Fenofibrate

Summary

Fenofibrate (CHEMBL672) is an approved small-molecule antilipemic drug (ATC C10AB05) targeting FABP1 and PPARA; indicated across 31 conditions including cardiovascular disorder and diabetes mellitus.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: C10AB05
• Targets: 2 (FABP1, PPARA)
• Indications: 31 conditions
• Clinical trials: 140
• Chemistry: 360.8 Da · C20H21ClO4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL672
Name	Fenofibrate
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	3339
ChEBI	CHEBI:5001
ATC	C10AB05
Molecular formula	C20H21ClO4
Molecular weight	360.8
InChIKey	YMTINGFKWWXKFG-UHFFFAOYSA-N

SMILES: CC(C)OC(=O)C(C)(C)OC1=CC=C(C=C1)C(=O)C2=CC=C(C=C2)Cl

IUPAC name: propan-2-yl 2-[4-(4-chlorobenzoyl)phenoxy]-2-methylpropanoate

ChEBI definition: A chlorobenzophenone that is (4-chlorophenyl)(phenyl)methanone substituted by a [2-methyl-1-oxo-1-(propan-2-yloxy)propan-2-yl]oxy group at position 1 on the phenyl ring.

Pharmacological roles (ChEBI): antilipemic drug, geroprotector.

Other ChEBI roles (chemical / environmental): environmental contaminant, xenobiotic.

Also known as: Antara, Antara (micronized), Fenofibrate, Fenofibrate (micronized), Fenofibrate delayed release, Fenofibrate micronized, Fenofibrato, Fenogal, Fenoglide, Lipantil, Lipantil micro 200, Lipantil micro 267

Patent coverage: 12,545 distinct patent families (42,568 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
FABP1	fatty acid binding protein 1	Inhibition	7.62	0%	P07148
PPARA	Peroxisome proliferator-activated receptor-α	Agonist	4.52	0.7%	Q07869

Broader ChEMBL bioactivity targets: 41 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Microtubule-associated protein tau, Ubiquitin carboxyl-terminal hydrolase 2, Nuclear receptor ROR-gamma, Survival motor neuron protein, Prelamin-A/C, RecQ-like DNA helicase BLM, 4’-phosphopantetheinyl transferase ffp, Ferritin light chain, 15-hydroxyprostaglandin dehydrogenase [NAD(+)].

Bioactivity

ChEMBL activities: 43 potent at pChembl ≥ 5 of 97 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
P02692	7.75	Kd	18	nM	CHEMBL_ACT_2690511
P02692	7.64	Kd	23	nM	CHEMBL_ACT_2690513
P02692	7.62	Ki	24	nM	CHEMBL_ACT_2445225
P02692	7.62	Kd	24	nM	CHEMBL_ACT_2690515
P02692	7.57	Kd	27	nM	CHEMBL_ACT_2690517
P02692	7.5	Kd	32	nM	CHEMBL_ACT_2690519
P02692	7.39	Kd	41	nM	CHEMBL_ACT_2690521
P02692	7.21	Kd	62	nM	CHEMBL_ACT_2690523
P08482	7.2	Potency	63.1	nM	CHEMBL_ACT_4803532
P02692	6.89	Kd	130	nM	CHEMBL_ACT_2690512
P02692	6.82	Kd	150	nM	CHEMBL_ACT_2690514
P02692	6.8	Kd	160	nM	CHEMBL_ACT_2690516
P02692	6.7	Kd	200	nM	CHEMBL_ACT_2690518
P02692	6.6	Kd	250	nM	CHEMBL_ACT_2690520
P02692	6.57	Kd	270	nM	CHEMBL_ACT_2690522
P02692	6.5	Kd	320	nM	CHEMBL_ACT_2690524
P02692	6.44	Kd	360	nM	CHEMBL_ACT_2690526
P02692	6.39	Ki	405	nM	CHEMBL_ACT_2445252
PPARG	6.24	EC50	570	nM	CHEMBL_ACT_327685
HTR2A	6.22	Ki	605	nM	CHEMBL_ACT_7646199
PPARA	6	IC50	1000	nM	CHEMBL_ACT_2649207
HTR2C	5.91	Ki	1242	nM	CHEMBL_ACT_7646203
PPARA	5.7	EC50	2000	nM	CHEMBL_ACT_2649177
HTR2A	5.67	IC50	2118	nM	CHEMBL_ACT_7646198
HTR2C	5.62	IC50	2371	nM	CHEMBL_ACT_7646202
CNR1	5.53	AC50	2929	nM	CHEMBL_ACT_25181516
PPARA	5.49	EC50	3210	nM	CHEMBL_ACT_327683
ADORA3	5.49	Ki	3222	nM	CHEMBL_ACT_7673950
TDP1	5.45	Potency	3548	nM	CHEMBL_ACT_3940711
CYP3A4	5.4	Potency	3981	nM	CHEMBL_ACT_4949246

Target pathways

Aggregated over 2 target gene(s): FABP1, PPARA.

