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Details

Stereochemistry ABSOLUTE
Molecular Formula C26H34FNO5
Molecular Weight 459.5513
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of CERIVASTATIN

SMILES

CC(C)c1c(/C(/[H])=C(\[H])/[C@]([H])(C[C@]([H])(CC(=O)O)O)O)c(-c2ccc(cc2)F)c(COC)c(C(C)C)n1

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

HIDE SMILES / InChI

Molecular Formula C26H34FNO5
Molecular Weight 459.5513
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.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 It has also been withdrawn from the Canadian market.

CNS Activity

Curator's Comment:: Cerivastatin, fluvastatin, and pravastatin are hydrophilic compounds incapable of affecting the CNS.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
BAYCOL

Approved Use

BAYCOL® (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 Date

867283200000
Primary
BAYCOL

Approved Use

BAYCOL® (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 Date

867283200000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
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

AUC

ValueDoseCo-administeredAnalytePopulation
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

T1/2

ValueDoseCo-administeredAnalytePopulation
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

Funbound

ValueDoseCo-administeredAnalytePopulation
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

Doses

DosePopulationAdverse 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
Health Status: unhealthy
Age Group: 57.2 years
Sex: M+F
Sources:
Disc. AE: CPK increased, Elevated liver enzymes...
AEs leading to
discontinuation/dose reduction:
CPK increased (10 patients)
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)
Sources:
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
Health Status: unhealthy
Age Group: 57.3 years
Sex: M+F
Sources:
Disc. AE: CPK increased, Elevated liver enzymes...
AEs leading to
discontinuation/dose reduction:
CPK increased (2 patients)
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)
Sources:
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
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Disc. AE: Rhinitis, Headache...
AEs leading to
discontinuation/dose reduction:
Rhinitis (2.8%)
Headache (3%)
Sources:
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
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Disc. AE: Gastrointestinal disorders...
AEs leading to
discontinuation/dose reduction:
Gastrointestinal disorders (3%)
Sources:
AEs

AEs

AESignificanceDosePopulation
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
Health Status: unhealthy
Age Group: 57.2 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.2 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.2 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.2 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.2 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.2 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.2 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.2 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.2 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.2 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.2 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.2 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.2 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.2 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.2 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.2 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.2 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.2 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.3 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.3 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.3 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.3 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.3 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.3 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.3 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 57.3 years
Sex: M+F
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
Health Status: unhealthy
Age Group: adult
Sex: unknown
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
Health Status: unhealthy
Age Group: adult
Sex: unknown
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
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer







Drug as perpetrator​

Drug as perpetrator​

Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical 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
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
PubMed

PubMed

TitleDatePubMed
Withdrawal of cerivastatin from the world market.
2001
Preclinical and clinical pharmacology of Rosuvastatin, a new 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor.
2001 Mar 8
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
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 Sat Jun 26 03:33:12 UTC 2021
Edited
by admin
on Sat Jun 26 03:33:12 UTC 2021
Record UNII
AM91H2KS67
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
CERIVASTATIN
HSDB   INN   MI   VANDF   WHO-DD  
INN  
Official Name English
CERIVASTATIN [HSDB]
Common Name English
CERIVASTATIN [INN]
Common Name English
CERIVASTATIN [MI]
Common Name English
CERIVASTATIN [WHO-DD]
Common Name English
CERIVASTATIN [VANDF]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C1655
Created by admin on Sat Jun 26 03:33:12 UTC 2021 , Edited by admin on Sat Jun 26 03:33:12 UTC 2021
WHO-ATC C10AA06
Created by admin on Sat Jun 26 03:33:12 UTC 2021 , Edited by admin on Sat Jun 26 03:33:12 UTC 2021
WHO-VATC QC10AA06
Created by admin on Sat Jun 26 03:33:12 UTC 2021 , Edited by admin on Sat Jun 26 03:33:12 UTC 2021
Code System Code Type Description
WIKIPEDIA
CERIVASTATIN
Created by admin on Sat Jun 26 03:33:12 UTC 2021 , Edited by admin on Sat Jun 26 03:33:12 UTC 2021
PRIMARY
EPA CompTox
145599-86-6
Created by admin on Sat Jun 26 03:33:12 UTC 2021 , Edited by admin on Sat Jun 26 03:33:12 UTC 2021
PRIMARY
PUBCHEM
446156
Created by admin on Sat Jun 26 03:33:12 UTC 2021 , Edited by admin on Sat Jun 26 03:33:12 UTC 2021
PRIMARY
MERCK INDEX
M3262
Created by admin on Sat Jun 26 03:33:12 UTC 2021 , Edited by admin on Sat Jun 26 03:33:12 UTC 2021
PRIMARY Merck Index
IUPHAR
2950
Created by admin on Sat Jun 26 03:33:12 UTC 2021 , Edited by admin on Sat Jun 26 03:33:12 UTC 2021
PRIMARY
INN
7083
Created by admin on Sat Jun 26 03:33:12 UTC 2021 , Edited by admin on Sat Jun 26 03:33:12 UTC 2021
PRIMARY
MESH
C086276
Created by admin on Sat Jun 26 03:33:12 UTC 2021 , Edited by admin on Sat Jun 26 03:33:12 UTC 2021
PRIMARY
DRUG CENTRAL
577
Created by admin on Sat Jun 26 03:33:12 UTC 2021 , Edited by admin on Sat Jun 26 03:33:12 UTC 2021
PRIMARY
DRUG BANK
DB00439
Created by admin on Sat Jun 26 03:33:12 UTC 2021 , Edited by admin on Sat Jun 26 03:33:12 UTC 2021
PRIMARY
ChEMBL
CHEMBL1477
Created by admin on Sat Jun 26 03:33:12 UTC 2021 , Edited by admin on Sat Jun 26 03:33:12 UTC 2021
PRIMARY
NCI_THESAURUS
C65308
Created by admin on Sat Jun 26 03:33:12 UTC 2021 , Edited by admin on Sat Jun 26 03:33:12 UTC 2021
PRIMARY
CAS
145599-86-6
Created by admin on Sat Jun 26 03:33:12 UTC 2021 , Edited by admin on Sat Jun 26 03:33:12 UTC 2021
PRIMARY
HSDB
7357
Created by admin on Sat Jun 26 03:33:12 UTC 2021 , Edited by admin on Sat Jun 26 03:33:12 UTC 2021
PRIMARY
EVMPD
SUB07440MIG
Created by admin on Sat Jun 26 03:33:12 UTC 2021 , Edited by admin on Sat Jun 26 03:33:12 UTC 2021
PRIMARY
FDA UNII
AM91H2KS67
Created by admin on Sat Jun 26 03:33:12 UTC 2021 , Edited by admin on Sat Jun 26 03:33:12 UTC 2021
PRIMARY
RXCUI
596723
Created by admin on Sat Jun 26 03:33:12 UTC 2021 , Edited by admin on Sat Jun 26 03:33:12 UTC 2021
PRIMARY
Related Record Type Details
SALT/SOLVATE -> PARENT
TRANSPORTER -> INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
TARGET -> INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
TRANSPORTER -> INHIBITOR
TRANSPORTER -> INHIBITOR
BINDER->LIGAND
BINDING
Related Record Type Details
METABOLITE -> PARENT
CYP2C8 accounts for up to 60% of cerivastatin?s oxidation
METABOLITE -> PARENT
CYP3A4 contributes to approximately 40% of mostly M-1 formation
METABOLITE -> PARENT
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC