Details
Stereochemistry | ABSOLUTE |
Molecular Formula | 2C25H23FNO4.Ca |
Molecular Weight | 880.984 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 2 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[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=RHGYHLPFVJEAOC-FFNUKLMVSA-L
InChI=1S/2C25H24FNO4.Ca/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);/q;;+2/p-2/b2*12-11+;/t2*18-,19-;/m11./s1
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 |
DescriptionCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/20179258
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.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL402 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20699675 |
1.7 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | LIVALO Approved UseDrug 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 Date2009 |
|||
Primary | LIVALO Approved UseDrug 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 Date2009 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
98.4 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/26082816 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/26082816 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
285.77 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/26082816 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/26082816 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
9.08 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/26082816 |
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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/26082816 |
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
Dose | Population | Adverse 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%) Sources: Page: p. 87Fatigue (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%) |
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%) Sources: Page: p. 87ALT increased (0.1%) Myalgia (0.7%) Urinary retention (0.1%) |
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%) Sources: Page: p. 87CPK increased (0.1%) Pollakiuria (0.1%) |
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%) Sources: Page: p. 87Pyrexia (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%) |
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%) Sources: Page: p. 87ALT 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%) |
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%) Sources: Page: p. 87CPK increased (0.4%) Rhabdomyolysis (0.4%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208379Orig1s000ClinPharmR.pdf#page=6 Page: 6.0 |
no | |||
no | ||||
yes [Ki 2.92 uM] | ||||
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
inconclusive | ||||
no | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes |
PubMed
Title | Date | PubMed |
---|---|---|
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 |
|
Functional characterization of mouse organic anion transporting peptide 1a4 in the uptake and efflux of drugs across the blood-brain barrier. | 2010 Jan |
|
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 |
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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27621652
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
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on
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Fri Dec 15 15:36:21 GMT 2023
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Record UNII |
IYD54XEG3W
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C1655
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Related Record | Type | Details | ||
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SOLVATE->ANHYDROUS | |||
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PARENT -> SALT/SOLVATE |
Related Record | Type | Details | ||
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ACTIVE MOIETY |