Icosapent Ethyl

Summary

Icosapent Ethyl (CHEMBL2095209) is an approved small-molecule anticholesteremic drug; indicated across 13 conditions including hypertriglyceridemia and pancreatitis.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Indications: 13 conditions
• Clinical trials: 15
• Chemistry: 330.5 Da · C22H34O2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2095209
Name	Icosapent Ethyl
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	9831415
ChEBI	CHEBI:84883
Molecular formula	C22H34O2
Molecular weight	330.5
InChIKey	SSQPWTVBQMWLSZ-AAQCHOMXSA-N

SMILES: CC/C=C\C/C=C\C/C=C\C/C=C\C/C=C\CCCC(=O)OCC

IUPAC name: ethyl (5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenoate

ChEBI definition: A long-chain fatty acid ethyl ester resulting from the formal condensation of the carboxy group of (5Z,8Z,11Z,14Z,17Z)-icosapentaenoic acid with the hydroxy group of ethanol.

Pharmacological roles (ChEBI): anticholesteremic drug, antipsychotic agent, antidepressant, prodrug.

Other ChEBI roles (chemical / environmental): marine metabolite.

Also known as: AMR 101, AMR-101, AMR101, Eicosapentaenoic acid ethyl ester, Epadel, Ethyl icosapent, Ethyl icosapentate, Icosapent ethyl, Icosapent ethyl ester, NSC-759597, Timnodonic acid ethyl ester, Vascepa

Patent coverage: 489 distinct patent families (1,541 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

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Progesterone receptor, Prostaglandin G/H synthase 2, Adenosine receptor A3, 3’,5’-cyclic-AMP phosphodiesterase 4D, Androgen receptor, Nuclear receptor subfamily 1 group I member 2, Prostaglandin G/H synthase 1.

Bioactivity

ChEMBL activities: 5 potent at pChembl ≥ 5 of 8 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
Q63921	5.62	AC50	2400	nM	CHEMBL_ACT_25174677
NR1I2	5.52	AC50	3000	nM	CHEMBL_ACT_25223916
PGR	5.46	AC50	3500	nM	CHEMBL_ACT_25222342
NR1I2	5.38	AC50	4200	nM	CHEMBL_ACT_25188380
PTGS2	5.04	AC50	9100	nM	CHEMBL_ACT_25166467

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

13 indications (3 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
hypertriglyceridemia	4	MONDO:0005347	EFO:0004211
pancreatitis	4	MONDO:0004982	EFO:0000278
cardiovascular disorder	3	MONDO:0004995	EFO:0000319
severe acute respiratory syndrome	3	MONDO:0005091	MONDO:0100096
colorectal adenoma	2	MONDO:0005484	EFO:0005406
metabolic dysfunction-associated steatohepatitis	2	MONDO:0007027	EFO:1001249
colonic neoplasm	2	MONDO:0005401	MONDO:0021063
Alzheimer disease	2	MONDO:0004975	MONDO:0004975
metabolic dysfunction-associated steatotic liver disease	2	MONDO:0013209	EFO:0003095
breast carcinoma	1	MONDO:0004989	EFO:0000305
breast neoplasm	1	MONDO:0021100	MONDO:0007254

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

Clinical trials

Total trials: 15.

Phase distribution

Phase	Trials
PHASE4	5
PHASE3	4
PHASE2	4
PHASE1/PHASE2	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00692718	PHASE4	UNKNOWN	N-3 Fatty Acids for the Prevention of Atrial Fibrillation in Patients With Acute Heart Failure
NCT00839449	PHASE4	COMPLETED	Eicosapentaenoic Acid Cerebral Vasospasm Therapy Study
NCT02926027	PHASE4	COMPLETED	Effect of Vascepa on Improving Coronary Atherosclerosis in People With High Triglycerides Taking Statin Therapy
NCT04505098	PHASE4	TERMINATED	A Pragmatic Randomized Trial of Icosapent Ethyl for High-Cardiovascular Risk Adults
NCT06280976	PHASE4	WITHDRAWN	Aggressive Risk-Prevention Therapies for Coronary Atherosclerotic Plaque (ART-CAP)
NCT03428477	PHASE3	ACTIVE_NOT_RECRUITING	EPA for Metastasis Trial 2
NCT01492361	PHASE3	COMPLETED	A Study of AMR101 to Evaluate Its Ability to Reduce Cardiovascular Events in High-Risk Patients With Hypertriglyceridemia and on Statin
NCT02422446	PHASE3	TERMINATED	Effects of Eicosapentaenoic Acid on Endothelial Function in Diabetic Subjects
NCT04239950	PHASE3	COMPLETED	Efficacy of Ethyl Icosapentate in Patients With Severe Hypertriglyceridemia
NCT06466278	PHASE2	ACTIVE_NOT_RECRUITING	IcoSApent ethyL to Slow Down Aortic VAlve Stenosis proGrEssion
NCT02940223	PHASE2	TERMINATED	Ethyl Icosapentate and Physical Activity in Treating Fatigue in Patients With Advanced Cancer
NCT04177680	PHASE2	COMPLETED	Pharmacodynamic Effects of a Free-Fatty Acid Formulation of Omega-3 Pentaenoic Acid in Adults With Hypertriglyceridemia
NCT04216251	PHASE1/PHASE2	COMPLETED	PRevention Using EPA Against coloREctal Cancer
NCT04412018	PHASE2	COMPLETED	An Investigation on the Effects of Icosapent Ethyl (VascepaTM) on Inflammatory Biomarkers in Individuals With COVID-19
NCT05198843	PHASE1/PHASE2	TERMINATED	Testing an Omega-3 Fatty Acid-Based Anti-Cancer Therapy for Patients With Triple-Negative Inflammatory Breast Cancer That Has Spread to Other Parts of the Body

Clinical evidence (CIViC)

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

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).