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 mg/1OralEli Lilly & Co. Ltd.2010-05-152016-10-13Us00002 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.2010-05-152016-10-13Us00002 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.2010-05-152016-10-13Us00002 4771 90 nlmimage10 8f16c7a6
LivaloTablet, film coated1.045 mg/1OralKowa Company, Ltd.2010-05-15Not applicableUs66869 0104 90 nlmimage10 323c1910
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
PitavastatinTablet, film coated1.045 mg/1OralOrient Pharma Co., Ltd.2016-01-292017-07-24Us
PitavastatinTablet, film coated4 mg/1OralStason Pharmaceuticals, Inc.2017-12-252018-01-23Us
PitavastatinTablet, film coated4.18 mg/1OralOrient Pharma Co., Ltd.2016-01-292017-07-24Us
PitavastatinTablet, film coated2 mg/1OralStason Pharmaceuticals, Inc.2017-12-252018-01-23Us
PitavastatinTablet, film coated2.09 mg/1OralOrient Pharma Co., Ltd.2016-01-292017-07-24Us
PitavastatinTablet, film coated1 mg/1OralStason Pharmaceuticals, Inc.2017-12-252018-01-23Us
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[[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

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.

Structured Indications
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
DrugInteractionDrug group
6-Deoxyerythronolide BThe risk or severity of rhabdomyolysis can be increased when 6-Deoxyerythronolide B is combined with Pitavastatin.Experimental
AbirateroneThe serum concentration of Pitavastatin can be increased when it is combined with Abiraterone.Approved
AcetaminophenThe serum concentration of Pitavastatin can be increased when it is combined with Acetaminophen.Approved
AcetazolamideThe serum concentration of Pitavastatin can be increased when it is combined with Acetazolamide.Approved, Vet Approved
AcipimoxAcipimox may increase the myopathic rhabdomyolysis activities of Pitavastatin.Approved, Investigational
AldesleukinThe serum concentration of Pitavastatin can be increased when it is combined with Aldesleukin.Approved
AlmasilateThe serum concentration of Pitavastatin can be decreased when it is combined with Almasilate.Approved, Experimental
AloglutamolThe serum concentration of Pitavastatin can be decreased when it is combined with Aloglutamol.Experimental
AlprazolamThe serum concentration of Pitavastatin can be increased when it is combined with Alprazolam.Approved, Illicit, Investigational
AluminiumThe serum concentration of Pitavastatin can be decreased when it is combined with Aluminium.Approved, Investigational
Aluminium acetoacetateThe serum concentration of Pitavastatin can be decreased when it is combined with Aluminium acetoacetate.Experimental
Aluminium glycinateThe serum concentration of Pitavastatin can be decreased when it is combined with Aluminium glycinate.Experimental
Aluminum hydroxideThe serum concentration of Pitavastatin can be decreased when it is combined with Aluminum hydroxide.Approved, Investigational
AmbroxolThe serum concentration of Pitavastatin can be increased when it is combined with Ambroxol.Approved, Investigational
AmiodaroneThe serum concentration of Pitavastatin can be decreased when it is combined with Amiodarone.Approved, Investigational
AmlodipineThe serum concentration of Pitavastatin can be increased when it is combined with Amlodipine.Approved
Amphotericin BThe risk or severity of rhabdomyolysis can be increased when Amphotericin B is combined with Pitavastatin.Approved, Investigational
AmprenavirThe serum concentration of Pitavastatin can be increased when it is combined with Amprenavir.Approved, Investigational
AnastrozoleThe serum concentration of Pitavastatin can be increased when it is combined with Anastrozole.Approved, Investigational
AntipyrineThe serum concentration of Pitavastatin can be increased when it is combined with Antipyrine.Approved, Investigational
AprepitantThe metabolism of Pitavastatin can be increased when combined with Aprepitant.Approved, Investigational
Arsenic trioxideThe serum concentration of Pitavastatin can be increased when it is combined with Arsenic trioxide.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
AtomoxetineThe serum concentration of Pitavastatin can be increased when it is combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Pitavastatin can be increased when it is combined with Atorvastatin.Approved
AVE9633The risk or severity of rhabdomyolysis can be increased when AVE9633 is combined with Pitavastatin.Investigational
AzelastineThe serum concentration of Pitavastatin can be increased when it is combined with Azelastine.Approved
AzithromycinThe risk or severity of rhabdomyolysis can be increased when Azithromycin is combined with Pitavastatin.Approved
BetamethasoneThe serum concentration of Pitavastatin can be increased when it is combined with Betamethasone.Approved, Vet Approved
BezafibrateBezafibrate may increase the myopathic rhabdomyolysis activities of Pitavastatin.Approved, Investigational
BicalutamideThe serum concentration of Pitavastatin can be increased when it is combined with Bicalutamide.Approved
BifonazoleThe serum concentration of Pitavastatin can be increased when it is combined with Bifonazole.Approved, Investigational
Bismuth SubcitrateThe serum concentration of Pitavastatin can be decreased when it is combined with Bismuth Subcitrate.Approved, Investigational
Bismuth subnitrateThe serum concentration of Pitavastatin can be decreased when it is combined with Bismuth subnitrate.Approved, Experimental
