PharmGKB: The Pharmacogenomics Knowledge Base

Drug/Small Molecule:
lovastatin

2D structure

Overview

Generic Names: 6 alpha-Methylcompactin; Lovastatina [Spanish]; Lovastatine [French]; Lovastatinum [Latin]; lovastatin
Trade Names: Altocor; Altoprev; Artein; Belvas; Cholestra; Closterol; Colevix; Hipolip; Hipovastin; Lestatin; Lipdip; Lipivas; Lipofren; Lovalip; Lovalord; Lovasterol; Lovastin; Lozutin; Mevacor; Mevinacor; Mevlor; Monacolin K; Nergadan; Paschol; Rodatin; Rovacor; Sivlor; Taucor; Tecnolip; Teroltrat
PharmGKB Accession Id: PA450272

Description

A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (hydroxymethylglutaryl COA reductases), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver. PubChem (source: Drug Bank)

Indication

For management as an adjunct to diet to reduce elevated total-C, LDL-C, apo B, and TG levels in patients with primary hypercholesterolemia and mixed dyslipidemia; For primary prevention of coronary heart disease (source: Drug Bank)

ATC Therapeutic Category

  • C10AA:HMG CoA reductase inhibitors

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Lovastatin is a lactone that is readily hydrolyzed in vivo to the corresponding b-hydroxyacid, a potent inhibitor of HMG-CoA reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate. The conversion of HMG-CoA to mevalonate is an early step in the biosynthetic pathway for cholesterol. (source: Drug Bank)

Pharmacology

Lovastatin, an antilipemic agent produced by fermentation of <i>Aspergillus terreus</i>, is the first of a class of lipid-lowering agents known as the HMG-CoA reductase inhibitors. Lovastatin is used to treat hypercholesterolemia, to slow coronary atherosclerosis, and to prevent myocardial infarction and stroke. Lovastatin, like simvastin and unlike pravastatin, is a prodrug, concentrating active drug in the liver during first-pass circulation. (source: Drug Bank)

Food Interactions

Avoid alcohol.
Avoid drastic changes in dietary habit.
Avoid taking with grapefruit juice.
Take with food, 50% increase in bioavailability when taken with food. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

hepatic (source: Drug Bank)

Protein Binding

>95% (source: Drug Bank)

Absorption

30% (source: Drug Bank)

Toxicity

LD<sub>50</sub>>1000 mg/kg (orally in mice) (source: Drug Bank)

Isomeric SMILES Code:

CC[C@H](C)C(=O)O[C@H]1C[C@H](C=C2[C@H]1[C@H]([C@H](C=C2)C)CC[C@@H]3C[C@H](CC(=O)O3)O)C (source: Drug Bank)

Curated Annotations (Curated Annotation)

  1. rs5443 at chr12:6825136 in GNB3, USP5
    This variant is associated with statin response. Patients carring T allele have less risk of MI and are more likely to benefit from statin therapy in a hypercholesterolemic population of antihypertensive drug users.
    Variant Name:
    GNB3:825C>T; GNB3:Ser275Ser
    Related Drugs:
    atorvastatin, fluvastatin, hmg coa reductase inhibitors, lovastatin, pravastatin, rosuvastatin, simvastatin
    Related Diseases:
    Hypercholesterolemia
    Evidence:
    PMID:18551043
Variant names are different names that have been used in the literature and other resources to refer to the same variant.

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
ABCB1
  •   
  • PD
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
ABCG8
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
APOA5
  •   
  •   
  •   
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2C19
  •   
  •   
  • PK
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
CYP2C8
  •   
  • PD
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2C9
  •   
  • PD
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
CYP3A
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A4
  • CO
  • PD
  • PK
  • FA
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A5
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
GNB3
  •   
  •   
  •   
  •   
  •   
Variants
No phenotype data Genotype Data Available Literature annotations available Has annotations
HMGCR
  • CO
  •   
  •   
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
KCNH2
  •   
  • PD
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
NOS2
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
NR1I2
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data Genotype Data Available Literature annotations available Has annotations
SLCO1B1
  • CO
  • PD
  • PK
  • FA
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
SREBF1
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data Genotype Data Available No literature annotations Not annotated
USP5
  •   
  •   
  •   
  •   
  •   
Variants

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
HMGCR Uncurated Annotation (source: Drug Bank)

The following drugs are in curated knowledge about this drug.

