Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C26H34FNO5 |
Molecular Weight | 459.5503 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 1 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COCC1=C(C2=CC=C(F)C=C2)C(\C=C\[C@@H](O)C[C@@H](O)CC(O)=O)=C(N=C1C(C)C)C(C)C
InChI
InChIKey=SEERZIQQUAZTOL-ANMDKAQQSA-N
InChI=1S/C26H34FNO5/c1-15(2)25-21(11-10-19(29)12-20(30)13-23(31)32)24(17-6-8-18(27)9-7-17)22(14-33-5)26(28-25)16(3)4/h6-11,15-16,19-20,29-30H,12-14H2,1-5H3,(H,31,32)/b11-10+/t19-,20-/m1/s1
Molecular Formula | C26H34FNO5 |
Molecular Weight | 459.5503 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 1 |
Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: description was created based on several sources, including
https://www.drugbank.ca/drugs/DB00439
Curator's Comment: description was created based on several sources, including
https://www.drugbank.ca/drugs/DB00439
Cerivastatin (BAYCOL®) is a competitive inhibitor of HMG-CoA reductase, which is responsible for the conversion of 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) to mevalonate, a precursor of sterols, including cholesterol. The inhibition of cholesterol biosynthesis by cerivastatin reduces the level of cholesterol in hepatic cells, which stimulates the synthesis of low-density lipoprotein (LDL) receptors, thereby increasing the uptake of cellular LDL particles. The end result of these biochemical processes is a reduction of the plasma cholesterol concentration. On August 8, 2001 the U.S. Food and Drug Administration (FDA) announced that Bayer Pharmaceutical Division voluntarily withdrew BAYCOL® from the U.S. market, due to reports of fatal rhabdomyolysis, a severe adverse reaction from this cholesterol-lowering (lipid-lowering) product. It has also been withdrawn from the Canadian market.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL402 |
5.7 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | BAYCOL Approved UseBAYCOL® (cerivastatin sodium tablets) is indicated as an adjunct to diet to reduce elevated Total-C, LDLC, apo B, and TG and to increase HDL-C levels in patients with primary hypercholesterolemia and mixed dyslipidemia (Fredrickson Types IIa and IIb) when the response to dietary restriction of saturated fat and cholesterol and other non-pharmacological measures alone has been inadequate. Therapy with lipidaltering drugs should be a component of multiple risk factor intervention in those patients at significantly high risk for atherosclerotic vascular disease due to hypercholesterolemia Launch Date1997 |
|||
Primary | BAYCOL Approved UseBAYCOL® (cerivastatin sodium tablets) is indicated as an adjunct to diet to reduce elevated Total-C, LDLC, apo B, and TG and to increase HDL-C levels in patients with primary hypercholesterolemia and mixed dyslipidemia (Fredrickson Types IIa and IIb) when the response to dietary restriction of saturated fat and cholesterol and other non-pharmacological measures alone has been inadequate. Therapy with lipidaltering drugs should be a component of multiple risk factor intervention in those patients at significantly high risk for atherosclerotic vascular disease due to hypercholesterolemia Launch Date1997 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2.31 μg/L |
200 μg 1 times / day steady-state, oral dose: 200 μg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
3.96 μg/L |
300 μg 1 times / day steady-state, oral dose: 300 μg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
4.41 μg/L |
400 μg 1 times / day steady-state, oral dose: 400 μg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
1.14 μg/L |
100 μg 1 times / day steady-state, oral dose: 100 μg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
2.15 μg/L |
200 μg single, oral dose: 200 μg route of administration: Oral experiment type: SINGLE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
3.55 μg/L |
300 μg single, oral dose: 300 μg route of administration: Oral experiment type: SINGLE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
4.04 μg/L |
400 μg single, oral dose: 400 μg route of administration: Oral experiment type: SINGLE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
