafenib.Approved
DaclatasvirThe serum concentration of Pitavastatin can be increased when it is combined with Daclatasvir.Approved
DactinomycinThe serum concentration of Pitavastatin can be increased when it is combined with Dactinomycin.Approved
DanazolThe serum concentration of Pitavastatin can be increased when it is combined with Danazol.Approved
DaptomycinThe risk or severity of adverse effects can be increased when Pitavastatin is combined with Daptomycin.Approved, Investigational
DasabuvirThe serum concentration of Pitavastatin can be increased when it is combined with Dasabuvir.Approved
DasatinibThe serum concentration of Pitavastatin can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Pitavastatin can be decreased when it is combined with Daunorubicin.Approved
DeferasiroxThe serum concentration of Pitavastatin can be increased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Pitavastatin can be decreased when combined with Delavirdine.Approved
DesipramineThe serum concentration of Pitavastatin can be increased when it is combined with Desipramine.Approved
DesloratadineThe serum concentration of Pitavastatin can be increased when it is combined with Desloratadine.Approved, Investigational
DexamethasoneThe serum concentration of Pitavastatin can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe serum concentration of Pitavastatin can be increased when it is combined with Dextromethorphan.Approved
DiclofenacThe serum concentration of Pitavastatin can be increased when it is combined with Diclofenac.Approved, Vet Approved
DicoumarolPitavastatin may increase the anticoagulant activities of Dicoumarol.Approved
DigoxinThe serum concentration of Pitavastatin can be decreased when it is combined with Digoxin.Approved
DihydroergotamineThe serum concentration of Pitavastatin can be increased when it is combined with Dihydroergotamine.Approved
DiltiazemThe serum concentration of Pitavastatin can be increased when it is combined with Diltiazem.Approved
DipyridamoleThe serum concentration of Pitavastatin can be increased when it is combined with Dipyridamole.Approved
DoxazosinThe serum concentration of Pitavastatin can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Pitavastatin can be increased when it is combined with Doxepin.Approved
DoxorubicinThe serum concentration of Pitavastatin can be decreased when it is combined with Doxorubicin.Approved, Investigational
DronabinolThe serum concentration of Pitavastatin can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneThe serum concentration of Pitavastatin can be increased when it is combined with Dronedarone.Approved
EfavirenzThe metabolism of Pitavastatin can be decreased when combined with Efavirenz.Approved, Investigational
ElbasvirThe serum concentration of Pitavastatin can be increased when it is combined with Elbasvir.Approved
EltrombopagThe serum concentration of Pitavastatin can be increased when it is combined with Eltrombopag.Approved
EnalaprilThe serum concentration of Pitavastatin can be increased when it is combined with Enalapril.Approved, Vet Approved
EnzalutamideThe serum concentration of Pitavastatin can be increased when it is combined with Enzalutamide.Approved
ErgonovineThe serum concentration of Pitavastatin can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Pitavastatin can be increased when it is combined with Ergotamine.Approved
ErythromycinThe serum concentration of Pitavastatin can be increased when it is combined with Erythromycin.Approved, Vet Approved
ErythromycinThe serum concentration of Pitavastatin can be decreased when it is combined with Erythromycin.Approved, Vet Approved
EstramustineThe serum concentration of Pitavastatin can be increased when it is combined with Estramustine.Approved
EstriolThe serum concentration of Pitavastatin can be decreased when it is combined with Estriol.Approved, Vet Approved
EstroneThe serum concentration of Pitavastatin can be decreased when it is combined with Estrone.Approved
Ethyl biscoumacetatePitavastatin may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
EtoposideThe serum concentration of Pitavastatin can be increased when it is combined with Etoposide.Approved
EtravirineThe serum concentration of Pitavastatin can be decreased when it is combined with Etravirine.Approved
FelodipineThe serum concentration of Pitavastatin can be increased when it is combined with Felodipine.Approved, Investigational
FenofibrateThe risk or severity of adverse effects can be increased when Fenofibrate is combined with Pitavastatin.Approved
FentanylThe serum concentration of Pitavastatin can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe serum concentration of Pitavastatin can be increased when it is combined with Fexofenadine.Approved
FidaxomicinThe serum concentration of Pitavastatin can be increased when it is combined with Fidaxomicin.Approved
