Details
Stereochemistry | ACHIRAL |
Molecular Formula | C17H15ClO4 |
Molecular Weight | 318.752 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)(OC1=CC=C(C=C1)C(=O)C2=CC=C(Cl)C=C2)C(O)=O
InChI
InChIKey=MQOBSOSZFYZQOK-UHFFFAOYSA-N
InChI=1S/C17H15ClO4/c1-17(2,16(20)21)22-14-9-5-12(6-10-14)15(19)11-3-7-13(18)8-4-11/h3-10H,1-2H3,(H,20,21)
Molecular Formula | C17H15ClO4 |
Molecular Weight | 318.752 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL239 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17343371 |
4500.0 nM [EC50] | ||
Target ID: CHEMBL4879 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18533710 |
1000.0 µM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | FIBRICOR Approved UseFIBRICOR is a peroxisome proliferator receptor alpha (PPARα) activator
indicated as an adjunct to diet: to reduce triglyceride (TG) levels in adult patients with severe
hypertriglyceridemia (> 500 mg/dL); to reduce elevated total cholesterol (TC), low-density-lipoprotein cholesterol (LDL-C), TG and apolipoprotein (Apo) B and to increase high-density lipoprotein cholesterol (HDL-C) in adult patients with primary hypercholesterolemia or mixed dyslipidemia. Launch Date1.25020799E12 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
8.37 μg/mL |
105 mg 1 times / day steady-state, oral dose: 105 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
FENOFIBRIC ACID unknown | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: FED |
|
12 μg/mL |
105 mg 1 times / day steady-state, oral dose: 105 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
FENOFIBRIC ACID unknown | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
124 μg × h/mL |
105 mg 1 times / day steady-state, oral dose: 105 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
FENOFIBRIC ACID unknown | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: FED |
|
162.96 μg × h/mL |
105 mg 1 times / day steady-state, oral dose: 105 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
FENOFIBRIC ACID unknown | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1% |
105 mg 1 times / day steady-state, oral dose: 105 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
FENOFIBRIC ACID unknown | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
135 mg 1 times / day multiple, oral Recommended Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, adult n = 490 Health Status: unhealthy Age Group: adult Population Size: 490 Sources: |
Other AEs: Constipation, Diarrhea... Other AEs: Constipation (3.3%) Sources: Diarrhea (3.9%) Dyspepsia (3.7%) Nausea (4.3%) Fatigue (2%) Pain (3.5%) Nasopharyngitis (3.5%) Sinusitis (3.3%) Upper respiratory tract infection (5.3%) ALT increased (1.2%) Arthralgia (3.9%) Back pain (6.3%) Muscle spasms (1.6%) Myalgia (3.3%) Pain in extremity (4.5%) Dizziness (4.1%) Headache (12.7%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
ALT increased | 1.2% | 135 mg 1 times / day multiple, oral Recommended Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, adult n = 490 Health Status: unhealthy Age Group: adult Population Size: 490 Sources: |
Muscle spasms | 1.6% | 135 mg 1 times / day multiple, oral Recommended Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, adult n = 490 Health Status: unhealthy Age Group: adult Population Size: 490 Sources: |
Headache | 12.7% | 135 mg 1 times / day multiple, oral Recommended Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, adult n = 490 Health Status: unhealthy Age Group: adult Population Size: 490 Sources: |
Fatigue | 2% | 135 mg 1 times / day multiple, oral Recommended Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, adult n = 490 Health Status: unhealthy Age Group: adult Population Size: 490 Sources: |
Constipation | 3.3% | 135 mg 1 times / day multiple, oral Recommended Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, adult n = 490 Health Status: unhealthy Age Group: adult Population Size: 490 Sources: |
Myalgia | 3.3% | 135 mg 1 times / day multiple, oral Recommended Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, adult n = 490 Health Status: unhealthy Age Group: adult Population Size: 490 Sources: |
Sinusitis | 3.3% | 135 mg 1 times / day multiple, oral Recommended Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, adult n = 490 Health Status: unhealthy Age Group: adult Population Size: 490 Sources: |
Nasopharyngitis | 3.5% | 135 mg 1 times / day multiple, oral Recommended Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, adult n = 490 Health Status: unhealthy Age Group: adult Population Size: 490 Sources: |