1.01 μg/L |
100 μg single, oral dose: 100 μg route of administration: Oral experiment type: SINGLE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
12.4 μg × h/L |
200 μg 1 times / day steady-state, oral dose: 200 μg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
21.73 μg × h/L |
300 μg 1 times / day steady-state, oral dose: 300 μg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
24.67 μg × h/L |
400 μg 1 times / day steady-state, oral dose: 400 μg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
6.33 μg × h/L |
100 μg 1 times / day steady-state, oral dose: 100 μg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
11.71 μg × h/L |
200 μg single, oral dose: 200 μg route of administration: Oral experiment type: SINGLE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
20.52 μg × h/L |
300 μg single, oral dose: 300 μg route of administration: Oral experiment type: SINGLE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
22.45 μg × h/L |
400 μg single, oral dose: 400 μg route of administration: Oral experiment type: SINGLE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
6.25 μg × h/L |
100 μg single, oral dose: 100 μg route of administration: Oral experiment type: SINGLE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2.74 h |
200 μg 1 times / day steady-state, oral dose: 200 μg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
3.79 h |
300 μg 1 times / day steady-state, oral dose: 300 μg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
5.16 h |
400 μg 1 times / day steady-state, oral dose: 400 μg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
3.19 h |
100 μg 1 times / day steady-state, oral dose: 100 μg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
3.08 h |
200 μg single, oral dose: 200 μg route of administration: Oral experiment type: SINGLE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
4.89 h |
300 μg single, oral dose: 300 μg route of administration: Oral experiment type: SINGLE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
4.23 h |
400 μg single, oral dose: 400 μg route of administration: Oral experiment type: SINGLE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
3.37 h |
100 μg single, oral dose: 100 μg route of administration: Oral experiment type: SINGLE co-administered: |
CERIVASTATIN SODIUM plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1% |
200 μg 1 times / day steady-state, oral dose: 200 μg route of administration: Oral experiment type: STEADY-STATE co-administered: |
CERIVASTATIN SODIUM blood | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
0.8 mg 1 times / day steady, oral Studied dose Dose: 0.8 mg, 1 times / day Route: oral Route: steady Dose: 0.8 mg, 1 times / day Sources: |
unhealthy, 57.2 years n = 776 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.2 years Sex: M+F Population Size: 776 Sources: |
Disc. AE: CPK increased, Elevated liver enzymes... AEs leading to discontinuation/dose reduction: CPK increased (10 patients) Sources: Elevated liver enzymes (7 patients) Constipation (1 patient) Dyspepsia (1 patient) Flatulence (2 patients) Nausea (2 patients) Vomiting (2 patients) Chest pain (1 patient) Eye pain (1 patient) Head pain (1 patient) Leg pain (1 patient) Skin disorder (3 patients) Dizziness (2 patients) Insomnia (1 patient) Arthralgia (1 patient) Leg cramps (1 patient) Myalgia (3 patients) Myasthenia (1 patient) |
0.4 mg 1 times / day steady, oral Recommended Dose: 0.4 mg, 1 times / day Route: oral Route: steady Dose: 0.4 mg, 1 times / day Sources: |
unhealthy, 57.3 years n = 195 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.3 years Sex: M+F Population Size: 195 Sources: |
Disc. AE: CPK increased, Elevated liver enzymes... AEs leading to discontinuation/dose reduction: CPK increased (2 patients) Sources: Elevated liver enzymes (2 patients) Ulcerative colitis (1 patient) Headache (1 patient) Rash (2 patients) Exfoliative dermatitis (2 patients) Leg cramps (1 patient) Myalgia (2 patients) |
0.4 mg 1 times / day steady, oral Recommended Dose: 0.4 mg, 1 times / day Route: oral Route: steady Dose: 0.4 mg, 1 times / day Sources: |