BoceprevirThe serum concentration of Pitavastatin can be increased when it is combined with Boceprevir.Approved, Withdrawn
BortezomibThe serum concentration of Pitavastatin can be increased when it is combined with Bortezomib.Approved, Investigational
BosentanThe metabolism of Pitavastatin can be increased when combined with Bosentan.Approved, Investigational
Brefeldin AThe risk or severity of rhabdomyolysis can be increased when Brefeldin A is combined with Pitavastatin.Experimental
Brentuximab vedotinThe serum concentration of Pitavastatin can be increased when it is combined with Brentuximab vedotin.Approved
BromocriptineThe serum concentration of Pitavastatin can be increased when it is combined with Bromocriptine.Approved, Investigational
Bryostatin 1The risk or severity of rhabdomyolysis can be increased when Bryostatin 1 is combined with Pitavastatin.Investigational
BuprenorphineThe serum concentration of Pitavastatin can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
CabergolineThe serum concentration of Pitavastatin can be increased when it is combined with Cabergoline.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, Investigational
Calcium silicateThe serum concentration of Pitavastatin can be decreased when it is combined with Calcium silicate.Experimental
CandicidinThe risk or severity of rhabdomyolysis can be increased when Candicidin is combined with Pitavastatin.Withdrawn
CapecitabineThe metabolism of Pitavastatin can be decreased when combined with Capecitabine.Approved, Investigational
CapsaicinThe serum concentration of Pitavastatin can be increased when it is combined with Capsaicin.Approved
CarbamazepineThe metabolism of Pitavastatin can be increased when combined with Carbamazepine.Approved, Investigational
CarbomycinThe risk or severity of rhabdomyolysis can be increased when Carbomycin is combined with Pitavastatin.Vet Approved
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
CerivastatinThe serum concentration of Pitavastatin can be increased when it is combined with Cerivastatin.Approved, Withdrawn
CethromycinThe risk or severity of rhabdomyolysis can be increased when Cethromycin is combined with Pitavastatin.Investigational
ChloramphenicolThe serum concentration of Pitavastatin can be increased when it is combined with Chloramphenicol.Approved, Vet Approved
ChlorzoxazoneThe serum concentration of Pitavastatin can be increased when it is combined with Chlorzoxazone.Approved
CholecalciferolThe metabolism of Pitavastatin can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CholestyramineCholestyramine can cause a decrease in the absorption of Pitavastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Investigational
CilostazolThe serum concentration of Pitavastatin can be increased when it is combined with Cilostazol.Approved, Investigational
CimetidineThe serum concentration of Pitavastatin can be increased when it is combined with Cimetidine.Approved, Investigational
CiprofibrateThe risk or severity of myopathy, rhabdomyolysis, and myoglobinuria can be increased when Ciprofibrate is combined with Pitavastatin.Approved, Investigational
CiprofloxacinThe serum concentration of Pitavastatin can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CisaprideThe serum concentration of Pitavastatin can be increased when it is combined with Cisapride.Approved, Investigational, Withdrawn
ClarithromycinThe serum concentration of Pitavastatin can be increased when it is combined with Clarithromycin.Approved
ClemastineThe serum concentration of Pitavastatin can be increased when it is combined with Clemastine.Approved, Investigational
ClindamycinThe serum concentration of Pitavastatin can be increased when it is combined with Clindamycin.Approved, Vet Approved
ClofazimineThe serum concentration of Pitavastatin can be increased when it is combined with Clofazimine.Approved, Investigational
ClomifeneThe serum concentration of Pitavastatin can be increased when it is combined with Clomifene.Approved, Investigational
ClotiazepamThe serum concentration of Pitavastatin can be increased when it is combined with Clotiazepam.Approved, Illicit
ClotrimazoleThe metabolism of Pitavastatin can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe serum concentration of Pitavastatin can be increased when it is combined with Clozapine.Approved
CobicistatThe serum concentration of Pitavastatin can be increased when it is combined with Cobicistat.Approved
CocaineThe serum concentration of Pitavastatin can be increased when it is combined with Cocaine.Approved, Illicit
ColchicineColchicine may increase the myopathic rhabdomyolysis activities of Pitavastatin.Approved
ColesevelamColesevelam can cause a decrease in the absorption of Pitavastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
ColestipolColestipol can cause a decrease in the absorption of Pitavastatin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Coltuximab ravtansineThe risk or severity of rhabdomyolysis can be increased when Coltuximab ravtansine is combined with Pitavastatin.Investigational
ConivaptanThe serum concentration of Pitavastatin can be increased when it is combined with Conivaptan.Approved, Investigational
Cortisone acetateThe serum concentration of Pitavastatin can be increased when it is combined with Cortisone acetate.Approved, Investigational
CrisaboroleThe metabolism of Pitavastatin can be decreased when combined with Crisaborole.Approved, Investigational
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
