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Drug

D0021 | Cerivastatin

Molecular Formula C26H34FNO5
Molecular Weight 459.5
Structure
State solid
Protein binding More than 99% of the circulating drug is bound to plasma proteins (80% to albumin).
Half life 2-3 hours
Absorption The mean absolute oral bioavailability 60% (range 39 - 101%).
Trade names Baycol, Lipobay
Description synthetic member of the class of statins (HMG-CoA reductase inhibitors); cholesterol-lowering (lipid-lowering)

C

C10AA06 Cerivastatin


[C10AA] HMG CoA reductase inhibitors


[C10A] LIPID MODIFYING AGENTS, PLAIN


[C10] LIPID MODIFYING AGENTS


[C] Cardiovascular system

Toxicity Dose Time Species Model Method Action Positive criterion Reference
OPENING OF PERMEABILITY TRANSITION PORE (PTP) 10 µM 1 hour Human HepG2 High-content screening assay Decrease MEC 306
MEMBRANE POTENTIAL 50 µM 1 hour Human HepG2 High-content screening assay Decrease MEC 306
ELECTRON TRANSPORT CHAIN 100uM C2C12 myoblasts measured ubiquinol:cytochrome c oxidoreductase activity in broken C2C12 mitochondria after acute statin exposure at a fixed concentration for all compounds decrease 180
ROS PRODUCTION 5 µM 1 hour Human HepG2 High-content screening assay Increase MEC 306

Target Dose Time Species Model Method Action Positive criterion Reference
Quinol--cytochrome-c reductase 100uM C2C12 myoblasts measured ubiquinol:cytochrome c oxidoreductase activity in broken C2C12 mitochondria after acute statin exposure at a fixed concentration for all compounds inhibitor 180
Reactive oxygen species 5 µM 1 hour Human HepG2 High-content screening assay increase MEC 306

Organism Test type Route Dose (normalized dose) Effect Source
mouse LD50 intravenous 221mg/kg (221mg/kg) Gekkan Yakuji. Pharmaceuticals Monthly. Vol. 42, Pg. 402, 2000.
rat LD50 oral 416mg/kg (416mg/kg) Gekkan Yakuji. Pharmaceuticals Monthly. Vol. 42, Pg. 402, 2000.
mouse LD50 oral 416mg/kg (416mg/kg) Gekkan Yakuji. Pharmaceuticals Monthly. Vol. 42, Pg. 402, 2000.
dog LDLo oral 32mg/kg (32mg/kg) Gekkan Yakuji. Pharmaceuticals Monthly. Vol. 42, Pg. 402, 2000.

  • Blood triglycerides increased

  • Carotid artery disease

  • Coronary artery disease

  • Diabetes mellitus

  • Dyslipidaemia

  • High density lipoprotein decreased

  • Hypercholesterolaemia

  • Hyperlipidaemia

  • Hypertension

  • Hypertriglyceridaemia

  • Low density lipoprotein increased

  • Peripheral vascular disorder

  • Premature menopause

  • Type IIb hyperlipidaemia

  • Abdominal pain

  • Arthralgia

  • Asthenia

  • Back pain

  • Bronchitis

  • Chest pain

  • Constipation

  • Dermatitis

  • Diarrhoea

  • Dizziness

  • Dyspepsia

  • Flatulence

  • Gastrointestinal pain

  • Headache

  • Influenza

  • Injury

  • Musculoskeletal discomfort

  • Myalgia

  • Nausea

  • Pain in extremity

  • Pharyngitis

  • Rash

  • Rhinitis

  • Sinusitis

    • (3R,5S,6E)-7-(4-(4-Fluorophenyl)-5-(methoxymethyl)-2,6-bis(1-methylethyl)-3-pyridinyl)-3,5-dihydroxy-6-heptenoic acid (3R,5S,6E)-7-(4-(p-Fluorophenyl)-2,6-diisopropyl-5-(methoxymethyl)-3-pyridyl)-3,5-dihydroxy-6-heptenoic acid (3R,5S,6E)-7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-bis(propan-2-yl)pyridin-3-yl]-3,5-dihydroxyhept-6-enoic acid
    (3R,5S,6E)-7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-di(propan-2-yl)pyridin-3-yl]-3,5-dihydroxyhept-6-enoic acid (3R,5S,6E)-7-{4-(4-fluorophenyl)-2,6-bis(1-methylethyl)-5-[(methyloxy)methyl]pyridin-3-yl}-3,5-dihydroxyhept-6-enoic acid (3R,5S,E)-7-(4-(4-fluorophenyl)-2,6-diisopropyl-5-(methoxymethyl)pyridin-3-yl)-3,5-dihydroxyhept-6-enoic acid
    (E,3R,5S)-7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-di(propan-2-yl)pyridin-3-yl]-3,5-dihydroxyhept-6-enoic acid 145599-86-6 599C866
    6-Heptenoic acid, 7-(4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-bis(1-methylethyl)-3-pyridinyl)-3,5-dihydroxy-, (3R,5S,6E)- 6-Heptenoic acid, 7-(4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-bis(1-methylethyl)-3-pyridinyl)-3,5-dihydroxy-, (S-(R*,S*-(E)))- AB01275453-01
    AM91H2KS67 API0000459 BDBM18376
    BIDD:GT0367 BRD-K81169441-236-04-1 C07966
    CHEBI:3558 CHEBI:94755 CHEMBL1477
    CS-0105635 Cerivastatin (INN) Cerivastatin [INN:BAN]
    Cervastatin D07661 DB00439
    DTXSID9022786 GTPL2950 HMS2089B11
    HSDB 7357 HY-129458 LS-183259
    LS-187162 Q423439 SCHEMBL16346
    SCHEMBL16347 SEERZIQQUAZTOL-ANMDKAQQSA-N SR-01000763520
    SR-01000763520-3 UNII-AM91H2KS67 ZINC11330186
    [S-[R*,S*-(E)]]-7-[4-(4-fluorophenyl)-5-methoxymethyl)-2,6bis(1-methylethyl)-3-pyridinyl]-3,5-dihydroxy-6-heptenoate cerivastatin cerivastatin acid

    DrugBank Name Cerivastatin
    DrugBank DB00439
    CAS Number 143201-11-0, 145599-86-6
    PubChem Compound 446156
    KEGG Compound ID C07966
    KEGG Drug D07661
    PubChem.Substance 46505877
    ChEBI 3558
    PharmGKB PA448897
    ChemSpider 393588
    BindingDB 18376.0
    TTD DNC000403
    Wikipedia Cerivastatin
    HET 116
    DPD 11747

    1. Dykens et al. (2014)