FloxuridineThe metabolism of Pitavastatin can be decreased when combined with Floxuridine.Approved
FluconazoleThe metabolism of Pitavastatin can be decreased when combined with Fluconazole.Approved
FluindionePitavastatin may increase the anticoagulant activities of Fluindione.Investigational
FluorouracilThe metabolism of Pitavastatin can be decreased when combined with Fluorouracil.Approved
FluoxetineThe serum concentration of Pitavastatin can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe serum concentration of Pitavastatin can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Pitavastatin can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Pitavastatin can be increased when it is combined with Flurazepam.Approved, Illicit
FluvastatinThe metabolism of Pitavastatin can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe serum concentration of Pitavastatin can be increased when it is combined with Fluvoxamine.Approved, Investigational
FosphenytoinThe serum concentration of Pitavastatin can be decreased when it is combined with Fosphenytoin.Approved
Fusidic AcidThe risk or severity of adverse effects can be increased when Fusidic Acid is combined with Pitavastatin.Approved
GefitinibThe serum concentration of Pitavastatin can be increased when it is combined with Gefitinib.Approved, Investigational
GemfibrozilGemfibrozil may increase the myopathic rhabdomyolysis activities of Pitavastatin.Approved
GenisteinThe serum concentration of Pitavastatin can be increased when it is combined with Genistein.Investigational
GlyburideThe serum concentration of Pitavastatin can be increased when it is combined with Glyburide.Approved
GlycerolThe serum concentration of Pitavastatin can be increased when it is combined with Glycerol.Experimental
Gramicidin DThe serum concentration of Pitavastatin can be increased when it is combined with Gramicidin D.Approved
GrepafloxacinThe serum concentration of Pitavastatin can be increased when it is combined with Grepafloxacin.Withdrawn
HaloperidolThe serum concentration of Pitavastatin can be increased when it is combined with Haloperidol.Approved
HydrocortisoneThe serum concentration of Pitavastatin can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
IdelalisibThe serum concentration of Pitavastatin can be increased when it is combined with Idelalisib.Approved
ImatinibThe serum concentration of Pitavastatin can be increased when it is combined with Imatinib.Approved
ImipramineThe serum concentration of Pitavastatin can be increased when it is combined with Imipramine.Approved
IndinavirThe serum concentration of Pitavastatin can be decreased when it is combined with Indinavir.Approved
IndomethacinThe serum concentration of Pitavastatin can be increased when it is combined with Indomethacin.Approved, Investigational
IrbesartanThe metabolism of Pitavastatin can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoniumThe serum concentration of Pitavastatin can be increased when it is combined with Isavuconazonium.Approved, Investigational
ItraconazoleThe serum concentration of Pitavastatin can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Pitavastatin can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Pitavastatin can be increased when it is combined with Ivermectin.Approved, Vet Approved
KetamineThe serum concentration of Pitavastatin can be increased when it is combined with Ketamine.Approved, Vet Approved
KetoconazoleThe serum concentration of Pitavastatin can be increased when it is combined with Ketoconazole.Approved, Investigational
LansoprazoleThe serum concentration of Pitavastatin can be increased when it is combined with Lansoprazole.Approved, Investigational
Lanthanum carbonateThe serum concentration of Lanthanum carbonate can be decreased when it is combined with Pitavastatin.Approved
LapatinibThe serum concentration of Pitavastatin can be increased when it is combined with Lapatinib.Approved, Investigational
LeflunomideThe metabolism of Pitavastatin can be decreased when combined with Leflunomide.Approved, Investigational
LevofloxacinThe serum concentration of Pitavastatin can be increased when it is combined with Levofloxacin.Approved, Investigational
LevothyroxineThe serum concentration of Pitavastatin can be decreased when it is combined with Levothyroxine.Approved
LidocaineThe serum concentration of Pitavastatin can be increased when it is combined with Lidocaine.Approved, Vet Approved
LiothyronineThe serum concentration of Pitavastatin can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Pitavastatin can be decreased when it is combined with Liotrix.Approved
LisinoprilThe serum concentration of Pitavastatin can be increased when it is combined with Lisinopril.Approved, Investigational
LomitapideThe serum concentration of Pitavastatin can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Pitavastatin can be increased when it is combined with Loperamide.Approved