Top Reactome pathways

15 total, by targets touching each:

Pathway	Targets	Genes
PPARA activates gene expression	2	FABP1, PPARA
Regulation of lipid metabolism by PPARalpha	2	FABP1, PPARA
Cytoprotection by HMOX1	2	FABP1, PPARA
BMAL1:CLOCK,NPAS2 activates circadian expression	1	PPARA
Triglyceride catabolism	1	FABP1
Heme degradation	1	FABP1
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
SUMOylation of intracellular receptors	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
fatty acid transport	1
cellular response to hydrogen peroxide	1
cellular response to hypoxia	1
cellular detoxification	1
cellular oxidant detoxification	1
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

Indications & clinical

Indications

31 indications (6 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
diabetes mellitus	4	MONDO:0005015	EFO:0000400
hypothyroidism	4	MONDO:0005420	EFO:0004705
type 2 diabetes mellitus	4	MONDO:0005148	MONDO:0005148
hypertriglyceridemia	3	MONDO:0005347	EFO:0004211
metabolic disease	3	MONDO:0005066	EFO:0000589
diabetic retinopathy	3	MONDO:0005266	EFO:0003770
primary biliary cholangitis	3	MONDO:0005388	EFO:1001486
hypertensive disorder	3	MONDO:0005044	EFO:0000537
atherosclerosis	3	MONDO:0005311	EFO:0003914
lipodystrophy	3	MONDO:0006573	EFO:1000727
hyperlipoproteinemia	3	MONDO:0037748	MONDO:0037748
coronary artery disorder	3	MONDO:0005010	EFO:0001645
hyperlipidemia	3	MONDO:0021187	MONDO:0021187
metabolic syndrome X	2	MONDO:0011565	EFO:0000195
HIV infectious disease	2	MONDO:0005109	EFO:0000180
plasma cell myeloma	2	MONDO:0009693	EFO:0001378
obesity disorder	2	MONDO:0011122	EFO:0001073
burn	2	MONDO:0043519	EFO:0009516
metabolic dysfunction-associated steatohepatitis	2	MONDO:0007027	EFO:1001249
diabetic kidney disease	2	MONDO:0005016	EFO:0000401
alcohol abuse	2	MONDO:0002046	MONDO:0007079
Huntington disease	2	MONDO:0007739	MONDO:0007739
inflammatory bowel disease	2	MONDO:0005265	EFO:0003767
metabolic dysfunction-associated steatotic liver disease	2	MONDO:0013209	EFO:0003095
sclerosing cholangitis	1	MONDO:0018646	EFO:0004268

5 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 140.

