PharmGKB: The Pharmacogenomics Knowledge Base

Drug/Small Molecule:
fenofibrate

2D structure

Overview

Generic Names: FNF; Fenofibrato [INN-Spanish]; Fenofibratum [INN-Latin]; Finofibrate
Trade Names: Ankebin; Antara; Elasterate; Elasterin; Fenobrate; Fenogal; Fenotard; Lipanthyl; Lipantil; Lipidex; Lipidil; Lipidil Micro; Lipidil Supra; Lipifen; Lipirex; Lipoclar; Lipofene; Liposit; Lipsin; Lofibra; Luxacor; Nolipax; Procetofen; Proctofene; Protolipan; Secalip; Sedufen; Tricor; Triglide
PharmGKB Accession Id: PA449594

Description

An antilipemic agent which reduces both cholesterol and triglycerides in the blood. PubChem (source: Drug Bank)

Indication

For use as adjunctive therapy to diet to reduce elevated LDL-C, Total-C,Triglycerides and Apo B, and to increase HDL-C in adult patients with primary hypercholesterolemia or mixed dyslipidemia (Fredrickson Types IIa and IIb) (source: Drug Bank)

ATC Therapeutic Category

  • C10AB:Fibrates

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Fenofibrate exerts its therapeutic effects through activation of peroxisome proliferator activated receptor a (PPARa). This increases lipolysis and elimination of triglyceride-rich particles from plasma by activating lipoprotein lipase and reducing production of apoprotein C-III. The resulting fall in triglycerides produces an alteration in the size and composition of LDL from small, dense particles, to large buoyant particles. These larger particles have a greater affinity for cholesterol receptors and are catabolized rapidly. (source: Drug Bank)

Pharmacology

Fenofibrate is a lipid regulating agent indicated as adjunctive therapy to diet to reduce elevated LDL-C, Total-C,Triglycerides and Apo B, and to increase HDL-C in adult patients with primary hypercholesterolemia or mixed dyslipidemia (Fredrickson Types IIa and IIb). Fenofibrate is also indicated as adjunctive therapy to diet for treatment of adult patients with hypertriglyceridemia (Fredrickson Types IV and V hyperlipidemia). Fenofibric acid, the active metabolite of Fenofibrate, produces reductions in total cholesterol, LDL cholesterol, apolipoprotein B, total triglycerides and triglyceride rich lipoprotein (VLDL) in treated patients. In addition, treatment with fenofibrate results in increases in high density lipoprotein (HDL) and apoproteins apoAI and apoAII. (source: Drug Bank)

Food Interactions

Increased absorption- take with meals. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Protein Binding

~99% (Serum protein binding) (source: Drug Bank)

Absorption

Fenofibrate is well absorbed from the gastrointestinal tract. After absorption, fenofibrate is mainly excreted in the urine in the form of metabolites, primarily fenofibric acid and fenofibric acid glucuronide (source: Drug Bank)

Toxicity

LD<sub>50</sub>=1600 mg/kg (Oral, in mice); Investigated as a teratogen and reproductive hazard. (source: Drug Bank)

Isomeric SMILES Code:

CC(C)OC(=O)C(C)(C)Oc1ccc(cc1)C(=O)c2ccc(cc2)Cl (source: Drug Bank)

Curated Annotations (Curated Annotation)

  1. rs320 at chr8:19863357 in LPL
    This variant is associated with triglyceride lowering response after fibrate treatment in patients with hypertriglyceridemia. Individuals with the G/G genotype had a significantly lower triglyceride lowering reponse than those with wild type.
    Variant Name:
    LPL: 483T>G
    Related Drugs:
    fenofibrate
    Related Diseases:
    Hyperlipidemias, Hypertriglyceridemia
    Evidence:
    PMID:19207029
  2. rs2727786 at chr11:116213733 in APOA1, KIAA0999
    This variant is associated with triglyceride lowering response after fibrate treatment in patients with hypertriglyceridemia. Individuals with the G/C genotype had a significantly lower triglyceride lowering reponse than those with wild type.
    Variant Name:
    APOA1: 2169G>C
    Related Drugs:
    fenofibrate
    Related Diseases:
    Hyperlipidemias, Hypertriglyceridemia
    Evidence:
    PMID:19207029
  3. rs4238001 at chr12:123914216 in SCARB1
    This variant was significantly associated with postfenofibrate change for triglycerides. Subjects bearing minor allele A tend to have higher responsiveness to fenofibrate in lowering TG. A total of 1,327 subjects (639 men and 688 women) from 148 families were genotyped. Of these 1,327 subjects, 861 subjects (427 men and 434 women) went through the fenofibrate trial and had complete lipid phenotype and genotype data.
    Variant Name:
    SCARB1: G2S
    Related Drugs:
    fenofibrate
    Evidence:
    PMID:18542840
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
No phenotype data Genotype Data Available Literature annotations available Not annotated
ABCA1
  •   
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  •   
  • FA
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
ACOX1
  •   
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  •   
  • FA
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Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
APOA1
  •   
  •   
  •   
  •   
  •   
Variants
No phenotype data No genotype data Literature annotations available Not annotated
APOE
  •   
  • PD
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  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
CYP3A
  •   
  •   
  • PK
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  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A4
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A5
  •   
  •   
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
ESRRG
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
KIAA0999
  •   
  •   
  •   
  •   
  •   
Variants
Phenotype data available No genotype data Literature annotations available Not annotated
LPL
  •   
  • PD
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  •   
  •   
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
NPC1L1
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
PPARA
  •   
  • PD
  •   
  • FA
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
SCARB1
  • CO
  •   
  •   
  • FA
  • GN
Publications, Variants

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

Drug Targets

Gene Description
PPARA 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
  •   
  •   
  • PK
  • 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 fibrate increases the anticoagulant effect (source: Drug Bank)
atorvastatin Uncurated Annotation Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
cerivastatin Uncurated Annotation Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
dicumarol Uncurated Annotation The fibrate increases the anticoagulant effect (source: Drug Bank)
fluvastatin Uncurated Annotation Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
lovastatin Uncurated Annotation Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
pravastatin Uncurated Annotation Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
rosuvastatin Uncurated Annotation Rosuvastatin possibly increases the effect of the fibrate (source: Drug Bank)
simvastatin Uncurated Annotation Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
ursodeoxycholic acid Uncurated Annotation The fibric acid derivative decreases the effect of ursodiol (source: Drug Bank)
warfarin Uncurated Annotation The fibrate 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
Cardiomyopathies
  •   
  • PD
  •   
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  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Diabetes Mellitus
  •   
  • PD
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Diabetes Mellitus, Type 2
  •   
  • PD
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Hyperlipidemias
  •   
  • PD
  •   
  •   
  •   
Publications, Variants

Non-Curated Information

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

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

  1. The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB01039
ChEBI ID:
5001
KEGG Compound ID:
C07586
KEGG Drug ID:
D00565
PubChem Compound ID:
3339
PubChem Substance ID:
180502

Common Searches

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Non-Curated Publications

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

PharmGKB integrates drug information from different sources: DrugBank, Open Eye Scientific Software.
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