LopinavirThe metabolism of Pitavastatin can be decreased when combined with Lopinavir.Approved
LoratadineThe serum concentration of Pitavastatin can be increased when it is combined with Loratadine.Approved
LosartanThe serum concentration of Pitavastatin can be increased when it is combined with Losartan.Approved
LovastatinThe serum concentration of Pitavastatin can be increased when it is combined with Lovastatin.Approved, Investigational
LumacaftorThe serum concentration of Pitavastatin can be increased when it is combined with Lumacaftor.Approved
MagaldrateThe serum concentration of Pitavastatin can be decreased when it is combined with Magaldrate.Withdrawn
Magnesium carbonateThe serum concentration of Pitavastatin can be decreased when it is combined with Magnesium carbonate.Approved
Magnesium hydroxideThe serum concentration of Pitavastatin can be decreased when it is combined with Magnesium hydroxide.Approved
Magnesium oxideThe serum concentration of Pitavastatin can be decreased when it is combined with Magnesium oxide.Approved
Magnesium TrisilicateThe serum concentration of Pitavastatin can be decreased when it is combined with Magnesium Trisilicate.Approved
MaprotilineThe serum concentration of Pitavastatin can be increased when it is combined with Maprotiline.Approved
MebendazoleThe serum concentration of Pitavastatin can be increased when it is combined with Mebendazole.Approved, Vet Approved
MefloquineThe serum concentration of Pitavastatin can be increased when it is combined with Mefloquine.Approved
Megestrol acetateThe serum concentration of Pitavastatin can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MeprobamateThe serum concentration of Pitavastatin can be increased when it is combined with Meprobamate.Approved, Illicit
MethadoneThe serum concentration of Pitavastatin can be increased when it is combined with Methadone.Approved
MetoprololThe serum concentration of Pitavastatin can be increased when it is combined with Metoprolol.Approved, Investigational
MibefradilThe serum concentration of Pitavastatin can be increased when it is combined with Mibefradil.Withdrawn
MiconazoleThe serum concentration of Pitavastatin can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Pitavastatin can be decreased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Pitavastatin can be increased when it is combined with Mifepristone.Approved, Investigational
MitomycinThe serum concentration of Pitavastatin can be increased when it is combined with Mitomycin.Approved
MitoxantroneThe serum concentration of Pitavastatin can be decreased when it is combined with Mitoxantrone.Approved, Investigational
MorphineThe serum concentration of Pitavastatin can be increased when it is combined with Morphine.Approved, Investigational
NaltrexoneThe serum concentration of Pitavastatin can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Pitavastatin can be increased when it is combined with Naringenin.Experimental
NefazodoneThe serum concentration of Pitavastatin can be decreased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Pitavastatin can be decreased when it is combined with Nelfinavir.Approved
NeostigmineThe serum concentration of Pitavastatin can be increased when it is combined with Neostigmine.Approved, Vet Approved
NiacinThe risk or severity of adverse effects can be increased when Niacin is combined with Pitavastatin.Approved, Investigational, Nutraceutical
NicardipineThe metabolism of Pitavastatin can be decreased when combined with Nicardipine.Approved
NicotinamideThe risk or severity of adverse effects can be increased when Nicotinamide is combined with Pitavastatin.Approved
NifedipineThe serum concentration of Pitavastatin can be decreased when it is combined with Nifedipine.Approved
NilotinibThe serum concentration of Pitavastatin can be increased when it is combined with Nilotinib.Approved, Investigational
NisoldipineThe serum concentration of Pitavastatin can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Pitavastatin can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Pitavastatin can be increased when it is combined with Nitrendipine.Approved
NorethisteroneThe serum concentration of Pitavastatin can be decreased when it is combined with Norethisterone.Approved
OmbitasvirThe serum concentration of Pitavastatin can be increased when it is combined with Ombitasvir.Approved
OmeprazoleThe serum concentration of Pitavastatin can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
P-NitrophenolThe serum concentration of Pitavastatin can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe serum concentration of Pitavastatin can be increased when it is combined with Paclitaxel.Approved, Vet Approved
Palmitic AcidThe serum concentration of Pitavastatin can be increased when it is combined with Palmitic Acid.Experimental
