U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C25H24FNO4
Molecular Weight 421.4617
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of PITAVASTATIN

SMILES

c1ccc2c(c1)c(-c3ccc(cc3)F)c(/C(/[H])=C(\[H])/[C@]([H])(C[C@]([H])(CC(=O)O)O)O)c(C4CC4)n2

InChI

InChIKey=VGYFMXBACGZSIL-MCBHFWOFSA-N
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

HIDE SMILES / InChI

Molecular Formula C25H24FNO4
Molecular Weight 421.4617
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 1
Optical Activity UNSPECIFIED

Description
Curator's Comment:: https://www.ncbi.nlm.nih.gov/pubmed/20179258

Pitavastatin is a new synthetic 3-hydroxy-3-methyl glutaryl coenzyme A reductase (HMG-CoA reductase) inhibitor, which was developed, and has been available in Japan since July 2003. Metabolism of pitavastatin by the cytochrome P450 (CYP) system is minimal, principally through CYP 2C9, with little involvement of the CYP 3A4 isoenzyme, potentially reducing the risk of drug-drug interactions between pitavastatin and other drugs known to inhibit CYP enzymes. To date, human and animal studies have shown pitavastatin to be potentially as effective in lowering LDL-cholesterol levels as rosuvastatin. Pitavastatin under the trade name Livalo is indicated as an adjunctive therapy to diet to reduce elevated total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), triglycerides (TG), and to increase HDL-C in adult patients with primary hyperlipidemia or mixed dyslipidemia. Pitavastatin competitively inhibits HMG-CoA reductase, which is a rate-determining enzyme involved with biosynthesis of cholesterol, in a manner of competition with the substrate so that it inhibits cholesterol synthesis in the liver. As a result, the expression of LDL-receptors followed by the uptake of LDL from blood to liver is accelerated and then the plasma TC decreases. Further, the sustained inhibition of cholesterol synthesis in the liver decreases levels of very low density lipoproteins. Common statin-related side effects (headaches, stomach upset, abnormal liver function tests and muscle cramps) were similar to other statins.

Originator

Curator's Comment:: was discovered by Nissan Chemical Industries and developed further by Kowa Pharmaceuticals

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
1.69999999999999996 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
LIVALO

Approved Use

Drug therapy should be one component of multiple-risk-factor intervention in individuals who require modifications of their lipid profile. Lipid-altering agents should be used in addition to a diet restricted in saturated fat and cholesterol only when the response to diet and other nonpharmacological measures has been inadequate. LIVALO is a HMG-CoA reductase inhibitor indicated for: Patients with primary hyperlipidemia or mixed dyslipidemia as an adjunctive therapy to diet to reduce elevated total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), triglycerides (TG), and to increase high-density lipoprotein cholesterol (HDL-C) (1.1) Limitations of Use (1.2): Doses of LIVALO greater than 4 mg once daily were associated with an increased risk for severe myopathy in premarketing clinical studies. Do not exceed 4 mg once daily dosing of LIVALO. The effect of LIVALO on cardiovascular morbidity and mortality has not been determined. LIVALO has not been studied in Fredrickson Type I, III, and V dyslipidemias. 1.1 Primary Hyperlipidemia and Mixed Dyslipidemia LIVALO® is indicated as an adjunctive therapy to diet to reduce elevated total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), triglycerides (TG), and to increase HDL-C in adult patients with primary hyperlipidemia or mixed dyslipidemia. 1.2 Limitations of Use Doses of LIVALO greater than 4 mg once daily were associated with an increased risk for severe myopathy in premarketing clinical studies. Do not exceed 4 mg once daily dosing of LIVALO. The effect of LIVALO on cardiovascular morbidity and mortality has not been determined. LIVALO has not been studied in Fredrickson Type I, III, and V dyslipidemias.

