Eptifibatide

Summary

Eptifibatide (CHEMBL1174) is an approved protein platelet aggregation inhibitor (ATC B01AC16); indicated across 15 conditions including myocardial infarction and thrombotic disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Protein
• ATC class: B01AC16
• Indications: 15 conditions
• Clinical trials: 24
• Chemistry: 832 Da · C35H49N11O9S2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1174
Name	Eptifibatide
Type	Protein
Max phase	4
FDA approved	yes
PubChem CID	448812
ChEBI	CHEBI:291902
ATC	B01AC16
Molecular formula	C35H49N11O9S2
Molecular weight	832
InChIKey	CZKPOZZJODAYPZ-LROMGURASA-N

SMILES: C1C[C@H]2C(=O)N[C@@H](CSSCCC(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N2C1)CC3=CNC4=CC=CC=C43)CC(=O)O)CCCCN=C(N)N)C(=O)N

IUPAC name: 2-[(3S,6S,12S,20R,23S)-20-carbamoyl-12-[4-(diaminomethylideneamino)butyl]-3-(1H-indol-3-ylmethyl)-2,5,8,11,14,22-hexaoxo-17,18-dithia-1,4,7,10,13,21-hexazabicyclo[21.3.0]hexacosan-6-yl]acetic acid

ChEBI definition: A synthetic homodetic cyclic peptide comprising Nα-(3-sulfanylpropanoyl)homoarginyl, glycyl, aspartyl, tryptophyl, prolyl and cysteinamide residues connected in sequence and cyclised via a disulfide bond. Derived from a protein found in the venom of the southeastern pygmy rattlesnake, Sistrurus miliarus barbouri, eptifibatide is an anti-coagulant that inhibits platelet aggregation by selectively blocking the platelet glycoprotein IIb/IIIa receptor, so preventing the binding of fibrinogen, von Willebrand factor, and other adhesive ligands. It is used in the management of unstable angina and in patients undergoing coronary angioplasty and stenting procedures.

Pharmacological roles (ChEBI): platelet aggregation inhibitor, anticoagulant.

Also known as: Eptifibatida, Eptifibatide, Eptifibatide accord, Integrelin, Integrilin, EPTIFIBATIDE, eptifibatide, SID144206056, SID170465043

Parent form; salt/anhydrous children: CHEMBL4068311

Patent coverage: 4,557 distinct patent families (17,269 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 16,273 (94%) of the total. 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
	integrin αIIbβ3	Inhibition	6.85

Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Integrin alpha-V/beta-3, Integrin alpha-IIb/beta-3.

Bioactivity

ChEMBL activities: 3 potent at pChembl ≥ 5 of 3 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ITGB3	6.92	Kd	120	nM	CHEMBL_ACT_20604685
ITGB3	6.85	IC50	140	nM	CHEMBL_ACT_921611
ITGB3	6.24	IC50	570	nM	CHEMBL_ACT_921612

Target pathways

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

Indications & clinical

Indications

15 indications (5 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
myocardial infarction	4	MONDO:0005068	EFO:0000612
thrombotic disease	4	MONDO:0000831	HP:0004419
acute coronary syndrome	4	MONDO:0005542	EFO:0005672
acute myocardial infarction	4	MONDO:0004781	EFO:0008583
intermediate coronary syndrome	4	MONDO:0006805	EFO:1000985
cardiovascular disorder	3	MONDO:0004995	EFO:0000319
myocardial ischemia	3	MONDO:0024644	EFO:1001375
stroke disorder	2	MONDO:0005098	EFO:0000712
pneumonia	2	MONDO:0005249	EFO:0003106
brain infarction	2	MONDO:0005394	EFO:0004277
toxic shock syndrome	2	MONDO:0001881	EFO:0006834
ST-elevation myocardial infarction	2	MONDO:0041656	EFO:0008585
coronary artery disorder	2	MONDO:0005010	EFO:0001645
sickle cell disease	1	MONDO:0011382	MONDO:0011382

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

Clinical trials

Total trials: 24.