PantoprazoleThe serum concentration of Pitavastatin can be increased when it is combined with Pantoprazole.Approved
ParitaprevirThe serum concentration of Pitavastatin can be increased when it is combined with Paritaprevir.Approved
ParoxetineThe serum concentration of Pitavastatin can be increased when it is combined with Paroxetine.Approved, Investigational
PazopanibPitavastatin may increase the hepatotoxic activities of Pazopanib.Approved
PerindoprilThe serum concentration of Pitavastatin can be increased when it is combined with Perindopril.Approved
PhenindionePitavastatin may increase the anticoagulant activities of Phenindione.Approved
PhenobarbitalThe metabolism of Pitavastatin can be increased when combined with Phenobarbital.Approved
PhenprocoumonPitavastatin may increase the anticoagulant activities of Phenprocoumon.Approved
PhenytoinThe serum concentration of Pitavastatin can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PimozideThe serum concentration of Pitavastatin can be increased when it is combined with Pimozide.Approved
PioglitazoneThe metabolism of Pitavastatin can be decreased when combined with Pioglitazone.Approved, Investigational
Platelet Activating FactorThe serum concentration of Pitavastatin can be decreased when it is combined with Platelet Activating Factor.Experimental
PonatinibThe serum concentration of Pitavastatin can be increased when it is combined with Ponatinib.Approved
PosaconazoleThe serum concentration of Pitavastatin can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Pitavastatin can be increased when it is combined with Pravastatin.Approved
PrazosinThe serum concentration of Pitavastatin can be increased when it is combined with Prazosin.Approved
PrednisoneThe serum concentration of Pitavastatin can be increased when it is combined with Prednisone.Approved, Vet Approved
PrimidoneThe metabolism of Pitavastatin can be increased when combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Pitavastatin can be increased when it is combined with Probenecid.Approved
ProgesteroneThe serum concentration of Pitavastatin can be decreased when it is combined with Progesterone.Approved, Vet Approved
PromethazineThe serum concentration of Pitavastatin can be increased when it is combined with Promethazine.Approved
PropafenoneThe serum concentration of Pitavastatin can be increased when it is combined with Propafenone.Approved
PropranololThe serum concentration of Pitavastatin can be increased when it is combined with Propranolol.Approved, Investigational
ProtriptylineThe serum concentration of Pitavastatin can be increased when it is combined with Protriptyline.Approved
PyrimethamineThe metabolism of Pitavastatin can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuercetinThe serum concentration of Pitavastatin can be increased when it is combined with Quercetin.Experimental
QuinacrineThe serum concentration of Pitavastatin can be increased when it is combined with Quinacrine.Approved
QuinidineThe serum concentration of Pitavastatin can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of Pitavastatin can be increased when it is combined with Quinine.Approved
RabeprazoleThe metabolism of Pitavastatin can be decreased when combined with Rabeprazole.Approved, Investigational
RaltegravirRaltegravir may increase the myopathic rhabdomyolysis activities of Pitavastatin.Approved
RanitidineThe serum concentration of Pitavastatin can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Pitavastatin can be increased when it is combined with Ranolazine.Approved, Investigational
ReboxetineThe serum concentration of Pitavastatin can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Pitavastatin can be increased when it is combined with Regorafenib.Approved
ReserpineThe serum concentration of Pitavastatin can be decreased when it is combined with Reserpine.Approved
RifabutinThe serum concentration of Pitavastatin can be increased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Pitavastatin can be increased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Pitavastatin can be increased when it is combined with Rifapentine.Approved
RilpivirineThe serum concentration of Pitavastatin can be increased when it is combined with Rilpivirine.Approved
RitonavirThe serum concentration of Pitavastatin can be increased when it is combined with Ritonavir.Approved, Investigational
RolapitantThe serum concentration of Pitavastatin can be increased when it is combined with Rolapitant.Approved
RosiglitazoneThe metabolism of Pitavastatin can be decreased when combined with Rosiglitazone.Approved, Investigational
SaquinavirThe serum concentration of Pitavastatin can be decreased when it is combined with Saquinavir.Approved, Investigational
ScopolamineThe serum concentration of Pitavastatin can be increased when it is combined with Scopolamine.Approved
SecobarbitalThe metabolism of Pitavastatin can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineThe serum concentration of Pitavastatin can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
SertralineThe serum concentration of Pitavastatin can be increased when it is combined with Sertraline.Approved
SildenafilThe metabolism of Pitavastatin can be decreased when combined with Sildenafil.Approved, Investigational
SimeprevirThe serum concentration of Pitavastatin can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Pitavastatin can be increased when it is combined with Simvastatin.Approved
SirolimusThe serum concentration of Pitavastatin can be decreased when it is combined with Sirolimus.Approved, Investigational
SorafenibThe serum concentration of Pitavastatin can be increased when it is combined with Sorafenib.Approved, Investigational
SpironolactoneThe serum concentration of Pitavastatin can be increased when it is combined with Spironolactone.Approved
St. John's WortThe metabolism of Pitavastatin can be increased when combined with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Pitavastatin can be increased when it is combined with Staurosporine.Experimental
StiripentolThe metabolism of Pitavastatin can be decreased when combined with Stiripentol.Approved
StreptozocinThe serum concentration of Pitavastatin can be decreased when it is combined with Streptozocin.Approved
SulfadiazineThe metabolism of Pitavastatin can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Pitavastatin can be decreased when combined with Sulfamethoxazole.Approved
SulfinpyrazoneThe serum concentration of Pitavastatin can be increased when it is combined with Sulfinpyrazone.Approved
SulfisoxazoleThe metabolism of Pitavastatin can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SumatriptanThe serum concentration of Pitavastatin can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe serum concentration of Pitavastatin can be increased when it is combined with Sunitinib.Approved, Investigational
TacrineThe serum concentration of Pitavastatin can be increased when it is combined with Tacrine.Withdrawn
TacrolimusThe serum concentration of Pitavastatin can be decreased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Pitavastatin can be decreased when it is combined with Tamoxifen.Approved
Taurocholic AcidThe serum concentration of Pitavastatin can be increased when it is combined with Taurocholic Acid.Experimental
TelaprevirThe serum concentration of Pitavastatin can be increased when it is combined with Telaprevir.Approved
TelithromycinThe serum concentration of Pitavastatin can be increased when it is combined with Telithromycin.Approved
TelmisartanThe serum concentration of Pitavastatin can be increased when it is combined with Telmisartan.Approved, Investigational
TemsirolimusThe serum concentration of Pitavastatin can be increased when it is combined with Temsirolimus.Approved
TerazosinThe serum concentration of Pitavastatin can be increased when it is combined with Terazosin.Approved
TerfenadineThe serum concentration of Pitavastatin can be increased when it is combined with Terfenadine.Withdrawn
TeriflunomideThe serum concentration of Pitavastatin can be increased when it is combined with Teriflunomide.Approved
TesmilifeneThe serum concentration of Pitavastatin can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Pitavastatin can be increased when it is combined with Testosterone.Approved, Investigational
TicagrelorThe serum concentration of Pitavastatin can be increased when it is combined with Ticagrelor.Approved
TiclopidineThe metabolism of Pitavastatin can be decreased when combined with Ticlopidine.Approved
TolbutamideThe metabolism of Pitavastatin can be decreased when combined with Tolbutamide.Approved
TolvaptanThe serum concentration of Pitavastatin can be increased when it is combined with Tolvaptan.Approved
TrabectedinPitavastatin may increase the myopathic rhabdomyolysis activities of Trabectedin.Approved, Investigational
TrazodoneThe serum concentration of Pitavastatin can be decreased when it is combined with Trazodone.Approved, Investigational
TrifluoperazineThe serum concentration of Pitavastatin can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Pitavastatin can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimThe serum concentration of Pitavastatin can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Pitavastatin can be increased when it is combined with Trimipramine.Approved
TroleandomycinThe serum concentration of Pitavastatin can be increased when it is combined with Troleandomycin.Approved
Valproic AcidThe metabolism of Pitavastatin can be decreased when combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Pitavastatin can be decreased when combined with Valsartan.Approved, Investigational