Launch Date

1249257600000
Primary
LIVALO

Approved Use

Drug therapy should be one component of multiple-risk-factor intervention in individuals who require modifications of their lipid profile. Lipid-altering agents should be used in addition to a diet restricted in saturated fat and cholesterol only when the response to diet and other nonpharmacological measures has been inadequate. LIVALO is a HMG-CoA reductase inhibitor indicated for: Patients with primary hyperlipidemia or mixed dyslipidemia as an adjunctive therapy to diet to reduce elevated total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), triglycerides (TG), and to increase high-density lipoprotein cholesterol (HDL-C) (1.1) Limitations of Use (1.2): Doses of LIVALO greater than 4 mg once daily were associated with an increased risk for severe myopathy in premarketing clinical studies. Do not exceed 4 mg once daily dosing of LIVALO. The effect of LIVALO on cardiovascular morbidity and mortality has not been determined. LIVALO has not been studied in Fredrickson Type I, III, and V dyslipidemias. 1.1 Primary Hyperlipidemia and Mixed Dyslipidemia LIVALO® is indicated as an adjunctive therapy to diet to reduce elevated total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), triglycerides (TG), and to increase HDL-C in adult patients with primary hyperlipidemia or mixed dyslipidemia. 1.2 Limitations of Use Doses of LIVALO greater than 4 mg once daily were associated with an increased risk for severe myopathy in premarketing clinical studies. Do not exceed 4 mg once daily dosing of LIVALO. The effect of LIVALO on cardiovascular morbidity and mortality has not been determined. LIVALO has not been studied in Fredrickson Type I, III, and V dyslipidemias.

Launch Date

1249257600000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
98.4 ng/mL
2 mg single, oral
dose: 2 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PITAVASTATIN blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
113 ng/mL
2 mg single, oral
dose: 2 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PITAVASTATIN blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
285.77 ng × h/mL
2 mg single, oral
dose: 2 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PITAVASTATIN blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
329.96 ng × h/mL
2 mg single, oral
dose: 2 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PITAVASTATIN blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
9.08 h
2 mg single, oral
dose: 2 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PITAVASTATIN blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
9.95 h
2 mg single, oral
dose: 2 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PITAVASTATIN blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
64 mg 1 times / day steady, oral
Highest studied dose
Dose: 64 mg, 1 times / day
Route: oral
Route: steady
Dose: 64 mg, 1 times / day
Sources:
unhealthy, adult
Disc. AE: Gastrointestinal disorders, Fatigue...
AEs leading to
discontinuation/dose reduction:
Gastrointestinal disorders (3%)
Fatigue (9.1%)
ALT increased (9.1%)
AST increased (9.1%)
Aspartate aminotransferase abnormal NOS (6.1%)
CPK increased (12.1%)
Blood creatine phosphokinase abnormal (6.1%)
Myalgia (18.2%)
Myopathy (6.1%)
Pain in extremity (3%)
Rhabdomyolysis (9.1%)
Renal and urinary disorders (6.1%)
Proteinuria (3%)
Renal failure (3%)
Sources:
1 mg 1 times / day steady, oral
Recommended
Dose: 1 mg, 1 times / day
Route: oral
Route: steady
Dose: 1 mg, 1 times / day
Sources:
unhealthy, adult
Disc. AE: Fatigue...
AEs leading to
discontinuation/dose reduction:
Fatigue (0.3%)
Sources:
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
unhealthy, adult
Disc. AE: Fatigue, ALT increased...
AEs leading to
discontinuation/dose reduction:
Fatigue (0.3%)
ALT increased (0.1%)
Myalgia (0.7%)
Urinary retention (0.1%)
Sources:
4 mg 1 times / day steady, oral
Recommended
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources:
unhealthy, adult
Disc. AE: Fatigue, CPK increased...
AEs leading to
discontinuation/dose reduction:
Fatigue (0.1%)
CPK increased (0.1%)
Pollakiuria (0.1%)
Sources:
16 mg 1 times / day steady, oral
Dose: 16 mg, 1 times / day
Route: oral
Route: steady
Dose: 16 mg, 1 times / day
Sources:
unhealthy, adult
Disc. AE: Fatigue, Pyrexia...
AEs leading to
discontinuation/dose reduction:
Fatigue (2.9%)
Pyrexia (2%)
CPK increased (10.8%)
ALT increased (5.9%)
AST increased (4.9%)
Back pain (2%)
Myalgia (5.9%)
Myopathy (1%)
Rhabdomyolysis (1%)
Myoglobinuria (1%)
Proteinuria (1%)
Sources:
32 mg 1 times / day steady, oral
Dose: 32 mg, 1 times / day
Route: oral
Route: steady
Dose: 32 mg, 1 times / day
Sources:
unhealthy, adult
Disc. AE: Gastrointestinal disorders, ALT increased...
AEs leading to
discontinuation/dose reduction:
Gastrointestinal disorders (2.9%)
ALT increased (11.8%)
AST increased (11.8%)
Blood creatine phosphokinase abnormal (2.9%)
CPK increased (5.9%)
Myalgia (8.8%)
Rhabdomyolysis (5.9%)
Myoglobinuria (2.9%)
Renal and urinary disorders (2.9%)
Sources:
8 mg 1 times / day steady, oral
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Disc. AE: Fatigue, CPK increased...
AEs leading to
discontinuation/dose reduction:
Fatigue (0.2%)
CPK increased (0.4%)
Rhabdomyolysis (0.4%)
Sources:
AEs