unhealthy, adult n = 1263 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: adult Sex: unknown Population Size: 1263 Sources: |
Disc. AE: Rhinitis, Headache... AEs leading to discontinuation/dose reduction: Rhinitis (2.8%) Sources: Headache (3%) |
0.4 mg 1 times / day steady, oral Recommended Dose: 0.4 mg, 1 times / day Route: oral Route: steady Dose: 0.4 mg, 1 times / day Sources: |
unhealthy, adult n = 2816 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: adult Sex: unknown Population Size: 2816 Sources: |
Disc. AE: Gastrointestinal disorders... AEs leading to discontinuation/dose reduction: Gastrointestinal disorders (3%) Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Arthralgia | 1 patient Disc. AE |
0.8 mg 1 times / day steady, oral Studied dose Dose: 0.8 mg, 1 times / day Route: oral Route: steady Dose: 0.8 mg, 1 times / day Sources: |
unhealthy, 57.2 years n = 776 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.2 years Sex: M+F Population Size: 776 Sources: |
Chest pain | 1 patient Disc. AE |
0.8 mg 1 times / day steady, oral Studied dose Dose: 0.8 mg, 1 times / day Route: oral Route: steady Dose: 0.8 mg, 1 times / day Sources: |
unhealthy, 57.2 years n = 776 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.2 years Sex: M+F Population Size: 776 Sources: |
Constipation | 1 patient Disc. AE |
0.8 mg 1 times / day steady, oral Studied dose Dose: 0.8 mg, 1 times / day Route: oral Route: steady Dose: 0.8 mg, 1 times / day Sources: |
unhealthy, 57.2 years n = 776 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.2 years Sex: M+F Population Size: 776 Sources: |
Dyspepsia | 1 patient Disc. AE |
0.8 mg 1 times / day steady, oral Studied dose Dose: 0.8 mg, 1 times / day Route: oral Route: steady Dose: 0.8 mg, 1 times / day Sources: |
unhealthy, 57.2 years n = 776 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.2 years Sex: M+F Population Size: 776 Sources: |
Eye pain | 1 patient Disc. AE |
0.8 mg 1 times / day steady, oral Studied dose Dose: 0.8 mg, 1 times / day Route: oral Route: steady Dose: 0.8 mg, 1 times / day Sources: |
unhealthy, 57.2 years n = 776 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.2 years Sex: M+F Population Size: 776 Sources: |
Head pain | 1 patient Disc. AE |
0.8 mg 1 times / day steady, oral Studied dose Dose: 0.8 mg, 1 times / day Route: oral Route: steady Dose: 0.8 mg, 1 times / day Sources: |
unhealthy, 57.2 years n = 776 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.2 years Sex: M+F Population Size: 776 Sources: |
Insomnia | 1 patient Disc. AE |
0.8 mg 1 times / day steady, oral Studied dose Dose: 0.8 mg, 1 times / day Route: oral Route: steady Dose: 0.8 mg, 1 times / day Sources: |
unhealthy, 57.2 years n = 776 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.2 years Sex: M+F Population Size: 776 Sources: |
Leg cramps | 1 patient Disc. AE |
0.8 mg 1 times / day steady, oral Studied dose Dose: 0.8 mg, 1 times / day Route: oral Route: steady Dose: 0.8 mg, 1 times / day Sources: |
unhealthy, 57.2 years n = 776 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.2 years Sex: M+F Population Size: 776 Sources: |
Leg pain | 1 patient Disc. AE |
0.8 mg 1 times / day steady, oral Studied dose Dose: 0.8 mg, 1 times / day Route: oral Route: steady Dose: 0.8 mg, 1 times / day Sources: |
unhealthy, 57.2 years n = 776 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.2 years Sex: M+F Population Size: 776 Sources: |
Myasthenia | 1 patient Disc. AE |
0.8 mg 1 times / day steady, oral Studied dose Dose: 0.8 mg, 1 times / day Route: oral Route: steady Dose: 0.8 mg, 1 times / day Sources: |
unhealthy, 57.2 years n = 776 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.2 years Sex: M+F Population Size: 776 Sources: |
CPK increased | 10 patients Disc. AE |
0.8 mg 1 times / day steady, oral Studied dose Dose: 0.8 mg, 1 times / day Route: oral Route: steady Dose: 0.8 mg, 1 times / day Sources: |
unhealthy, 57.2 years n = 776 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.2 years Sex: M+F Population Size: 776 Sources: |
Dizziness | 2 patients Disc. AE |
0.8 mg 1 times / day steady, oral Studied dose Dose: 0.8 mg, 1 times / day Route: oral Route: steady Dose: 0.8 mg, 1 times / day Sources: |