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, Investigational
DaclatasvirThe serum concentration of Pitavastatin can be increased when it is combined with Daclatasvir.Approved, Investigational
DalfopristinThe serum concentration of Pitavastatin can be increased when it is combined with Dalfopristin.Approved
DanazolThe risk or severity of myopathy and rhabdomyolysis can be increased when Danazol is combined with Pitavastatin.Approved
DaptomycinThe risk or severity of adverse effects can be increased when Pitavastatin is combined with Daptomycin.Approved, Investigational
DarunavirThe serum concentration of Pitavastatin can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Pitavastatin can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Pitavastatin can be increased 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, Investigational
DexamethasoneThe serum concentration of Pitavastatin can be increased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextropropoxypheneThe serum concentration of Pitavastatin can be increased when it is combined with Dextropropoxyphene.Approved, Illicit, Investigational, Withdrawn
DiazepamThe serum concentration of Pitavastatin can be increased when it is combined with Diazepam.Approved, Illicit, Investigational, Vet Approved
DiethylstilbestrolThe serum concentration of Pitavastatin can be increased when it is combined with Diethylstilbestrol.Approved, Investigational
DihydroergotamineThe serum concentration of Pitavastatin can be increased when it is combined with Dihydroergotamine.Approved, Investigational
DiltiazemThe serum concentration of Pitavastatin can be increased when it is combined with Diltiazem.Approved, Investigational
Dimethyl sulfoxideThe serum concentration of Pitavastatin can be increased when it is combined with Dimethyl sulfoxide.Approved, Vet Approved
DirithromycinThe risk or severity of rhabdomyolysis can be increased when Dirithromycin is combined with Pitavastatin.Approved, Investigational
DocetaxelThe serum concentration of Pitavastatin can be increased when it is combined with Docetaxel.Approved, Investigational
DoramectinThe risk or severity of rhabdomyolysis can be increased when Doramectin is combined with Pitavastatin.Vet Approved
DosulepinThe metabolism of Pitavastatin can be decreased when combined with Dosulepin.Approved
DoxorubicinThe serum concentration of Pitavastatin can be increased when it is combined with Doxorubicin.Approved, Investigational
DoxycyclineThe serum concentration of Pitavastatin can be increased when it is combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe serum concentration of Pitavastatin can be increased when it is combined with Dronedarone.Approved
EconazoleThe serum concentration of Pitavastatin can be increased when it is combined with Econazole.Approved
EfavirenzThe serum concentration of Pitavastatin can be decreased when it is 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
EnasidenibThe serum concentration of Pitavastatin can be increased when it is combined with Enasidenib.Approved, Investigational
EpinephrineThe serum concentration of Pitavastatin can be increased when it is combined with Epinephrine.Approved, Vet Approved
EpofolateThe risk or severity of rhabdomyolysis can be increased when Epofolate is combined with Pitavastatin.Investigational
Epothilone DThe risk or severity of rhabdomyolysis can be increased when Epothilone D is combined with Pitavastatin.Experimental, Investigational
EprinomectinThe risk or severity of rhabdomyolysis can be increased when Eprinomectin is combined with Pitavastatin.Vet Approved
Ergoloid mesylateThe serum concentration of Pitavastatin can be increased when it is combined with Ergoloid mesylate.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
ErlotinibThe risk or severity of adverse effects can be increased when Erlotinib is combined with Pitavastatin.Approved, Investigational
ErythromycinThe serum concentration of Pitavastatin can be increased when it is combined with Erythromycin.Approved, Investigational, Vet Approved
EthanolThe serum concentration of Pitavastatin can be increased when it is combined with Ethanol.Approved
EtoposideThe serum concentration of Pitavastatin can be increased when it is combined with Etoposide.Approved
EtoricoxibThe serum concentration of Pitavastatin can be increased when it is combined with Etoricoxib.Approved, Investigational
EtravirineThe serum concentration of Pitavastatin can be decreased when it is combined with Etravirine.Approved
EverolimusThe risk or severity of rhabdomyolysis can be increased when Everolimus is combined with Pitavastatin.Approved
EzetimibeThe serum concentration of Pitavastatin can be increased when it is combined with Ezetimibe.Approved
FelodipineThe metabolism of Pitavastatin can be decreased when combined with Felodipine.Approved, Investigational
FenofibrateThe risk or severity of myopathy and rhabdomyolysis 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
FloxuridineThe metabolism of Pitavastatin can be decreased when combined with Floxuridine.Approved
FluconazoleThe risk or severity of adverse effects can be increased when Fluconazole is combined with Pitavastatin.Approved, 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
FlurithromycinThe risk or severity of rhabdomyolysis can be increased when Flurithromycin is combined with Pitavastatin.Experimental
Fluticasone propionateThe serum concentration of Pitavastatin can be increased when it is combined with Fluticasone propionate.Approved