AEs

AESignificanceDosePopulation
CPK increased 12.1%
Disc. AE
64 mg 1 times / day steady, oral
Highest studied dose
Dose: 64 mg, 1 times / day
Route: oral
Route: steady
Dose: 64 mg, 1 times / day
Sources:
unhealthy, adult
Myalgia 18.2%
Disc. AE
64 mg 1 times / day steady, oral
Highest studied dose
Dose: 64 mg, 1 times / day
Route: oral
Route: steady
Dose: 64 mg, 1 times / day
Sources:
unhealthy, adult
Gastrointestinal disorders 3%
Disc. AE
64 mg 1 times / day steady, oral
Highest studied dose
Dose: 64 mg, 1 times / day
Route: oral
Route: steady
Dose: 64 mg, 1 times / day
Sources:
unhealthy, adult
Pain in extremity 3%
Disc. AE
64 mg 1 times / day steady, oral
Highest studied dose
Dose: 64 mg, 1 times / day
Route: oral
Route: steady
Dose: 64 mg, 1 times / day
Sources:
unhealthy, adult
Proteinuria 3%
Disc. AE
64 mg 1 times / day steady, oral
Highest studied dose
Dose: 64 mg, 1 times / day
Route: oral
Route: steady
Dose: 64 mg, 1 times / day
Sources:
unhealthy, adult
Renal failure 3%
Disc. AE
64 mg 1 times / day steady, oral
Highest studied dose
Dose: 64 mg, 1 times / day
Route: oral
Route: steady
Dose: 64 mg, 1 times / day
Sources:
unhealthy, adult
Aspartate aminotransferase abnormal NOS 6.1%
Disc. AE
64 mg 1 times / day steady, oral
Highest studied dose
Dose: 64 mg, 1 times / day
Route: oral
Route: steady
Dose: 64 mg, 1 times / day
Sources:
unhealthy, adult
Blood creatine phosphokinase abnormal 6.1%
Disc. AE
64 mg 1 times / day steady, oral
Highest studied dose
Dose: 64 mg, 1 times / day
Route: oral
Route: steady
Dose: 64 mg, 1 times / day
Sources:
unhealthy, adult
Myopathy 6.1%
Disc. AE
64 mg 1 times / day steady, oral
Highest studied dose
Dose: 64 mg, 1 times / day
Route: oral
Route: steady
Dose: 64 mg, 1 times / day
Sources:
unhealthy, adult
Renal and urinary disorders 6.1%
Disc. AE
64 mg 1 times / day steady, oral
Highest studied dose
Dose: 64 mg, 1 times / day
Route: oral
Route: steady
Dose: 64 mg, 1 times / day
Sources:
unhealthy, adult
ALT increased 9.1%
Disc. AE
64 mg 1 times / day steady, oral
Highest studied dose
Dose: 64 mg, 1 times / day
Route: oral
Route: steady
Dose: 64 mg, 1 times / day
Sources:
unhealthy, adult
AST increased 9.1%
Disc. AE
64 mg 1 times / day steady, oral
Highest studied dose
Dose: 64 mg, 1 times / day
Route: oral
Route: steady
Dose: 64 mg, 1 times / day
Sources:
unhealthy, adult
Fatigue 9.1%
Disc. AE
64 mg 1 times / day steady, oral
Highest studied dose
Dose: 64 mg, 1 times / day
Route: oral
Route: steady
Dose: 64 mg, 1 times / day
Sources:
unhealthy, adult
Rhabdomyolysis 9.1%
Disc. AE
64 mg 1 times / day steady, oral
Highest studied dose
Dose: 64 mg, 1 times / day
Route: oral
Route: steady
Dose: 64 mg, 1 times / day
Sources:
unhealthy, adult
Fatigue 0.3%
Disc. AE
1 mg 1 times / day steady, oral
Recommended
Dose: 1 mg, 1 times / day
Route: oral
Route: steady
Dose: 1 mg, 1 times / day
Sources:
unhealthy, adult
ALT increased 0.1%
Disc. AE
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
unhealthy, adult
Urinary retention 0.1%
Disc. AE
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
unhealthy, adult
Fatigue 0.3%
Disc. AE
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
unhealthy, adult
Myalgia 0.7%
Disc. AE
2 mg 1 times / day steady, oral
Recommended
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
unhealthy, adult
CPK increased 0.1%
Disc. AE
4 mg 1 times / day steady, oral
Recommended
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources:
unhealthy, adult
Fatigue 0.1%
Disc. AE
4 mg 1 times / day steady, oral
Recommended
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources:
unhealthy, adult
Pollakiuria 0.1%
Disc. AE
4 mg 1 times / day steady, oral
Recommended
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources:
unhealthy, adult
Myoglobinuria 1%
Disc. AE
16 mg 1 times / day steady, oral
Dose: 16 mg, 1 times / day
Route: oral
Route: steady
Dose: 16 mg, 1 times / day
Sources:
unhealthy, adult
Myopathy 1%
Disc. AE
16 mg 1 times / day steady, oral
Dose: 16 mg, 1 times / day
Route: oral
Route: steady
Dose: 16 mg, 1 times / day
Sources:
unhealthy, adult
Proteinuria 1%
Disc. AE
16 mg 1 times / day steady, oral
Dose: 16 mg, 1 times / day
Route: oral
Route: steady
Dose: 16 mg, 1 times / day
Sources:
unhealthy, adult
Rhabdomyolysis 1%
Disc. AE
16 mg 1 times / day steady, oral
Dose: 16 mg, 1 times / day
Route: oral
Route: steady
Dose: 16 mg, 1 times / day
Sources:
unhealthy, adult
CPK increased 10.8%
Disc. AE
16 mg 1 times / day steady, oral
Dose: 16 mg, 1 times / day
Route: oral
Route: steady
Dose: 16 mg, 1 times / day
Sources:
unhealthy, adult
Back pain 2%
Disc. AE
16 mg 1 times / day steady, oral
Dose: 16 mg, 1 times / day
Route: oral
Route: steady
Dose: 16 mg, 1 times / day
Sources:
unhealthy, adult
Pyrexia 2%
Disc. AE
16 mg 1 times / day steady, oral
Dose: 16 mg, 1 times / day
Route: oral
Route: steady
Dose: 16 mg, 1 times / day
Sources:
unhealthy, adult
Fatigue 2.9%
Disc. AE
16 mg 1 times / day steady, oral
Dose: 16 mg, 1 times / day
Route: oral
Route: steady
Dose: 16 mg, 1 times / day
Sources:
unhealthy, adult
AST increased 4.9%
Disc. AE
16 mg 1 times / day steady, oral
Dose: 16 mg, 1 times / day
Route: oral
Route: steady
Dose: 16 mg, 1 times / day
Sources:
unhealthy, adult
ALT increased 5.9%
Disc. AE
16 mg 1 times / day steady, oral
Dose: 16 mg, 1 times / day
Route: oral
Route: steady
Dose: 16 mg, 1 times / day
Sources:
unhealthy, adult
Myalgia 5.9%
Disc. AE
16 mg 1 times / day steady, oral
Dose: 16 mg, 1 times / day
Route: oral
Route: steady
Dose: 16 mg, 1 times / day
Sources:
unhealthy, adult
ALT increased 11.8%
Disc. AE
32 mg 1 times / day steady, oral
Dose: 32 mg, 1 times / day
Route: oral
Route: steady
Dose: 32 mg, 1 times / day
Sources:
unhealthy, adult
AST increased 11.8%
Disc. AE
32 mg 1 times / day steady, oral
Dose: 32 mg, 1 times / day
Route: oral
Route: steady
Dose: 32 mg, 1 times / day
Sources:
unhealthy, adult
Blood creatine phosphokinase abnormal 2.9%
Disc. AE
32 mg 1 times / day steady, oral
Dose: 32 mg, 1 times / day
Route: oral
Route: steady
Dose: 32 mg, 1 times / day
Sources:
unhealthy, adult
Gastrointestinal disorders 2.9%
Disc. AE
32 mg 1 times / day steady, oral
Dose: 32 mg, 1 times / day
Route: oral
Route: steady
Dose: 32 mg, 1 times / day
Sources:
unhealthy, adult
Myoglobinuria 2.9%
Disc. AE
32 mg 1 times / day steady, oral
Dose: 32 mg, 1 times / day
Route: oral
Route: steady
Dose: 32 mg, 1 times / day
Sources:
unhealthy, adult
Renal and urinary disorders 2.9%
Disc. AE
32 mg 1 times / day steady, oral
Dose: 32 mg, 1 times / day
Route: oral
Route: steady
Dose: 32 mg, 1 times / day
Sources:
unhealthy, adult
CPK increased 5.9%
Disc. AE
32 mg 1 times / day steady, oral
Dose: 32 mg, 1 times / day
Route: oral
Route: steady
Dose: 32 mg, 1 times / day
Sources:
unhealthy, adult
Rhabdomyolysis 5.9%
Disc. AE
32 mg 1 times / day steady, oral
Dose: 32 mg, 1 times / day
Route: oral
Route: steady
Dose: 32 mg, 1 times / day
Sources:
unhealthy, adult
Myalgia 8.8%
Disc. AE
32 mg 1 times / day steady, oral
Dose: 32 mg, 1 times / day
Route: oral
Route: steady
Dose: 32 mg, 1 times / day
Sources:
unhealthy, adult
Fatigue 0.2%
Disc. AE
8 mg 1 times / day steady, oral
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
CPK increased 0.4%
Disc. AE
8 mg 1 times / day steady, oral
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
Rhabdomyolysis 0.4%
Disc. AE
8 mg 1 times / day steady, oral
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources:
unhealthy, adult
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
yes [Ki 2.92 uM]
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
inconclusive
no
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
PubMed