Pain | 3.5% | 135 mg 1 times / day multiple, oral Recommended Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, adult n = 490 Health Status: unhealthy Age Group: adult Population Size: 490 Sources: |
Dyspepsia | 3.7% | 135 mg 1 times / day multiple, oral Recommended Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, adult n = 490 Health Status: unhealthy Age Group: adult Population Size: 490 Sources: |
Arthralgia | 3.9% | 135 mg 1 times / day multiple, oral Recommended Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, adult n = 490 Health Status: unhealthy Age Group: adult Population Size: 490 Sources: |
Diarrhea | 3.9% | 135 mg 1 times / day multiple, oral Recommended Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, adult n = 490 Health Status: unhealthy Age Group: adult Population Size: 490 Sources: |
Dizziness | 4.1% | 135 mg 1 times / day multiple, oral Recommended Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, adult n = 490 Health Status: unhealthy Age Group: adult Population Size: 490 Sources: |
Nausea | 4.3% | 135 mg 1 times / day multiple, oral Recommended Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, adult n = 490 Health Status: unhealthy Age Group: adult Population Size: 490 Sources: |
Pain in extremity | 4.5% | 135 mg 1 times / day multiple, oral Recommended Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, adult n = 490 Health Status: unhealthy Age Group: adult Population Size: 490 Sources: |
Upper respiratory tract infection | 5.3% | 135 mg 1 times / day multiple, oral Recommended Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, adult n = 490 Health Status: unhealthy Age Group: adult Population Size: 490 Sources: |
Back pain | 6.3% | 135 mg 1 times / day multiple, oral Recommended Dose: 135 mg, 1 times / day Route: oral Route: multiple Dose: 135 mg, 1 times / day Sources: |
unhealthy, adult n = 490 Health Status: unhealthy Age Group: adult Population Size: 490 Sources: |
Overview
OverviewOther
Drug as perpetrator
Drug as victim
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PubMed
Title | Date | PubMed |
---|---|---|
Statin-induced inhibition of the Rho-signaling pathway activates PPARalpha and induces HDL apoA-I. | 2001 Jun |
|
PPARalpha and PPARdelta activators inhibit cytokine-induced nuclear translocation of NF-kappaB and expression of VCAM-1 in EAhy926 endothelial cells. | 2002 Jan 25 |
|
Induction of plasminogen activator inhibitor-1 in endothelial cells by basic fibroblast growth factor and its modulation by fibric acid. | 2002 May 1 |
|
Dilazep and fenofibric acid inhibit MCP-1 mRNA expression in glycoxidized LDL-stimulated human endothelial cells. | 2003 Aug 15 |
|
Identification of hepatic transcriptional changes in insulin-resistant rats treated with peroxisome proliferator activated receptor-alpha agonists. | 2003 Jun |
|
Influence of lipid lowering fibrates on P-glycoprotein activity in vitro. | 2004 Jan 15 |
|
Fenofibrate and fenofibric acid analysis by capillary electrophoresis. | 2004 Jun |
|
A new fenofibrate formulation: results of six single-dose, clinical studies of bioavailability under fed and fasting conditions. | 2004 Sep |
|
Optimal lipid modification: the rationale for combination therapy. | 2005 |
|
Gene expression profiling of potential peroxisome proliferator-activated receptor (PPAR) target genes in human hepatoblastoma cell lines inducibly expressing different PPAR isoforms. | 2005 Oct 3 |
|
Bezafibrate increases very-long-chain acyl-CoA dehydrogenase protein and mRNA expression in deficient fibroblasts and is a potential therapy for fatty acid oxidation disorders. | 2005 Sep 15 |
|
Simultaneous determination of rosuvastatin and fenofibric acid in human plasma by LC-MS/MS with electrospray ionization: assay development, validation and application to a clinical study. | 2005 Sep 15 |
|
The effects of food on the bioavailability of fenofibrate administered orally in healthy volunteers via sustained-release capsule. | 2006 |
|
Rapid broad-spectrum analgesia through activation of peroxisome proliferator-activated receptor-alpha. | 2006 Dec |
|
Effects of fenofibrate on C-reactive protein levels in hypertriglyceridemic patients. | 2006 Jun |
|
Evaluation of the potential for pharmacokinetic interaction between fenofibrate and ezetimibe: A phase I, open-label, multiple-dose, three-period crossover study in healthy subjects. | 2006 Mar |
|