VenlafaxineThe serum concentration of Pitavastatin can be increased when it is combined with Venlafaxine.Approved
VerapamilThe serum concentration of Pitavastatin can be decreased when it is combined with Verapamil.Approved
VinblastineThe serum concentration of Pitavastatin can be decreased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Pitavastatin can be decreased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Pitavastatin can be increased when it is combined with Vinorelbine.Approved, Investigational
VoriconazoleThe metabolism of Pitavastatin can be decreased when combined with Voriconazole.Approved, Investigational
WarfarinPitavastatin may increase the anticoagulant activities of Warfarin.Approved
ZafirlukastThe metabolism of Pitavastatin can be decreased when combined with Zafirlukast.Approved, Investigational
ZimelidineThe serum concentration of Pitavastatin can be increased when it is combined with Zimelidine.Withdrawn
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
ATC CodesC10AA08
AHFS Codes
  • 24:0608
PDB EntriesNot Available
FDA labelDownload (460 KB)
MSDSDownload (116 KB)
ADMET
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 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot 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
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5,753,675 No2009-08-032015-05-19Us
US5,854,259 No2009-08-032015-12-29Us
US5,856,336 No2009-08-032016-01-05Us
US5854259 No1995-12-292015-12-29Us
US5856336 No2000-12-252020-12-25Us
US6,465,477 No2009-08-032016-12-20Us
US6465477 No1996-12-202016-12-20Us
US7,022,713 No2009-08-032024-02-19Us
US7022713 No2004-02-192024-02-19Us
US8557993 No2004-02-022024-02-02Us
Properties
StateSolid
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 RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylquinolines. These are heterocyclic compounds containing a quinoline moiety substituted with a phenyl group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassQuinolines and derivatives
Sub ClassPhenylquinolines
Direct ParentPhenylquinolines
Alternative Parents
Substituents
  • Phenylquinoline
  • 4-phenylpyridine
  • Medium-chain hydroxy acid
  • Medium-chain fatty acid
  • Heterocyclic fatty acid
  • Halogenated fatty acid
  • Halobenzene
  • Fluorobenzene
  • Beta-hydroxy acid
  • Fatty acyl
  • Fatty acid
  • Benzenoid
  • Unsaturated fatty acid
  • Pyridine
  • Hydroxy acid
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Heteroaromatic compound
  • Secondary alcohol
  • Azacycle
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Carbonyl group
  • Alcohol
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Nadph binding
Specific Function:
Transmembrane glycoprotein that is the rate-limiting enzyme in cholesterol biosynthesis as well as in the biosynthesis of nonsterol isoprenoids that are essential for normal cell function including ubiquinone and geranylgeranyl proteins.
Gene Name:
HMGCR
Uniprot ID:
P04035
Molecular Weight:
97475.155 Da
References
  1. 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 suggests it may play an important role in regulating the level and activity of these potent and active estrogen metabolites. Is also active with androsterone, hyodeoxycholic acid and tetrachlorocatechol...
Gene Name:
UGT2B7
Uniprot ID:
P16662
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 regulator of isoform 1.
Gene Name:
UGT1A3
Uniprot ID:
P35503
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. 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 unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
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 colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
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 the body. Appears to function in modulating the activity of the immune system during the acute-phase reaction.
Gene Name:
ORM1
Uniprot ID:
P02763
Molecular Weight:
23511.38 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
Molecular Weight:
76447.99 Da
References
  1. 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 uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP). Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B3
Uniprot ID:
Q9NPD5
Molecular Weight:
77402.175 Da
References
  1. 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
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 presence of sodium.(Microbial infection) Acts as a receptor for hepatitis B virus.
Gene Name:
SLC10A1
Uniprot ID:
Q14973
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 from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
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
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
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 ]
Comments
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Drug created on March 03, 2013 16:50 / Updated on December 09, 2016 02:39