PubMed

TitleDatePubMed
Fibrate and statin synergistically increase the transcriptional activities of PPARalpha/RXRalpha and decrease the transactivation of NFkappaB.
2002 Jan 11
Contribution of vascular NAD(P)H oxidase to endothelial dysfunction in heart failure and the therapeutic effects of HMG-CoA reductase inhibitor.
2004 Nov
Bile salt export pump (BSEP/ABCB11) can transport a nonbile acid substrate, pravastatin.
2005 Aug
Effect of pitavastatin on transactivation of human serum paraoxonase 1 gene.
2005 Feb
Modulation of celecoxib- and streptozotocin-induced experimental dementia of Alzheimer's disease by pitavastatin and donepezil.
2008 Mar
Effects of statins on adipose tissue inflammation: their inhibitory effect on MyD88-independent IRF3/IFN-beta pathway in macrophages.
2008 May
Synthesis and HMG-CoA reductase inhibition of 2-cyclopropyl-4-thiophenyl-quinoline mevalonolactones.
2009 Dec 1
Functional characterization of mouse organic anion transporting peptide 1a4 in the uptake and efflux of drugs across the blood-brain barrier.
2010 Jan
Co-administration of ezetimibe enhances proteinuria-lowering effects of pitavastatin in chronic kidney disease patients partly via a cholesterol-independent manner.
2010 Jan
Regulation mechanism of ABCA1 expression by statins in hepatocytes.
2011 Jul 15
Pharmacokinetic interaction between pitavastatin and valsartan: a randomized, open-labeled crossover study in healthy male Korean volunteers.
2012 Apr
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.
2012 Jul
Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11).
2013 Dec
Detection of statin cytotoxicity is increased in cells expressing the OATP1B1 transporter.
2013 Jul
ATP-dependent transport of statins by human and rat MRP2/Mrp2.
2013 Jun 1
Patents