Transport of the dipeptidyl peptidase-4 inhibitor sitagliptin by human organic anion transporter 3, organic anion transporting polypeptide 4C1, and multidrug resistance P-glycoprotein. | 2007 May |
|
Cryptochrome and Period Proteins Are Regulated by the CLOCK/BMAL1 Gene: Crosstalk between the PPARs/RXRalpha-Regulated and CLOCK/BMAL1-Regulated Systems. | 2008 |
|
PPARalpha regulates the hepatotoxic biomarker alanine aminotransferase (ALT1) gene expression in human hepatocytes. | 2008 Aug 15 |
|
A novel PPARalpha agonist ameliorates insulin resistance in dogs fed a high-fat diet. | 2008 May |
|
An automated method for the simultaneous determination of pravastatin, 3-hydroxy isomeric metabolite, pravalactone and fenofibric acid in human plasma by sensitive liquid chromatography combined with diode array and tandem mass spectrometry detection. | 2008 May 2 |
|
Fenofibrate set to benefit from new research on its active metabolite, fenofibric acid. | 2008 May-Jun |
|
Treatment of hyperlipidaemia with fenofibrate and related fibrates. | 2008 Oct |
|
Advances in the medical treatment of diabetic retinopathy. | 2009 Aug |
|
Capecitabine-induced severe hypertriglyceridaemia and diabetes: a case report and review of the literature. | 2009 Dec |
|
Differentiated CaCo-2 cells as an in-vitro model to evaluate de-novo apolipoprotein A-I production in the small intestine. | 2009 Jun |
|
IVIVC in oral absorption for fenofibrate immediate release tablets using a dissolution/permeation system. | 2009 Jun |
|
Efficacy and safety of ABT-335 (fenofibric acid) in combination with rosuvastatin in patients with mixed dyslipidemia: a phase 3 study. | 2009 May |
|
Selective modulation of amyloid-beta peptide degradation by flurbiprofen, fenofibrate, and related compounds regulates Abeta levels. | 2009 Nov |
|
Determination of fenofibric acid in human plasma by ultra performance liquid chromatography-electrospray ionization mass spectrometry: application to a bioequivalence study. | 2009 Sep |
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 16 20:29:48 UTC 2022
by
admin
on
Fri Dec 16 20:29:48 UTC 2022
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Record UNII |
BGF9MN2HU1
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Record Status |
Validated (UNII)
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Record Version |
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-
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NDF-RT |
N0000175596
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NCI_THESAURUS |
C98150
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24852
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BGF9MN2HU1
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DTXSID8041030
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64929
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SUB34521
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42017-89-0
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Fenofibric acid
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1269436
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83469
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BGF9MN2HU1
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M5279
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CHEMBL981
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C83804
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C006012
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DB13873
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255-626-9
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Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT |
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TRANSPORTER -> INHIBITOR |
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TRANSPORTER -> INHIBITOR |
Related Record | Type | Details | ||
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PRODRUG -> METABOLITE ACTIVE |
MAJOR
PLASMA; URINE
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METABOLITE -> PARENT |
MINOR
URINE
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METABOLITE -> PARENT |
MAJOR
URINE
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METABOLITE -> PARENT |
MINOR
URINE
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Related Record | Type | Details | ||
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PARENT -> IMPURITY |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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