unhealthy, 57.2 years n = 776 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.2 years Sex: M+F Population Size: 776 Sources: |
Flatulence | 2 patients Disc. AE |
0.8 mg 1 times / day steady, oral Studied dose Dose: 0.8 mg, 1 times / day Route: oral Route: steady Dose: 0.8 mg, 1 times / day Sources: |
unhealthy, 57.2 years n = 776 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.2 years Sex: M+F Population Size: 776 Sources: |
Nausea | 2 patients Disc. AE |
0.8 mg 1 times / day steady, oral Studied dose Dose: 0.8 mg, 1 times / day Route: oral Route: steady Dose: 0.8 mg, 1 times / day Sources: |
unhealthy, 57.2 years n = 776 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.2 years Sex: M+F Population Size: 776 Sources: |
Vomiting | 2 patients Disc. AE |
0.8 mg 1 times / day steady, oral Studied dose Dose: 0.8 mg, 1 times / day Route: oral Route: steady Dose: 0.8 mg, 1 times / day Sources: |
unhealthy, 57.2 years n = 776 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.2 years Sex: M+F Population Size: 776 Sources: |
Myalgia | 3 patients Disc. AE |
0.8 mg 1 times / day steady, oral Studied dose Dose: 0.8 mg, 1 times / day Route: oral Route: steady Dose: 0.8 mg, 1 times / day Sources: |
unhealthy, 57.2 years n = 776 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.2 years Sex: M+F Population Size: 776 Sources: |
Skin disorder | 3 patients Disc. AE |
0.8 mg 1 times / day steady, oral Studied dose Dose: 0.8 mg, 1 times / day Route: oral Route: steady Dose: 0.8 mg, 1 times / day Sources: |
unhealthy, 57.2 years n = 776 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.2 years Sex: M+F Population Size: 776 Sources: |
Elevated liver enzymes | 7 patients Disc. AE |
0.8 mg 1 times / day steady, oral Studied dose Dose: 0.8 mg, 1 times / day Route: oral Route: steady Dose: 0.8 mg, 1 times / day Sources: |
unhealthy, 57.2 years n = 776 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.2 years Sex: M+F Population Size: 776 Sources: |
Headache | 1 patient Disc. AE |
0.4 mg 1 times / day steady, oral Recommended Dose: 0.4 mg, 1 times / day Route: oral Route: steady Dose: 0.4 mg, 1 times / day Sources: |
unhealthy, 57.3 years n = 195 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.3 years Sex: M+F Population Size: 195 Sources: |
Leg cramps | 1 patient Disc. AE |
0.4 mg 1 times / day steady, oral Recommended Dose: 0.4 mg, 1 times / day Route: oral Route: steady Dose: 0.4 mg, 1 times / day Sources: |
unhealthy, 57.3 years n = 195 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.3 years Sex: M+F Population Size: 195 Sources: |
Ulcerative colitis | 1 patient Disc. AE |
0.4 mg 1 times / day steady, oral Recommended Dose: 0.4 mg, 1 times / day Route: oral Route: steady Dose: 0.4 mg, 1 times / day Sources: |
unhealthy, 57.3 years n = 195 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.3 years Sex: M+F Population Size: 195 Sources: |
CPK increased | 2 patients Disc. AE |
0.4 mg 1 times / day steady, oral Recommended Dose: 0.4 mg, 1 times / day Route: oral Route: steady Dose: 0.4 mg, 1 times / day Sources: |
unhealthy, 57.3 years n = 195 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.3 years Sex: M+F Population Size: 195 Sources: |
Elevated liver enzymes | 2 patients Disc. AE |
0.4 mg 1 times / day steady, oral Recommended Dose: 0.4 mg, 1 times / day Route: oral Route: steady Dose: 0.4 mg, 1 times / day Sources: |
unhealthy, 57.3 years n = 195 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.3 years Sex: M+F Population Size: 195 Sources: |
Exfoliative dermatitis | 2 patients Disc. AE |
0.4 mg 1 times / day steady, oral Recommended Dose: 0.4 mg, 1 times / day Route: oral Route: steady Dose: 0.4 mg, 1 times / day Sources: |
unhealthy, 57.3 years n = 195 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.3 years Sex: M+F Population Size: 195 Sources: |
Myalgia | 2 patients Disc. AE |
0.4 mg 1 times / day steady, oral Recommended Dose: 0.4 mg, 1 times / day Route: oral Route: steady Dose: 0.4 mg, 1 times / day Sources: |
unhealthy, 57.3 years n = 195 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.3 years Sex: M+F Population Size: 195 Sources: |