FluvastatinThe metabolism of Pitavastatin can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Pitavastatin can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe serum concentration of Pitavastatin can be increased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Pitavastatin can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Pitavastatin can be decreased when it is combined with Fosphenytoin.Approved, Investigational
Fusidic AcidThe risk or severity of adverse effects can be increased when Fusidic Acid is combined with Pitavastatin.Approved, Investigational
GemfibrozilThe risk or severity of rhabdomyolysis, myoglobinuria, and elevated creatine kinase (CPK) can be increased when Gemfibrozil is combined with Pitavastatin.Approved
GlyburideThe serum concentration of Pitavastatin can be increased when it is combined with Glyburide.Approved
Glycerol PhenylbutyrateThe serum concentration of Pitavastatin can be increased when it is combined with Glycerol Phenylbutyrate.Approved
GPI-1485The risk or severity of rhabdomyolysis can be increased when GPI-1485 is combined with Pitavastatin.Investigational
HaloperidolThe serum concentration of Pitavastatin can be increased when it is combined with Haloperidol.Approved
HistamineThe serum concentration of Pitavastatin can be increased when it is combined with Histamine.Approved, Investigational
HydralazineThe serum concentration of Pitavastatin can be increased when it is combined with Hydralazine.Approved
HydrocortisoneThe serum concentration of Pitavastatin can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
HydrotalciteThe serum concentration of Pitavastatin can be decreased when it is combined with Hydrotalcite.Approved, Experimental, Investigational
IdelalisibThe serum concentration of Pitavastatin can be increased when it is combined with Idelalisib.Approved
IfosfamideThe serum concentration of Pitavastatin can be increased when it is combined with Ifosfamide.Approved
IloperidoneThe serum concentration of Pitavastatin can be increased when it is combined with Iloperidone.Approved
ImatinibThe serum concentration of Pitavastatin can be increased when it is combined with Imatinib.Approved
IndinavirThe metabolism of Pitavastatin can be decreased when combined with Indinavir.Approved
IndisulamThe serum concentration of Pitavastatin can be increased when it is combined with Indisulam.Investigational
IrbesartanThe metabolism of Pitavastatin can be decreased when combined with Irbesartan.Approved, Investigational
IrinotecanThe serum concentration of Pitavastatin can be increased when it is combined with Irinotecan.Approved, Investigational
IsavuconazoniumThe serum concentration of Pitavastatin can be increased when it is combined with Isavuconazonium.Approved, Investigational
IsoniazidThe serum concentration of Pitavastatin can be increased when it is combined with Isoniazid.Approved, Investigational
IsradipineThe serum concentration of Pitavastatin can be increased when it is combined with Isradipine.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 risk or severity of rhabdomyolysis can be increased when Ivermectin is combined with Pitavastatin.Approved, Investigational, Vet Approved
IxabepiloneThe risk or severity of rhabdomyolysis can be increased when Ixabepilone is combined with Pitavastatin.Approved, Investigational
JosamycinThe risk or severity of rhabdomyolysis can be increased when Josamycin is combined with Pitavastatin.Approved, Investigational
KetazolamThe serum concentration of Pitavastatin can be increased when it is combined with Ketazolam.Approved
KetoconazoleThe serum concentration of Pitavastatin can be increased when it is combined with Ketoconazole.Approved, Investigational
KitasamycinThe risk or severity of rhabdomyolysis can be increased when Kitasamycin is combined with Pitavastatin.Experimental
KOS-1584The risk or severity of rhabdomyolysis can be increased when KOS-1584 is combined with Pitavastatin.Investigational
LansoprazoleThe serum concentration of Pitavastatin can be increased when it is combined with Lansoprazole.Approved, Investigational
Lanthanum carbonateThe serum concentration of Pitavastatin can be decreased when it is combined with Lanthanum carbonate.Approved
LapatinibThe metabolism of Pitavastatin can be decreased when combined with Lapatinib.Approved, Investigational
LeflunomideThe metabolism of Pitavastatin can be decreased when combined with Leflunomide.Approved, Investigational
LercanidipineThe serum concentration of Pitavastatin can be increased when it is combined with Lercanidipine.Approved, Investigational
LevofloxacinThe serum concentration of Pitavastatin can be increased when it is combined with Levofloxacin.Approved, Investigational
LevosalbutamolThe serum concentration of Pitavastatin can be increased when it is combined with Levosalbutamol.Approved, Investigational
LidocaineThe serum concentration of Pitavastatin can be increased when it is combined with Lidocaine.Approved, Vet Approved
LinagliptinThe serum concentration of Pitavastatin can be increased when it is combined with Linagliptin.Approved
LobeglitazoneThe metabolism of Pitavastatin can be decreased when combined with Lobeglitazone.Approved, Investigational
LomitapideThe serum concentration of Pitavastatin can be increased when it is combined with Lomitapide.Approved, Investigational
LomustineThe serum concentration of Pitavastatin can be increased when it is combined with Lomustine.Approved, Investigational
LopinavirThe serum concentration of Pitavastatin can be increased when it is combined with Lopinavir.Approved
LoratadineThe serum concentration of Pitavastatin can be increased when it is combined with Loratadine.Approved, Investigational
Lorvotuzumab mertansineThe risk or severity of rhabdomyolysis can be increased when Lorvotuzumab mertansine is combined with Pitavastatin.Investigational
LosartanThe metabolism of Pitavastatin can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Pitavastatin can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Pitavastatin can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Pitavastatin can be increased when it is combined with Lumacaftor.Approved
LurasidoneThe serum concentration of Pitavastatin can be increased when it is combined with Lurasidone.Approved, Investigational
MagaldrateThe serum concentration of Pitavastatin can be decreased when it is combined with Magaldrate.Approved, Withdrawn
Magnesium HydroxideThe serum concentration of Pitavastatin can be decreased when it is combined with Magnesium Hydroxide.Approved, Investigational
Magnesium oxideThe serum concentration of Pitavastatin can be decreased when it is combined with Magnesium oxide.Approved
Magnesium peroxideThe serum concentration of Pitavastatin can be decreased when it is combined with Magnesium peroxide.Experimental
Magnesium silicateThe serum concentration of Pitavastatin can be decreased when it is combined with Magnesium silicate.Approved, Experimental
Magnesium TrisilicateThe serum concentration of Pitavastatin can be decreased when it is combined with Magnesium Trisilicate.Approved
ManidipineThe metabolism of Pitavastatin can be decreased when combined with Manidipine.Approved, Investigational
MefloquineThe serum concentration of Pitavastatin can be increased when it is combined with Mefloquine.Approved, Investigational
MepartricinThe risk or severity of rhabdomyolysis can be increased when Mepartricin is combined with Pitavastatin.Experimental
MequitazineThe serum concentration of Pitavastatin can be increased when it is combined with Mequitazine.Approved
MethadoneThe serum concentration of Pitavastatin can be increased when it is combined with Methadone.Approved
MethazolamideThe serum concentration of Pitavastatin can be increased when it is combined with Methazolamide.Approved
MethimazoleThe serum concentration of Pitavastatin can be increased when it is combined with Methimazole.Approved
MethylergometrineThe serum concentration of Pitavastatin can be increased when it is combined with Methylergometrine.Approved
MethylprednisoloneThe serum concentration of Pitavastatin can be increased when it is combined with Methylprednisolone.Approved, Vet Approved
MetronidazoleThe serum concentration of Pitavastatin can be increased when it is combined with Metronidazole.Approved
MetyraponeThe serum concentration of Pitavastatin can be increased when it is combined with Metyrapone.Approved, Investigational
MibefradilThe serum concentration of Pitavastatin can be increased when it is combined with Mibefradil.Investigational, 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 increased when it is combined with Midazolam.Approved, Illicit
MidecamycinThe risk or severity of rhabdomyolysis can be increased when Midecamycin is combined with Pitavastatin.Experimental
MidostaurinThe metabolism of Pitavastatin can be decreased when combined with Midostaurin.Approved, Investigational
MifepristoneThe serum concentration of Pitavastatin can be increased when it is combined with Mifepristone.Approved, Investigational
MiocamycinThe risk or severity of rhabdomyolysis can be increased when Miocamycin is combined with Pitavastatin.Experimental
MirtazapineThe serum concentration of Pitavastatin can be increased when it is combined with Mirtazapine.Approved
Mirvetuximab SoravtansineThe risk or severity of rhabdomyolysis can be increased when Mirvetuximab Soravtansine is combined with Pitavastatin.Investigational
MitemcinalThe risk or severity of rhabdomyolysis can be increased when Mitemcinal is combined with Pitavastatin.Investigational
MitoxantroneThe serum concentration of Pitavastatin can be increased when it is combined with Mitoxantrone.Approved, Investigational
ModafinilThe serum concentration of Pitavastatin can be increased when it is combined with Modafinil.Approved, Investigational
NatamycinThe risk or severity of rhabdomyolysis can be increased when Natamycin is combined with Pitavastatin.Approved
NefazodoneThe serum concentration of Pitavastatin can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Pitavastatin can be increased when it is combined with Nelfinavir.Approved
NetupitantThe serum concentration of Pitavastatin can be increased when it is combined with Netupitant.Approved, Investigational
NevirapineThe serum concentration of Pitavastatin can be increased when it is combined with Nevirapine.Approved
NiacinThe risk or severity of rhabdomyolysis can be increased when Niacin is combined with Pitavastatin.Approved, Investigational, Nutraceutical
NicardipineThe metabolism of Pitavastatin can be decreased when combined with Nicardipine.Approved, Investigational
NicotinamideThe serum concentration of Pitavastatin can be increased when it is combined with Nicotinamide.Approved, Investigational
NifedipineThe serum concentration of Pitavastatin can be increased when it is combined with Nifedipine.Approved
NilotinibThe metabolism of Pitavastatin can be decreased when combined with Nilotinib.Approved, Investigational
