General
Preferred name
FENOFIBRIC ACID
Synonyms
Trilipix ()
FNF acid ()
NSC 281318 ()
ABT-335 ()
choline fenofibrate ()
NSC 281318, Trilipix, FNF acid ()
Supralip ()
LF-153 ()
Fibricor ()
Lofibra ()
Fenofibrate free acid ()
Procetofenic acid ()
NSC-281318 ()
Fenocor-67 ()
Lipanthyl ()
Fenofibrate related compound b ()
Fenofibric acid ()
Fenofibric acid choline salt ()
Fenofibrate de choline ()
Fenofibrato de colina ()
P&D ID
PD001159
CAS
856676-23-8
42017-89-0
Tags
available
drug
Approved by
FDA
First approval
2008
Drug indication
Disorder of lipid metabolism
Cardiovascular disease
Medulloblastoma
Drug Status
approved
Max Phase
4.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PHARMACODYNAMICS
Various clinical studies have shown that elevated levels of total cholesterol, low-desnsity-lipoprotein (LDL-C), and apolipoprotein B (apo B) - an LDL membrane complex - are associated with human atherosclerosis [FDA Label]. Concurrently, decreased levels of high-density-lioprotein (HDL-C) and its transport complex, apolipoproteins apo AI and apo AII, are associated with the development of atherosclerosis [FDA Label]. Furthermore, epidemiological investigations demonstrate that cardiovascular morbidity and mortality vary directly with the levels of total cholesterol, LDL-C, and triglycerides, and inversely with the level of HDL-C [FDA Label].; ; Fenofibric acid, the active metabolite of fenofibrate, subsequently produces reductions in total cholesterol, LDL-C, apo B, total triglycerides, and triglyceride rich lipoprotein (VLDL) in treated patients [FDA Label]. Moreover, such treatment with fenofibrate also results in increases in HDL-C and apo AI and apo AII [FDA Label].
MOA
Having performed clinical studies with in vivo transgenic mice and in vitro human hepatocyte cultures, it is believed that the principal mechanism of action of fenofibric acid is demonstrated through its capability to activate peroxisome proliferator receptor alpha (PPAR-alpha) [FDA Label].; ; By activating PPAR-alpha, fenofibric acid increases lipolysis and the elimination of triglyceride-rich particles from plasma by actuating lipoprotein lipase and reducing production of apoprotein C-III, which acts as an inhibitor of lipoprotein lipase activity [FDA Label]. The resultant decrease in triglycerides causes an alteration in the size and composition of low-density-lipoprotein from small, dense particles to large, buoyant ones [FDA Label]. The size of these larger low-density-lipoprotein particles have a greater affinity for cholesterol receptors and are therefore catabolized more rapidly [FDA Label]. Additionally, fenofibric acid's activation of PPAR-alpha also induces an increase in the synthesis of apoproteins apo A-I, apo A-II, and high-density-lipoprotein [FDA Label].; ; Moreover, the use of fenofibric acid can also act to reduce serum uric acid levels in ordinary or hyperuricemic individuals by increasing the urinary excretion of uric acid [FDA Label].
METABOLISM
In vitro and in vivo metabolism studies reveal that fenofibric acid does not experience significant oxidative metabolism via the cytochrome P450 isoenzymes [FDA Label]. The CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4 enzymes are not known to play a role in the metabolism of fenofibric acid [FDA Label].; ; Rather, fenofibric acid is predominantly conjugated with glucuronic acid and then excreted in urine [FDA Label]. A small amount of fenofibric acid is reduced at the carbonyl moiety to benzhydrol metabolite which is, in turn, conjugated with glucuronic acid and excreted in urine [FDA Label].
DESCRIPTION
Fenofibric acid is the active metabolite of the approved drug .
(GtoPdb)
DESCRIPTION
Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 ¦ÌM, 1.47 ¦ÌM, and 1.06 ¦ÌM for PPAR¦Á, PPAR¦Ã and PPAR¦Ä, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
PRICE
29
DESCRIPTION
Choline Fenofibrate (ABT-335), a choline salt of Fenofibric acid (HY-B0760), releases free Fenofibric acid in the gastrointestinal tract. Fenofibric acid is a PPAR activator with antihyperlipidemic effect[1].
PRICE
42
DESCRIPTION
Fenofibric acid (FNF acid) is the active form of fenofibrate, a synthetic phenoxy-isobutyric acid derivate with antihyperlipidemic activity.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Choline Fenofibrate (Trilipix) is a choline formulation of fenofibrate, a synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic activity.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
0
Compound Sets
25
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
NCATS Inxight Approved Drugs
ReFrame library
Selleckchem Bioactive Compound Library
The Spectrum Collection
ZINC Tool Compounds
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
54
Molecular Weight
318.07
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
1
Rotatable Bonds
5
Ring Count
2
Aromatic Ring Count
2
cLogP
3.81
TPSA
63.6
Fraction CSP3
0.18
Chiral centers
0.0
Largest ring
6.0
QED
0.85
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
COX
COX-2
MMP
PPAR
PPARα
p450
CLCN1, PPARA
MOA
P450
Cytochrome P450 inhibitor
Indication
dyslipidemia
Pathway
DNA Damage/DNA Repair
Immunology/Inflammation
Metabolism
Neuroscience
Proteases/Proteasome
Cell Cycle/DNA Damage
Metabolic Enzyme/Protease
Vitamin D Related/Nuclear Receptor
Source data

