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Details

Stereochemistry ABSOLUTE
Molecular Formula 2C25H23FNO4.Ca.5H2O
Molecular Weight 971.06
Optical Activity UNSPECIFIED
Defined Stereocenters 4 / 4
E/Z Centers 2
Charge 0

SHOW SMILES / InChI
Structure of PITAVASTATIN CALCIUM PENTAHYDRATE

SMILES

O.O.O.O.O.[Ca++].O[C@H](C[C@H](O)\C=C\C1=C(C2=CC=C(F)C=C2)C3=CC=CC=C3N=C1C4CC4)CC([O-])=O.O[C@H](C[C@H](O)\C=C\C5=C(C6=CC=C(F)C=C6)C7=CC=CC=C7N=C5C8CC8)CC([O-])=O

InChI

InChIKey=NDBJDUMINXAFLN-VKBJLXQDSA-L
InChI=1S/2C25H24FNO4.Ca.5H2O/c2*26-17-9-7-15(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;;;;;;/h2*1-4,7-12,16,18-19,28-29H,5-6,13-14H2,(H,30,31);;5*1H2/q;;+2;;;;;/p-2/b2*12-11+;;;;;;/t2*18-,19-;;;;;;/m11....../s1

HIDE SMILES / InChI

Molecular Formula C25H23FNO4
Molecular Weight 420.4528
Charge -1
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 1
Optical Activity UNSPECIFIED

Molecular Formula Ca
Molecular Weight 40.078
Charge 2
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula H2O
Molecular Weight 18.0153
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: description was created based on several sources, including 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
1.7 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

1.24925759E12
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

1.24925759E12
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: Page: p. 87
unhealthy, adult
n = 33
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 33
Sources: Page: p. 87
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: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 309
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 309
Sources: Page: p. 87
Disc. AE: Fatigue...
AEs leading to
discontinuation/dose reduction:
Fatigue (0.3%)
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 951
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 951
Sources: Page: p. 87
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: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 1540
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 1540
Sources: Page: p. 87
Disc. AE: Fatigue, CPK increased...
AEs leading to
discontinuation/dose reduction:
Fatigue (0.1%)
CPK increased (0.1%)
Pollakiuria (0.1%)
Sources: Page: p. 87
16 mg 1 times / day steady, oral
Dose: 16 mg, 1 times / day
Route: oral
Route: steady
Dose: 16 mg, 1 times / day
Sources: Page: p. 87
unhealthy, adult
n = 102
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 102
Sources: Page: p. 87
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: Page: p. 87
32 mg 1 times / day steady, oral
Dose: 32 mg, 1 times / day
Route: oral
Route: steady
Dose: 32 mg, 1 times / day
Sources: Page: p. 87
unhealthy, adult
n = 34
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 34
Sources: Page: p. 87
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: Page: p. 87
8 mg 1 times / day steady, oral
Dose: 8 mg, 1 times / day
Route: oral
Route: steady
Dose: 8 mg, 1 times / day
Sources: Page: p. 87
unhealthy, adult
n = 479
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 479
Sources: Page: p. 87
Disc. AE: Fatigue, CPK increased...
AEs leading to
discontinuation/dose reduction:
Fatigue (0.2%)
CPK increased (0.4%)
Rhabdomyolysis (0.4%)
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 33
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 33
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 33
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 33
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 33
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 33
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 33
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 33
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 33
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 33
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 33
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 33
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 33
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 33
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 33
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 33
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 33
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 33
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 33
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 33
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 33
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 33
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 33
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 33
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 33
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 33
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 33
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 33
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 309
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 309
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 951
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 951
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 951
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 951
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 951
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 951
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 951
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 951
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 1540
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 1540
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 1540
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 1540
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 1540
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 1540
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 102
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 102
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 102
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 102
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 102
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 102
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 102
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 102
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 102
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 102
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 102
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 102
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 102
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 102
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 102
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 102
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 102
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 102
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 102
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 102
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 102
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 102
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 34
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 34
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 34
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 34
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 34
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 34
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 34
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 34
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 34
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 34
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 34
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 34
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 34
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 34
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 34
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 34
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 34
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 34
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 479
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 479
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 479
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 479
Sources: Page: p. 87
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: Page: p. 87
unhealthy, adult
n = 479
Health Status: unhealthy
Condition: primary hyperlipidemia or mixed dyslipidemia
Age Group: adult
Population Size: 479
Sources: Page: p. 87
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
Effect of pitavastatin on transactivation of human serum paraoxonase 1 gene.
2005 Feb
Involvement of BCRP (ABCG2) in the biliary excretion of pitavastatin.
2005 Sep
Modulation of celecoxib- and streptozotocin-induced experimental dementia of Alzheimer's disease by pitavastatin and donepezil.
2008 Mar
Co-administration of ezetimibe enhances proteinuria-lowering effects of pitavastatin in chronic kidney disease patients partly via a cholesterol-independent manner.
2010 Jan
Pharmacokinetic interaction between pitavastatin and valsartan: a randomized, open-labeled crossover study in healthy male Korean volunteers.
2012 Apr
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 Thu Jul 06 18:27:04 UTC 2023
Edited
by admin
on Thu Jul 06 18:27:04 UTC 2023
Record UNII
GMK323785E
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PITAVASTATIN CALCIUM PENTAHYDRATE
Common Name English
6-HEPTENOIC ACID, 7-(2-CYCLOPROPYL-4-(4-FLUOROPHENYL)-3-QUINOLINYL)-3,5-DIHYDROXY-, CALCIUM SALT, (3R,5S,6E)-, HYDRATE (2:1:5)
Systematic Name English
Pitavastatin calcium pentahydrate [WHO-DD]
Common Name English
PITAVASTATIN CALCIUM HYDRATE [JAN]
Common Name English
PITAVASTATIN CALCIUM HYDRATE
JAN  
Common Name English
Code System Code Type Description
PUBCHEM
122706735
Created by admin on Thu Jul 06 18:27:04 UTC 2023 , Edited by admin on Thu Jul 06 18:27:04 UTC 2023
PRIMARY
SMS_ID
100000167198
Created by admin on Thu Jul 06 18:27:04 UTC 2023 , Edited by admin on Thu Jul 06 18:27:04 UTC 2023
PRIMARY
EVMPD
SUB181602
Created by admin on Thu Jul 06 18:27:04 UTC 2023 , Edited by admin on Thu Jul 06 18:27:04 UTC 2023
PRIMARY
FDA UNII
GMK323785E
Created by admin on Thu Jul 06 18:27:04 UTC 2023 , Edited by admin on Thu Jul 06 18:27:04 UTC 2023
PRIMARY
CAS
1852536-33-4
Created by admin on Thu Jul 06 18:27:04 UTC 2023 , Edited by admin on Thu Jul 06 18:27:04 UTC 2023
PRIMARY
Related Record Type Details
ANHYDROUS->SOLVATE
PARENT -> SALT/SOLVATE
Related Record Type Details
ACTIVE MOIETY