NilvadipineThe serum concentration of Pitavastatin can be increased when it is combined with Nilvadipine.Approved, Investigational
NisoldipineThe serum concentration of Pitavastatin can be increased when it is combined with Nisoldipine.Approved
NitrendipineThe serum concentration of Pitavastatin can be increased when it is combined with Nitrendipine.Approved, Investigational
Nitric OxideThe serum concentration of Pitavastatin can be increased when it is combined with Nitric Oxide.Approved
NorfloxacinThe serum concentration of Pitavastatin can be increased when it is combined with Norfloxacin.Approved
NoscapineThe serum concentration of Pitavastatin can be increased when it is combined with Noscapine.Investigational
NystatinThe risk or severity of rhabdomyolysis can be increased when Nystatin is combined with Pitavastatin.Approved, Vet Approved
OlanzapineThe serum concentration of Pitavastatin can be increased when it is combined with Olanzapine.Approved, Investigational
OlaparibThe serum concentration of Pitavastatin can be increased when it is combined with Olaparib.Approved
OleandomycinThe risk or severity of rhabdomyolysis can be increased when Oleandomycin is combined with Pitavastatin.Vet Approved
OmeprazoleThe metabolism of Pitavastatin can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OxybutyninThe serum concentration of Pitavastatin can be increased when it is combined with Oxybutynin.Approved, Investigational
OxymetholoneThe serum concentration of Pitavastatin can be increased when it is combined with Oxymetholone.Approved, Illicit
PaclitaxelThe serum concentration of Pitavastatin can be increased when it is combined with Paclitaxel.Approved, Vet Approved
PalbociclibThe serum concentration of Pitavastatin can be increased when it is combined with Palbociclib.Approved, Investigational
ParamethasoneThe serum concentration of Pitavastatin can be increased when it is combined with Paramethasone.Approved
PatupiloneThe risk or severity of rhabdomyolysis can be increased when Patupilone is combined with Pitavastatin.Experimental, Investigational
PazopanibPitavastatin may increase the hepatotoxic activities of Pazopanib.Approved
PergolideThe serum concentration of Pitavastatin can be increased when it is combined with Pergolide.Approved, Investigational, Vet Approved, Withdrawn
PhenelzineThe serum concentration of Pitavastatin can be increased when it is combined with Phenelzine.Approved
PhenobarbitalThe metabolism of Pitavastatin can be increased when combined with Phenobarbital.Approved, Investigational
PhenytoinThe serum concentration of Pitavastatin can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PilocarpineThe serum concentration of Pitavastatin can be increased when it is combined with Pilocarpine.Approved, Investigational
PimecrolimusThe risk or severity of rhabdomyolysis can be increased when Pimecrolimus is combined with Pitavastatin.Approved, Investigational
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
PiperaquineThe serum concentration of Pitavastatin can be increased when it is combined with Piperaquine.Approved, Investigational
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
PrednisoloneThe serum concentration of Pitavastatin can be increased when it is combined with Prednisolone.Approved, Vet Approved
PrednisoneThe serum concentration of Pitavastatin can be increased when it is combined with Prednisone.Approved, Vet Approved
PrimaquineThe serum concentration of Pitavastatin can be increased when it is combined with Primaquine.Approved
PrimidoneThe metabolism of Pitavastatin can be increased when combined with Primidone.Approved, Vet Approved
ProgesteroneThe serum concentration of Pitavastatin can be increased when it is combined with Progesterone.Approved, Vet Approved
PropofolThe serum concentration of Pitavastatin can be increased when it is combined with Propofol.Approved, Investigational, Vet Approved
PyrimethamineThe metabolism of Pitavastatin can be decreased when combined with Pyrimethamine.Approved, Investigational, Vet Approved
QuinidineThe serum concentration of Pitavastatin can be increased when it is combined with Quinidine.Approved, Investigational
QuinineThe metabolism of Pitavastatin can be decreased when combined with Quinine.Approved
QuinupristinThe serum concentration of Pitavastatin can be increased when it is combined with Quinupristin.Approved
RabeprazoleThe metabolism of Pitavastatin can be decreased when combined with Rabeprazole.Approved, Investigational
RaloxifeneThe serum concentration of Pitavastatin can be increased when it is combined with Raloxifene.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
RegorafenibThe serum concentration of Pitavastatin can be increased when it is combined with Regorafenib.Approved
RepaglinideThe serum concentration of Pitavastatin can be increased when it is combined with Repaglinide.Approved, Investigational
ResveratrolThe serum concentration of Pitavastatin can be increased when it is combined with Resveratrol.Approved, Experimental, Investigational
RidaforolimusThe risk or severity of rhabdomyolysis can be increased when Ridaforolimus is combined with Pitavastatin.Investigational
RifabutinThe serum concentration of Pitavastatin can be increased when it is combined with Rifabutin.Approved, Investigational
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, Investigational
RifaximinThe serum concentration of Pitavastatin can be increased when it is combined with Rifaximin.Approved, Investigational
