Clofibrate

Summary

Clofibrate (CHEMBL565) is an approved small-molecule anticholesteremic drug (ATC C10AB01) targeting PPARA; indicated across 5 conditions including cardiovascular disorder and myocardial infarction.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C10AB01
• Targets: 1 (PPARA)
• Indications: 5 conditions
• Clinical trials: 2
• Chemistry: 242.7 Da · C12H15ClO3

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL565
Name	Clofibrate
Type	Small molecule
Max phase	4
FDA approved	no
PubChem CID	2796
ChEBI	CHEBI:3750
ATC	C10AB01
Molecular formula	C12H15ClO3
Molecular weight	242.7
InChIKey	KNHUKKLJHYUCFP-UHFFFAOYSA-N

SMILES: CCOC(=O)C(C)(C)OC1=CC=C(C=C1)Cl

IUPAC name: ethyl 2-(4-chlorophenoxy)-2-methylpropanoate

ChEBI definition: The ethyl ester of clofibric acid.

Pharmacological roles (ChEBI): anticholesteremic drug, antilipemic drug, geroprotector, PPARα agonist.

Also known as: Atromid, Atromid-s, AY-61123, Chlorfenisate, Clofibrate, Clofibrato, Ethyl p-chlorophenoxyisobutyrate, ICI 28257, ICI-28257, NSC-79389, clofibrate, SID11110971

Patent coverage: 11,744 distinct patent families (39,543 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
PPARA	Peroxisome proliferator-activated receptor-α	Agonist	4.25	0.7%	Q07869

Broader ChEMBL bioactivity targets: 13 (assay-derived). Sample: Inositol monophosphatase 1, Ferritin light chain, Peripheral myelin protein 22, Thyrotropin receptor, Beta-lactamase, Peroxisome proliferator-activated receptor alpha, 5-hydroxytryptamine receptor 2A, Peroxisome proliferator-activated receptor alpha, Muscarinic acetylcholine receptor M1, Cytochrome P450 1A2.

Bioactivity

ChEMBL activities: 12 potent at pChembl ≥ 5 of 25 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P08482	8.2	Potency	6.3	nM	CHEMBL_ACT_4807519
TSHR	5.6	Potency	2512	nM	CHEMBL_ACT_3915508
P00811	5.25	Potency	5623	nM	CHEMBL_ACT_4629265
P02692	5.22	Kd	6000	nM	CHEMBL_ACT_2690527
P02692	5.17	Kd	6700	nM	CHEMBL_ACT_2690528
P02692	5.16	Ki	6920	nM	CHEMBL_ACT_2445227
P02692	5.14	Kd	7300	nM	CHEMBL_ACT_2690529
P02692	5.11	Kd	7800	nM	CHEMBL_ACT_2690530
P02692	5.05	Kd	8900	nM	CHEMBL_ACT_2690531
P02692	5.02	Kd	9600	nM	CHEMBL_ACT_2690532
CYP3A4	5	Potency	10000	nM	CHEMBL_ACT_4985959
CYP3A4	5	Potency	10000	nM	CHEMBL_ACT_5054984

Target pathways

Aggregated over 1 target gene(s): PPARA.

Top Reactome pathways

13 total, by targets touching each:

Pathway	Targets	Genes
BMAL1:CLOCK,NPAS2 activates circadian expression	1	PPARA
PPARA activates gene expression	1	PPARA
Transcriptional activation of mitochondrial biogenesis	1	PPARA
Activation of gene expression by SREBF (SREBP)	1	PPARA
Transcriptional regulation of white adipocyte differentiation	1	PPARA
Nuclear Receptor transcription pathway	1	PPARA
Regulation of lipid metabolism by PPARalpha	1	PPARA
SUMOylation of intracellular receptors	1	PPARA
Cytoprotection by HMOX1	1	PPARA
Heme signaling	1	PPARA
Transcriptional regulation of brown and beige adipocyte differentiation by EBF2	1	PPARA
Expression of BMAL (ARNTL), CLOCK, and NPAS2	1	PPARA
RORA,B,C and NR1D1 (REV-ERBA) regulate gene expression	1	PPARA