Sample Use Guides

1 to 4 mg orally once daily at any time of the day with or without food. The recommended starting dose is 2 mg and the maximum dose is 4 mg
Route of Administration: Oral
The liver cancer cells Huh-7 and SMMC7721 were trypsinized into single cells and split into 24-well dishes at 100 cells/well. The cells were pretreated with 0 µM, 0.5 µM, or 1 µM of pitavastatin and cultured for 8 days. Pitavastatin treatment increased the population of Huh-7 cells in the sub-G1 phase. It induced apoptosis of liver cancer cells. It was found that caspase-9 and caspase-3 as well as poly ADP ribose polymerase (PARP) were cleaved.
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:59:32 UTC 2021
Edited
by admin
on Fri Jun 25 21:59:32 UTC 2021
Record UNII
M5681Q5F9P
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PITAVASTATIN
DASH   INN   MART.   MI   VANDF   WHO-DD  
INN  
Official Name English
PITAVASTATIN [MI]
Common Name English
PITAVASTATIN [INN]
Common Name English
PITAVASTATIN [WHO-DD]
Common Name English
PITAVASTATIN [MART.]
Common Name English
NSC-760423
Code English
(3R,5S,6E)-7-(2-CYCLOPROPYL-4-(P-FLUOROPHENYL)-3-QUINOLYL)-3,5-DIHYDROXY-6-HEPTENOIC ACID
Common Name English
ITAVASTATIN
Common Name English
NIKITA
Brand Name English
PITAVASTATIN [VANDF]
Common Name English
Classification Tree Code System Code
WHO-VATC QC10AA08
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
NDF-RT N0000175589
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
LIVERTOX 783
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
NCI_THESAURUS C1655
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
WHO-ATC C10AA08
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
NDF-RT N0000000121
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
Code System Code Type Description
INN
7730
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
PRIMARY
HSDB
8367
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
PRIMARY
RXCUI
861634
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
PRIMARY RxNorm
WIKIPEDIA
PITAVASTATIN
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
PRIMARY
PUBCHEM
5282452
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
PRIMARY
NCI_THESAURUS
C87751
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
PRIMARY
DRUG BANK
DB08860
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
PRIMARY
ChEMBL
CHEMBL1201753
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
PRIMARY
DRUG CENTRAL
2214
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
PRIMARY
LACTMED
Pitavastatin
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
PRIMARY
MESH
C108475
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
PRIMARY
FDA UNII
M5681Q5F9P
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
PRIMARY
CAS
147511-69-1
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
PRIMARY
EVMPD
SUB21363
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
PRIMARY
EPA CompTox
147511-69-1
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
PRIMARY
MERCK INDEX
M8891
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
PRIMARY Merck Index
IUPHAR
3035
Created by admin on Fri Jun 25 21:59:32 UTC 2021 , Edited by admin on Fri Jun 25 21:59:32 UTC 2021
PRIMARY
Related Record Type Details
SALT/SOLVATE -> PARENT
TRANSPORTER -> INHIBITOR
SALT/SOLVATE -> PARENT
BINDER->LIGAND
BINDING
SALT/SOLVATE -> PARENT
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
TARGET -> INHIBITOR
EXCRETED UNCHANGED
AMOUNT EXCRETED
FECAL
SALT/SOLVATE -> PARENT
METABOLIC ENZYME -> SUBSTRATE
MAJOR
EXCRETED UNCHANGED
AMOUNT EXCRETED
URINE
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
METABOLITE -> PARENT
URINE
METABOLITE -> PARENT
FECAL
METABOLITE -> PARENT
MAJOR
PLASMA
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC ORAL ADMINISTRATION

SINGLE DOSE