Phase distribution

Phase	Trials
PHASE4	31
PHASE2	31
Not specified	30
PHASE3	27
PHASE2/PHASE3	10
PHASE1	7
PHASE1/PHASE2	2
EARLY_PHASE1	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00246636	PHASE4	COMPLETED	Evaluation of Efficacy and Safety of Omacor (Omega-3-acid Ethyl Esters) as Add-on Therapy in Hypertriglyceridemic Subjects Treated With Antara (Fenofibrate) Followed by an 8-week Extension
NCT00304993	PHASE4	COMPLETED	Study of Niacin and Rosiglitazone in Dysmetabolic Dyslipidemia
NCT00385658	PHASE4	COMPLETED	Efficacy of Fluvastatin and Fenofibrate in Comparison to Simvastatin and Ezetimibe in Patients With Metabolic Syndrome
NCT00552747	PHASE4	COMPLETED	Effect of Fenofibrate on Endothelial Function and High-density Lipoproteins (HDL)in Patients With Coronary Heart Disease
NCT00632840	PHASE4	COMPLETED	Pharmacological Regulation of Fat Transport in Metabolic Syndrome
NCT00745407	PHASE4	COMPLETED	Effects of Fenofibrate on Adipocytokine Levels In Hypertriglyceridemic Patients
NCT00754039	PHASE4	COMPLETED	Study to Compare Welchol and TriCor to TriCor Alone in Patients With High Cholesterol
NCT00809068	PHASE4	COMPLETED	High-density Lipoprotein (HDL) Cholesterol in Women Taking Tibolone
NCT00819910	PHASE4	TERMINATED	Rosiglitazone And Fenofibrate Additive Effects on Lipids (RAFAEL)
NCT00843661	PHASE4	UNKNOWN	Coadministration of Ezetimibe With Fenofibrate Versus Pravastatin Monotherapy for the Treatment of Hyperlipidaemia in HIV-infected Patients
NCT00872599	PHASE4	COMPLETED	The Effect of a Peroxisome Proliferator-activated Receptor (PPAR) Alpha Agonist on Cytochrome P450 (CYP) Monooxygenase Activity in Humans
NCT00923676	PHASE4	UNKNOWN	Treatment of Hyperlipidemia and Sexual Dysfunction
NCT01003847	PHASE4	COMPLETED	Differential Metabolic Effects of Fenofibrate and Fatty Acid
NCT01462877	PHASE4	COMPLETED	A Study to Evaluate Fenofibrate Combination With Statin in Chinese Patients With Dyslipidemic
NCT01574131	PHASE4	TERMINATED	Acute and Long-Term Outcome Investigations of Fenofibrate on Severely Burned Patients
NCT01666041	PHASE4	COMPLETED	Vascular and Metabolic Effects of Fenofibrate/Omega vs Fenofibrate
NCT01927315	PHASE4	COMPLETED	Effects of Fenofibrate on Endothelial Progenitor Cells in Diabetes
NCT02015988	PHASE4	UNKNOWN	Simvastatin and Fenofibrate vs Simvastatin Alone in Patients With Type 2 Diabetes Mellitus and Acute Coronary Syndrome
NCT02153879	PHASE4	COMPLETED	Characterization of High Density Lipoprotein (HDL) in Type 2 Diabetes (T2D) After Fenofibrate or Niacin Treatment
NCT02232360	PHASE4	UNKNOWN	Effects of Combined Therapy With Statin Plus Fenofibrate on Coronary Atherosclerotic Plaque Compared With Statin Alone
NCT02314533	PHASE4	UNKNOWN	Evaluate the Efficacy of Fenofibrate on Microalbuminuria
NCT02642159	PHASE4	COMPLETED	Efficacy and Safety of Alirocumab Versus Usual Care on Top of Maximally Tolerated Statin Therapy in Patients With Type 2 Diabetes and Mixed Dyslipidemia (ODYSSEY DM-Dyslipidemia)
NCT02886299	PHASE4	COMPLETED	Randomized Comparative Efficacy and Safety Study of Intermittent Simvastatin and Fenofibrate in Hemodialysis
NCT02984982	PHASE4	COMPLETED	Evaluation of Effect of Alirocumab on Coronary Atheroma Volume in Japanese Patients Hospitalized for Acute Coronary Syndrome With Hypercholesterolemia
NCT03439345	PHASE4	COMPLETED	Lowering Events in Non-proliferative Retinopathy in Scotland
NCT03615534	PHASE4	COMPLETED	Extended Release Niacin and Fenofibrate for the Treatment of Atherogenic Dyslipidemia in Obese Females
NCT03829514	PHASE4	COMPLETED	Fenofibrate in Type 2 Diabetes
NCT03874260	PHASE4	UNKNOWN	Cinical Trial to Explore the Efficacy of Statin/Choline Fenofibrate Combination Therapy vs Statin Monotherapy in Patients With Inadequately Controlled TG Despite Receiving Statin Monotherapy
NCT04140201	PHASE4	UNKNOWN	Effect of Lipid Lowering Agents on Diabetic Retinopathy and Cardiovascular Risk of Diabetic Patients
NCT05498090	PHASE4	UNKNOWN	Interrogating Fatty Acid Metabolism Impairment and Clinical Correlates in Males with Klinefelter Syndrome
NCT06451900	PHASE4	COMPLETED	Role of Fenofibrate in Neonatal Jaundice
NCT01320345	PHASE3	ACTIVE_NOT_RECRUITING	The Fenofibrate And Microvascular Events in Type 1 Diabetes Eye.
NCT04661358	PHASE3	RECRUITING	Fenofibrate for Prevention of DR Worsening
NCT05749822	PHASE2/PHASE3	RECRUITING	Fenofibrate for Compensated Cirrhosis Patients With Primary Biliary Cholangitis
NCT06174402	PHASE2/PHASE3	ACTIVE_NOT_RECRUITING	Fenofibrate in Combination With Ursodeoxycholic Acid in Primary Biliary Cholangitis
NCT06365424	PHASE2/PHASE3	RECRUITING	Fenofibrate in Patients With Primary Biliary Cholangitis (PBC)
NCT06755151	PHASE3	RECRUITING	Fenofibrate in Primary Biliary Cholangitis: a Real World Study
NCT07296458	PHASE3	RECRUITING	FIREFLY Trial: Fenofibrate Intervention—Randomized Evaluation in First-Line PBC Therapy
NCT00006412	PHASE3	COMPLETED	Safety and Effectiveness of Fenofibrate and Pravastatin in HIV-Positive Patients With Abnormal Blood Lipids
NCT00139061	PHASE3	COMPLETED	Assess HDL-C Increase And Non-HDL Lowering Effect Of Torcetrapib/Atorvastatin Vs. Fenofibrate

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 17 clinical and 51 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

38 molecules share ≥1 primary target. Top 38 by shared-target count:

Molecule	Source	Status	Shared targets
Fenofibric Acid	ChEMBL + PubChem	Phase 4 (approved)	FABP1, PPARA
OLEIC ACID	ChEMBL	Phase 2	FABP1, PPARA
SELADELPAR	ChEMBL + PubChem	Phase 4 (approved)	PPARA
BERBERINE	ChEMBL	Phase 4 (approved)	PPARA
CIPROFIBRATE	ChEMBL	Phase 4 (approved)	PPARA
CLOFIBRATE	ChEMBL	Phase 4 (approved)	PPARA
CYCLOSPORINE	ChEMBL	Phase 4 (approved)	PPARA
ELAFIBRANOR	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
TACRINE	ChEMBL	Phase 4 (approved)	FABP1
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
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