Phase distribution

Phase	Trials
PHASE2	11
PHASE3	7
PHASE4	4
PHASE1/PHASE2	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00111566	PHASE4	COMPLETED	BRIEF-PCI: Brief Infusion of Eptifibatide Following Percutaneous Coronary Intervention
NCT00289601	PHASE4	TERMINATED	Randomized Study of Aspirin Resistant Patients Undergoing Angioplasty
NCT01454440	PHASE4	TERMINATED	The INtegrilin Plus STenting to Avoid Myocardial Necrosis Trial (INSTANT)
NCT01863134	PHASE4	COMPLETED	Clinical Effects of Eptifibatide Administration in High Risk Patients Presenting With Non-ST Segment Elevation Acute Coronary Syndrome (NSTE-ACS) Requiring Urgent Coronary Artery Bypass Graft Surgery in Short- and Long-Term Follow-up
NCT07347626	PHASE3	NOT_YET_RECRUITING	Eptifibatide for Extended Window Ischemic Stroke After Thrombolysis
NCT00089895	PHASE3	COMPLETED	EARLY ACS: Early Glycoprotein IIb/IIIa Inhibition in Patients With Non-ST-segment Elevation Acute Coronary Syndrome (Study P03684AM2)(COMPLETED)
NCT00426751	PHASE3	COMPLETED	Efficacy Of Eptifibatide Compared To Abciximab In Primary Percutaneous Coronary Intervention (PCI) For Acute ST Elevation Myocardial Infarction (STEMI)
NCT00638976	PHASE3	COMPLETED	INSTANT: INtegrilin Plus STenting to Avoid Myocardial Necrosis Trial
NCT01076764	PHASE3	COMPLETED	Effect of Otamixaban Versus Unfractionated Heparin + Eptifibatide in Patients With Unstable Angina/Non ST Elevation Myocardial Infarction Undergoing Early Invasive Strategy
NCT03735979	PHASE3	COMPLETED	Multi-arm Optimization of Stroke Thrombolysis
NCT03844594	PHASE3	UNKNOWN	Eptifibatide in Endovascular Treatment of Acute Ischemic Stroke (EPOCH)
NCT00061373	PHASE2	COMPLETED	Combination Anti-Platelet and Anti-Coagulation Treatment After Lysis of Ischemic Stroke Trial (CATALIST)
NCT00250991	PHASE1/PHASE2	COMPLETED	Combined Approach to Lysis Utilizing Eptifibatide and rt-PA in Acute Ischemic Stroke (CLEAR Stroke) Trial
NCT00317395	PHASE2	COMPLETED	Study of Otamixaban Versus Unfractionated Heparin (UFH) and Eptifibatide in Non-ST Elevation Acute Coronary Syndrome
NCT00719914	PHASE2	TERMINATED	A Safety/Efficacy Study of Intracoronary Integrilin to Improve Balloon Angioplasty Outcomes for the Treatment of Heart Attacks
NCT00834899	PHASE1/PHASE2	TERMINATED	A Safety Study of Eptifibatide in Patients With Sickle Cell Disease
NCT00894803	PHASE2	COMPLETED	Study of the Combination Therapy of Rt-PA and Eptifibatide to Treat Acute Ischemic Stroke
NCT00945308	PHASE2	UNKNOWN	Effectiveness of Intracoronary Injection of Eptifibatide in Primary Coronary Intervention in STEMI Patients
NCT01522417	PHASE2	COMPLETED	Shortened Aggrastat® Versus Integrilin in Percutaneous Coronary Intervention
NCT01532544	PHASE2	TERMINATED	Integrilin and Ilomedin in Combination in Comparison to Standard Treatment in Severe Pneumonia Patients With Severe Sepsis
NCT01919723	PHASE2	COMPLETED	Ticagrelor and Eptifibatide Bolus-Only Versus Ticagrelor and Eptifibatide Bolus Plus Abbreviated Infusion
NCT01977456	PHASE2	COMPLETED	Study of the Combination Therapy of Rt-PA and Eptifibatide to Treat Acute Ischemic Stroke (CLEAR-FDR)
NCT02204852	PHASE2	COMPLETED	Co-administration of Iloprost and Eptifibatide in Septic Shock Patients
NCT02925923	PHASE2	COMPLETED	Crushed Ticagrelor Versus Eptifibatide Bolus + Clopidogrel

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).