Rash | 2 patients Disc. AE |
0.4 mg 1 times / day steady, oral Recommended Dose: 0.4 mg, 1 times / day Route: oral Route: steady Dose: 0.4 mg, 1 times / day Sources: |
unhealthy, 57.3 years n = 195 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: 57.3 years Sex: M+F Population Size: 195 Sources: |
Rhinitis | 2.8% Disc. AE |
0.4 mg 1 times / day steady, oral Recommended Dose: 0.4 mg, 1 times / day Route: oral Route: steady Dose: 0.4 mg, 1 times / day Sources: |
unhealthy, adult n = 1263 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: adult Sex: unknown Population Size: 1263 Sources: |
Headache | 3% Disc. AE |
0.4 mg 1 times / day steady, oral Recommended Dose: 0.4 mg, 1 times / day Route: oral Route: steady Dose: 0.4 mg, 1 times / day Sources: |
unhealthy, adult n = 1263 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: adult Sex: unknown Population Size: 1263 Sources: |
Gastrointestinal disorders | 3% Disc. AE |
0.4 mg 1 times / day steady, oral Recommended Dose: 0.4 mg, 1 times / day Route: oral Route: steady Dose: 0.4 mg, 1 times / day Sources: |
unhealthy, adult n = 2816 Health Status: unhealthy Condition: hypercholesterolaemia Age Group: adult Sex: unknown Population Size: 2816 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
weak [IC50 30 uM] | ||||
yes [IC50 66.2 uM] | ||||
yes [Ki 11.4 uM] | ||||
yes [Ki 18.1 uM] |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes | ||||
yes | ||||
yes | yes (co-administration study) Comment: inhibition by gemfibrozil have shown an increase in cerivastatin plasma AUC values from 1.3- to 10-fold. Page: 2.0 |
|||
Page: 2.0 |
yes | yes (co-administration study) Comment: specific inhibition of the CYP 3A4 enzyme sub-class resulted in a 1.4- to 1.5-fold mean increase in cerivastatin plasma levels following cotreatment with erythromycin or itraconazole, possibly because of metabolism via the alternate CYP 2C8 pathway Page: 2.0 |
PubMed
Title | Date | PubMed |
---|---|---|
Withdrawal of cerivastatin from the world market. | 2001 |
|
Three-dimensional quantitative structure (3-D QSAR) activity relationship studies on imidazolyl and N-pyrrolyl heptenoates as 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) inhibitors by comparative molecular similarity indices analysis (CoMSIA). | 2005 Feb 15 |
|
Prediction of genotoxicity of chemical compounds by statistical learning methods. | 2005 Jun |
|
Binding thermodynamics of statins to HMG-CoA reductase. | 2005 Sep 6 |
Patents
Sample Use Guides
The starting-dose of BAYCOL® is 0.4 mg once daily in the evening regardless of previous lipid therapy. Since the maximal effect of cerivastatin is seen within 4 weeks lipid determinations should be performed at this time and the dose adjusted based upon patient response. Only patients requiring further lipid adjustment should be titrated to 0.8 mg. The dosage range is 0.2 mg to 0.8 mg. Cerivastatin may be taken with or without food.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9395280
Cerivastatin inhibited the membrane-bound (non-solubilized) 3-hydroxy-3-methylglutaryl-CoA (HMG-CoA) reductase of the native microsomal fraction isolated from rat liver with a Ki value of 1.3 nM. Cerivastatin inhibited the cholesterol synthesis in the human hepatoma cell line HepG2 cells with a IC50 value of 1.0 nM.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 16:33:28 GMT 2023
by
admin
on
Fri Dec 15 16:33:28 GMT 2023
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Record UNII |
AM91H2KS67
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C1655
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WHO-ATC |
C10AA06
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WHO-VATC |
QC10AA06
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admin on Fri Dec 15 16:33:28 GMT 2023 , Edited by admin on Fri Dec 15 16:33:28 GMT 2023
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Code System | Code | Type | Description | ||
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100000082046
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PRIMARY | |||