  Drug Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
ezetimibe
  •   
  • PD
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
warfarin
  •   
  •   
  •   
  •   
  •   
Publications

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
acenocoumarol Uncurated Annotation The statin increases the anticoagulant effect (source: Drug Bank)
amprenavir Uncurated Annotation Amprenavir can possibly increase the statin toxicity (source: Drug Bank)
atazanavir Uncurated Annotation Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
azithromycin Uncurated Annotation Azithromycin can possibly increase the statin toxicity (source: Drug Bank)
bezafibrate Uncurated Annotation Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
bosentan Uncurated Annotation Bosentan could decrease the statin effect (source: Drug Bank)
carbamazepine Uncurated Annotation Carbamazepine decreases the effect of the statin (source: Drug Bank)
clarithromycin Uncurated Annotation The macrolide possibly increases the statin toxicity (source: Drug Bank)
colchicine Uncurated Annotation Increased risk of rhabdomyolysis with this combination (source: Drug Bank)
cyclosporine Uncurated Annotation Possible myopathy and rhabdomyolysis (source: Drug Bank)
delavirdine Uncurated Annotation The NNRT inhibitor increases the effect and toxicity of the statin (source: Drug Bank)
dicumarol Uncurated Annotation The statin increases the anticoagulant effect (source: Drug Bank)
diltiazem Uncurated Annotation Diltiazem increases the effect and toxicity of the statin (source: Drug Bank)
efavirenz Uncurated Annotation The NNRT inhibitor increases the effect and toxicity of the statin (source: Drug Bank)
erythromycin Uncurated Annotation The macrolide possibly increases the statin toxicity (source: Drug Bank)
fenofibrate Uncurated Annotation Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
fluconazole Uncurated Annotation Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
fosamprenavir Uncurated Annotation Amprenavir can possibly increase the statin toxicity (source: Drug Bank)
gemfibrozil Uncurated Annotation Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
imatinib Uncurated Annotation Imatinib increases the effect and toxicity of statin (source: Drug Bank)
itraconazole Uncurated Annotation Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
ketoconazole Uncurated Annotation Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
nefazodone Uncurated Annotation Nefazodone increases the effect and toxicity of the statin (source: Drug Bank)
nelfinavir Uncurated Annotation Nelfinavir increases the effect and toxicity of the statin (source: Drug Bank)
nevirapine Uncurated Annotation The NNRT inhibitor increases the effect and toxicity of the statin (source: Drug Bank)
niacin Uncurated Annotation Risk of severe myopathy/rhabdomyolysis with this combination (source: Drug Bank)
rifabutin Uncurated Annotation The rifamycin decreases the effect of statin drug (source: Drug Bank)
rifampin Uncurated Annotation The rifamycin decreases the effect of statin drug (source: Drug Bank)
ritonavir Uncurated Annotation Ritonavir increases the effect and toxicity of the statin (source: Drug Bank)
tacrolimus Uncurated Annotation Tacrolimus increases the effect and toxicity of the statin (source: Drug Bank)
telithromycin Uncurated Annotation Telithromycin may possibly increase statin toxicity (source: Drug Bank)
verapamil Uncurated Annotation Verapamil increases the effect and toxicity of statin (source: Drug Bank)
warfarin Uncurated Annotation The statin increases the anticoagulant effect (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Carotid Artery Diseases
  •   
  • PD
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Drug Toxicity
  • CO
  • PD
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Hypercholesterolemia
  • CO
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Myalgia unspecified
  • CO
  • PD
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Rhabdomyolysis
  • CO
  • PD
  • PK
  •   
  • GN
Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00227
KEGG Compound ID:
C07074
KEGG Drug ID:
D00359
PubChem Compound ID:
53232
PubChem Substance ID:
191104

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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