RilpivirineThe serum concentration of Pitavastatin can be increased when it is combined with Rilpivirine.Approved
RisperidoneThe serum concentration of Pitavastatin can be increased when it is combined with Risperidone.Approved, Investigational
RitonavirThe serum concentration of Pitavastatin can be increased when it is combined with Ritonavir.Approved, Investigational
RivastigmineThe serum concentration of Pitavastatin can be increased when it is combined with Rivastigmine.Approved, Investigational
RokitamycinThe risk or severity of rhabdomyolysis can be increased when Rokitamycin is combined with Pitavastatin.Experimental
RolapitantThe serum concentration of Pitavastatin can be increased when it is combined with Rolapitant.Approved, Investigational
RolitetracyclineThe serum concentration of Pitavastatin can be increased when it is combined with Rolitetracycline.Approved
RosiglitazoneThe metabolism of Pitavastatin can be decreased when combined with Rosiglitazone.Approved, Investigational
RosuvastatinThe serum concentration of Pitavastatin can be increased when it is combined with Rosuvastatin.Approved
RoxithromycinThe risk or severity of rhabdomyolysis can be increased when Roxithromycin is combined with Pitavastatin.Approved, Investigational, Withdrawn
RucaparibThe metabolism of Pitavastatin can be decreased when combined with Rucaparib.Approved, Investigational
RutinThe serum concentration of Pitavastatin can be increased when it is combined with Rutin.Experimental, Investigational
SagopiloneThe risk or severity of rhabdomyolysis can be increased when Sagopilone is combined with Pitavastatin.Investigational
SalbutamolThe serum concentration of Pitavastatin can be increased when it is combined with Salbutamol.Approved, Vet Approved
SaquinavirThe serum concentration of Pitavastatin can be increased when it is combined with Saquinavir.Approved, Investigational
SarilumabThe serum concentration of Pitavastatin can be increased when it is combined with Sarilumab.Approved, Investigational
SecobarbitalThe metabolism of Pitavastatin can be increased when combined with Secobarbital.Approved, Vet Approved
SelamectinThe risk or severity of rhabdomyolysis can be increased when Selamectin is combined with Pitavastatin.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 risk or severity of rhabdomyolysis can be increased when Sirolimus is combined with Pitavastatin.Approved, Investigational
SitaxentanThe serum concentration of Pitavastatin can be increased when it is combined with Sitaxentan.Approved, Investigational, Withdrawn
Sodium bicarbonateThe serum concentration of Pitavastatin can be decreased when it is combined with Sodium bicarbonate.Approved
SorafenibThe metabolism of Pitavastatin can be decreased when combined with Sorafenib.Approved, Investigational
SpiramycinThe risk or severity of rhabdomyolysis can be increased when Spiramycin is combined with Pitavastatin.Approved
St. John's WortThe metabolism of Pitavastatin can be increased when combined with St. John's Wort.Approved, Investigational, Nutraceutical
StiripentolThe serum concentration of Pitavastatin can be increased when it is combined with Stiripentol.Approved
SulfadiazineThe metabolism of Pitavastatin can be decreased when combined with Sulfadiazine.Approved, Investigational, Vet Approved
SulfamethoxazoleThe metabolism of Pitavastatin can be decreased when combined with Sulfamethoxazole.Approved
SulfanilamideThe serum concentration of Pitavastatin can be increased when it is combined with Sulfanilamide.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
TacrolimusThe risk or severity of rhabdomyolysis can be increased when Tacrolimus is combined with Pitavastatin.Approved, Investigational
TadalafilThe serum concentration of Pitavastatin can be increased when it is combined with Tadalafil.Approved, Investigational
TamoxifenThe metabolism of Pitavastatin can be decreased when combined with Tamoxifen.Approved
TelaprevirThe serum concentration of Pitavastatin can be increased when it is combined with Telaprevir.Approved, Withdrawn
TelithromycinThe serum concentration of Pitavastatin can be increased when it is combined with Telithromycin.Approved
TemsirolimusThe risk or severity of rhabdomyolysis can be increased when Temsirolimus is combined with Pitavastatin.Approved
TeniposideThe serum concentration of Pitavastatin can be increased when it is combined with Teniposide.Approved
TerfenadineThe serum concentration of Pitavastatin can be increased when it is combined with Terfenadine.Approved, Withdrawn
TeriflunomideThe serum concentration of Pitavastatin can be increased when it is combined with Teriflunomide.Approved
TesmilifeneThe serum concentration of Pitavastatin can be increased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Pitavastatin can be increased when it is combined with Testosterone.Approved, Investigational
Testosterone cypionateThe serum concentration of Pitavastatin can be increased when it is combined with Testosterone cypionate.Approved
Testosterone enanthateThe serum concentration of Pitavastatin can be increased when it is combined with Testosterone enanthate.Approved
Testosterone undecanoateThe serum concentration of Pitavastatin can be increased when it is combined with Testosterone undecanoate.Approved, Investigational
TetracyclineThe serum concentration of Pitavastatin can be increased when it is combined with Tetracycline.Approved, Vet Approved
ThiopentalThe serum concentration of Pitavastatin can be increased when it is combined with Thiopental.Approved, Vet Approved
TicagrelorThe metabolism of Pitavastatin can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Pitavastatin can be decreased when combined with Ticlopidine.Approved
TildipirosinThe risk or severity of rhabdomyolysis can be increased when Tildipirosin is combined with Pitavastatin.Vet Approved
TilmicosinThe risk or severity of rhabdomyolysis can be increased when Tilmicosin is combined with Pitavastatin.Investigational, Vet Approved
TioconazoleThe serum concentration of Pitavastatin can be increased when it is combined with Tioconazole.Approved
TipranavirThe serum concentration of Pitavastatin can be increased when it is combined with Tipranavir.Approved, Investigational
TofisopamThe serum concentration of Pitavastatin can be increased when it is combined with Tofisopam.Approved
TolbutamideThe metabolism of Pitavastatin can be decreased when combined with Tolbutamide.Approved, Investigational
TopiroxostatThe metabolism of Pitavastatin can be decreased when combined with Topiroxostat.Approved, Investigational
TopotecanThe serum concentration of Pitavastatin can be increased when it is combined with Topotecan.Approved, Investigational
TrabectedinPitavastatin may increase the myopathic rhabdomyolysis activities of Trabectedin.Approved, Investigational
TramadolThe serum concentration of Pitavastatin can be increased when it is combined with Tramadol.Approved, Investigational
TranylcypromineThe serum concentration of Pitavastatin can be increased when it is combined with Tranylcypromine.Approved, Investigational
Trastuzumab emtansineThe risk or severity of rhabdomyolysis can be increased when Trastuzumab emtansine is combined with Pitavastatin.Approved, Investigational
TrimethoprimThe metabolism of Pitavastatin can be decreased when combined with Trimethoprim.Approved, Vet Approved
TroglitazoneThe serum concentration of Pitavastatin can be increased when it is combined with Troglitazone.Investigational, Withdrawn
TroleandomycinThe risk or severity of rhabdomyolysis can be increased when Troleandomycin is combined with Pitavastatin.Approved
TromethamineThe serum concentration of Pitavastatin can be decreased when it is combined with Tromethamine.Approved
TylosinThe risk or severity of rhabdomyolysis can be increased when Tylosin is combined with Pitavastatin.Vet Approved
TylvalosinThe risk or severity of rhabdomyolysis can be increased when Tylvalosin is combined with Pitavastatin.Vet 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
VemurafenibThe serum concentration of Pitavastatin can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe serum concentration of Pitavastatin can be increased when it is combined with Venlafaxine.Approved
VerapamilThe serum concentration of Pitavastatin can be increased when it is combined with Verapamil.Approved
VinblastineThe serum concentration of Pitavastatin can be increased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Pitavastatin can be increased 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 serum concentration of Pitavastatin can be increased when it is combined with Voriconazole.Approved, Investigational
ZafirlukastThe metabolism of Pitavastatin can be decreased when combined with Zafirlukast.Approved, Investigational
ZiprasidoneThe serum concentration of Pitavastatin can be increased when it is combined with Ziprasidone.Approved
ZucapsaicinThe serum concentration of Pitavastatin can be increased when it is combined with Zucapsaicin.Approved, Investigational
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
1Active Not RecruitingTreatmentInfluenza in Humans1
1CompletedNot AvailableHealthy Volunteers1
1CompletedNot AvailableHigh Blood Pressure (Hypertension) / Hyperlipidemias1
1CompletedOtherHigh Blood Pressure (Hypertension) / Hyperlipidemias1
1CompletedSupportive CareHealthy Volunteers1
1CompletedTreatmentHigh Blood Cholesterol Level1
1CompletedTreatmentMetabolic Syndromes1
1Not Yet RecruitingTreatmentImpaired Renal Function1
1Unknown StatusNot AvailableHuman Immunodeficiency Virus (HIV) / Hyperlipidemias1
3CompletedTreatmentCoronary Heart Disease (CHD) / Dyslipidemias / High Blood Cholesterol Level1
3CompletedTreatmentDyslipidemias / High Blood Cholesterol Level4
3CompletedTreatmentDyslipidemias / High Blood Pressure (Hypertension)1
3CompletedTreatmentDyslipidemias / Hypercholesterolemia, Familial1
3CompletedTreatmentDyslipidemias / Type 2 Diabetes Mellitus2
3CompletedTreatmentHigh Blood Cholesterol Level1
3CompletedTreatmentHypercholesterolemia or Combined Dyslipidemia1
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
4Active Not RecruitingTreatmentHbA1c Level Associated With Lipid Compositions1
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
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
4Not Yet RecruitingTreatmentBMI >30 kg/m2 / Dyslipidemias1
4RecruitingPreventionCardiovascular Disease (CVD) / Human Immunodeficiency Virus (HIV) Infections1
4Unknown StatusPreventionProphylaxis of Contrast-induced nephropathy1
4WithdrawnPreventionPercutaneous Coronary Intervention1
Not AvailableActive Not RecruitingTreatmentBMI >30 kg/m2 / Fatty Liver, Nonalcoholic1
Not AvailableCompletedTreatmentHealthy Volunteers1
Not AvailableRecruitingNot AvailableInfection, Human Immunodeficiency Virus I1
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
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]
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]

Drug created on March 03, 2013 16:50 / Updated on January 19, 2018 10:58