Dominant GO biological processes

GO term	Targets
negative regulation of transcription by RNA polymerase II	1
response to hypoxia	1
gluconeogenesis	1
fatty acid metabolic process	1
heart development	1
response to nutrient	1
lactation	1
epidermis development	1
cellular response to starvation	1
hormone-mediated signaling pathway	1
gene expression	1
regulation of ketone metabolic process	1
negative regulation of macrophage derived foam cell differentiation	1
negative regulation of cholesterol storage	1
protein ubiquitination	1

Indications & clinical

Indications

5 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
cardiovascular disorder	4	MONDO:0004995	EFO:0000319
myocardial infarction	3	MONDO:0005068	EFO:0000612
myocardial ischemia	3	MONDO:0024644	EFO:1001375
coronary artery disorder	3	MONDO:0005010	EFO:0001645
heart disorder	3	MONDO:0005267	EFO:0003777

Clinical trials

Total trials: 2.

Phase distribution

Phase	Trials
PHASE3	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00000482	PHASE3	COMPLETED	Coronary Drug Project
NCT00000483	Not specified	COMPLETED	Coronary Drug Project Mortality Surveillance

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

37 molecules share ≥1 primary target. Top 37 by shared-target count:

Molecule	Source	Status	Shared targets
SELADELPAR	ChEMBL + PubChem	Phase 4 (approved)	PPARA
BERBERINE	ChEMBL	Phase 4 (approved)	PPARA
CIPROFIBRATE	ChEMBL	Phase 4 (approved)	PPARA
CYCLOSPORINE	ChEMBL	Phase 4 (approved)	PPARA
ELAFIBRANOR	ChEMBL	Phase 4 (approved)	PPARA
FENOFIBRATE	ChEMBL	Phase 4 (approved)	PPARA
FENOFIBRIC ACID	ChEMBL	Phase 4 (approved)	PPARA
GEMFIBROZIL	ChEMBL	Phase 4 (approved)	PPARA
PEMAFIBRATE	ChEMBL	Phase 4 (approved)	PPARA
PIOGLITAZONE	ChEMBL	Phase 4 (approved)	PPARA
RACECADOTRIL	ChEMBL	Phase 4 (approved)	PPARA
ROSIGLITAZONE	ChEMBL	Phase 4 (approved)	PPARA
ALEGLITAZAR	ChEMBL	Phase 3	PPARA
BEZAFIBRATE	ChEMBL	Phase 3	PPARA
GAMOLENIC ACID	ChEMBL	Phase 3	PPARA
ICOSAPENT	ChEMBL	Phase 3	PPARA
IMIGLITAZAR	ChEMBL	Phase 3	PPARA
LANIFIBRANOR	ChEMBL	Phase 3	PPARA
LOBEGLITAZONE	ChEMBL	Phase 3	PPARA
MURAGLITAZAR	ChEMBL	Phase 3	PPARA
TESAGLITAZAR	ChEMBL	Phase 3	PPARA
CLOFIBRIC ACID	ChEMBL	Phase 2	PPARA
DIHOMO-GAMMA-LINOLENIC ACID	ChEMBL	Phase 2	PPARA
FARGLITAZAR	ChEMBL	Phase 2	PPARA
GW501516	ChEMBL	Phase 2	PPARA
GW590735	ChEMBL	Phase 2	PPARA
INDEGLITAZAR	ChEMBL	Phase 2	PPARA
LINOLEIC ACID	ChEMBL	Phase 2	PPARA
LY-518674	ChEMBL	Phase 2	PPARA
NAVEGLITAZAR	ChEMBL	Phase 2	PPARA
OLEIC ACID	ChEMBL	Phase 2	PPARA
PIRINIXIC ACID	ChEMBL	Phase 2	PPARA
RAGAGLITAZAR	ChEMBL	Phase 2	PPARA
REGLITAZAR	ChEMBL	Phase 2	PPARA
URSOLIC ACID	ChEMBL	Phase 2	PPARA
Bosentan	PubChem	Approved	PPARA
regorafenib	PubChem	Approved	PPARA