Bivalirudin

Summary

Bivalirudin (CHEMBL5314348) is an approved protein (ATC B01AE06) targeting F2; indicated across 17 conditions including acute coronary syndrome and thrombotic disease.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Protein
• ATC class: B01AE06
• Targets: 1 (F2)
• Indications: 17 conditions
• Clinical trials: 55

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL5314348
Name	Bivalirudin
Type	Protein
Max phase	4
ATC	B01AE06

Also known as: Angiomax, Angiomax rtu, Angiox, BG-8967, BG8967, Bivalirudin, Bivalirudin in 0.9% sodium chloride, Bivalirudina, Bivalirudine, BIVALIRUDIN, bivalirudin

Parent form; salt/anhydrous children: CHEMBL5314353

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
F2	coagulation factor II, thrombin	Inhibition	8.6	1.4%	P00734

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Prothrombin.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
F2	8.04	AC50	9.2	nM	CHEMBL_ACT_25197250

Target pathways

Aggregated over 1 target gene(s): F2.

Top Reactome pathways

38 total, by targets touching each:

Pathway	Targets	Genes
Hemostasis	1	F2
R-HSA-140837	1	F2
R-HSA-140875	1	F2
R-HSA-140877	1	F2
Gamma-carboxylation of protein precursors	1	F2
Transport of gamma-carboxylated protein precursors from the endoplasmic reticulum to the Golgi apparatus	1	F2
Removal of aminoterminal propeptides from gamma-carboxylated proteins	1	F2
Gamma-carboxylation, transport, and amino-terminal cleavage of proteins	1	F2
Signal Transduction	1	F2
Gamma carboxylation, hypusinylation, hydroxylation, and arylsulfatase activation	1	F2
Disease	1	F2
Complement cascade	1	F2
Innate Immune System	1	F2
Immune System	1	F2
Cell surface interactions at the vascular wall	1	F2
Signaling by GPCR	1	F2
Class A/1 (Rhodopsin-like receptors)	1	F2
Peptide ligand-binding receptors	1	F2
Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)	1	F2
GPCR downstream signalling	1	F2
Metabolism of proteins	1	F2
G alpha (q) signalling events	1	F2
Thrombin signalling through proteinase activated receptors (PARs)	1	F2
GPCR ligand binding	1	F2
Post-translational protein modification	1	F2
Platelet activation, signaling and aggregation	1	F2
Platelet Aggregation (Plug Formation)	1	F2
R-HSA-9651496	1	F2
Defective factor XII causes hereditary angioedema	1	F2
Defective factor VIII causes hemophilia A	1	F2

Dominant GO biological processes

GO term	Targets
proteolysis	1
acute-phase response	1
cell surface receptor signaling pathway	1
blood coagulation	1
positive regulation of cell population proliferation	1
regulation of cell shape	1
response to wounding	1
negative regulation of platelet activation	1
platelet activation	1
regulation of blood coagulation	1
positive regulation of blood coagulation	1
negative regulation of blood coagulation	1
positive regulation of cell growth	1
positive regulation of insulin secretion	1
positive regulation of collagen biosynthetic process	1

Indications & clinical

Indications

17 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
acute coronary syndrome	4	MONDO:0005542	EFO:0005672
thrombotic disease	4	MONDO:0000831	HP:0004419
intermediate coronary syndrome	4	MONDO:0006805	EFO:1000985
thrombocytopenia	4	MONDO:0002049	HP:0001873
syndromic disease	4	MONDO:0002254	MONDO:0002254
myocardial infarction	3	MONDO:0005068	EFO:0000612
cardiovascular disorder	3	MONDO:0004995	EFO:0000319
aortic valve stenosis	3	MONDO:0042981	EFO:0000266
hematologic disorder	3	MONDO:0005570	HP:0001871
coronary artery disorder	3	MONDO:0005010	EFO:0001645
heart disorder	3	MONDO:0005267	EFO:0003777
acute disease	3	MONDO:0020683	MONDO:0020683
subarachnoid hemorrhage	3	MONDO:0005099	EFO:0000713
acute myocardial infarction	3	MONDO:0004781	EFO:0008583

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

Clinical trials

Total trials: 55.