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CERIVASTATIN
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DTXSID9022786
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PRIMARY | |||
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446156
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admin on Fri Dec 15 16:33:28 GMT 2023 , Edited by admin on Fri Dec 15 16:33:28 GMT 2023
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m3262
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admin on Fri Dec 15 16:33:28 GMT 2023 , Edited by admin on Fri Dec 15 16:33:28 GMT 2023
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2950
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admin on Fri Dec 15 16:33:28 GMT 2023 , Edited by admin on Fri Dec 15 16:33:28 GMT 2023
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7083
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3558
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admin on Fri Dec 15 16:33:28 GMT 2023 , Edited by admin on Fri Dec 15 16:33:28 GMT 2023
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C086276
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577
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DB00439
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CHEMBL1477
Created by
admin on Fri Dec 15 16:33:28 GMT 2023 , Edited by admin on Fri Dec 15 16:33:28 GMT 2023
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C65308
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admin on Fri Dec 15 16:33:28 GMT 2023 , Edited by admin on Fri Dec 15 16:33:28 GMT 2023
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145599-86-6
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admin on Fri Dec 15 16:33:28 GMT 2023 , Edited by admin on Fri Dec 15 16:33:28 GMT 2023
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7357
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admin on Fri Dec 15 16:33:28 GMT 2023 , Edited by admin on Fri Dec 15 16:33:28 GMT 2023
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SUB07440MIG
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admin on Fri Dec 15 16:33:28 GMT 2023 , Edited by admin on Fri Dec 15 16:33:28 GMT 2023
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AM91H2KS67
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596723
Created by
admin on Fri Dec 15 16:33:28 GMT 2023 , Edited by admin on Fri Dec 15 16:33:28 GMT 2023
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Related Record | Type | Details | ||
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TRANSPORTER -> INHIBITOR | |||
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SALT/SOLVATE -> PARENT |
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TRANSPORTER -> INHIBITOR | |||
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METABOLIC ENZYME -> SUBSTRATE |
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TRANSPORTER -> INHIBITOR | |||
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TARGET -> INHIBITOR |
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METABOLIC ENZYME -> SUBSTRATE |
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TARGET -> INHIBITOR |
Cerivastatin inhibited the cholesterol synthesis in the human hepatoma cell line HepG2 cells with a similar IC50 value of 1.0 x 10(-9) M.
IC50
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BINDER->LIGAND |
BINDING
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Related Record | Type | Details | ||
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METABOLITE -> PARENT |
CYP2C8 accounts for
up to 60% of cerivastatin?s oxidation
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METABOLITE -> PARENT |
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METABOLITE -> PARENT |
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METABOLITE -> PARENT |
CYP3A4 contributes to approximately 40% of
mostly M-1 formation
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METABOLITE -> PARENT |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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Volume of Distribution | PHARMACOKINETIC |
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