Phase distribution

Phase	Trials
PHASE4	25
PHASE3	15
Not specified	9
PHASE2	5
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05984537	PHASE4	RECRUITING	A Study on the Impact of Bivalirudin Usage During PCI for High-risk Plaques on Post-PCI Coronary Microcirculation.
NCT00262054	PHASE4	COMPLETED	Un-fractionated Heparin Versus Bivalirudin During Percutaneous Coronary Interventions (PCI) (ISAR-REACT-3)
NCT00373451	PHASE4	COMPLETED	Randomized Comparison of Abciximab Plus Heparin With Bivalirudin in Acute Coronary Syndrome
NCT00448461	PHASE4	COMPLETED	Antithrombotic Regimens and Outcome
NCT00669149	PHASE4	TERMINATED	Anticoagulant Treatments and Percutaneous Coronary Angioplasty
NCT00759083	PHASE4	WITHDRAWN	Bivalirudin PCI Registry in Heparin Induced Thrombocytopenia/Heparin Induced Thrombocytopenia and Thrombosis Syndrome (HIT/HITTS) Patients
NCT00976092	PHASE4	UNKNOWN	Efficacy Study of Combined Prasugrel and Bivalirudin Versus Clopidogrel and Heparin in Myocardial Infarction
NCT01084993	PHASE4	UNKNOWN	EArly Discharge After Transradial Stenting of CoronarY Arteries in High-Risk Patients of Bleeding
NCT01158846	PHASE4	UNKNOWN	Bivalirudin/Prasugrel Versus Abciximab/Clopidogrel in Patients Presenting With STEMI
NCT01464671	PHASE4	TERMINATED	Angiomax® or Unfractionated Heparin for Patients Undergoing Percutaneous Coronary Intervention
NCT01519518	PHASE4	COMPLETED	How Effective Are Antithrombotic Therapies in Primary Percutaneous Coronary Intervention
NCT01642238	PHASE4	COMPLETED	Antithrombotic Effects of Ticagrelor Versus Clopidogrel
NCT01696110	PHASE4	COMPLETED	BivaliRudin in Acute Myocardial Infarction vs Glycoprotein IIb/IIIa and Heparin :a Randomised Controlled Trial.
NCT01848899	PHASE4	COMPLETED	Effects Contrast on Platelet Activity, Thrombosis and Fibrinolysis in Patients Undergoing Coronary Angiography
NCT02311231	PHASE4	COMPLETED	Bivalirudin vs Heparin in NSTEMI and STEMI in Patients on Modern Antiplatelet Therapy in SWEDEHEART
NCT02787317	PHASE4	UNKNOWN	Bivalirudin in Stable Ischemic Heart Disease Patients Undergoing PCI
NCT03318393	PHASE4	COMPLETED	Study Comparing Bivalirudin Versus Heparin in Neonatal and Pediatric ECMO
NCT03588611	PHASE4	COMPLETED	Reduce Bolus Injection of Bivalirudin
NCT03664180	PHASE4	COMPLETED	Comparison of Anticoagulation Prolongation vs. no Anticoagulation in STEMI Patients After Primary PCI
NCT03882775	PHASE4	UNKNOWN	Bivalirudin in Elderly Patients With Acute ST-segment Elevation Myocardial Infarction
NCT03965208	PHASE4	UNKNOWN	Safety and Efficacy of Bivalirudin Versus Heparin for Systemic Anticoagulation in Extracorporeal Membrane Oxygenation
NCT04046029	PHASE4	UNKNOWN	Bivalirudin in Elderly Patients Undergoing Elective Percutaneous Coronary Intervention.
NCT04185077	PHASE4	UNKNOWN	Bivalirudin in Late PCI for Oatients With STEMI
NCT04195997	PHASE4	UNKNOWN	Multi-center Application of Bivalirudin in Left Atrial Appendage Occlusion
NCT04445935	PHASE4	UNKNOWN	Anticoagulation in Patients Suffering From COVID-19 Disease The ANTI-CO Trial
NCT00043940	PHASE3	COMPLETED	Anticoagulant Therapy With Bivalirudin in the Performance of Percutaneous Coronary Intervention in Patients With Heparin-Induced Thrombocytopenia (AT BAT, First Inning)
NCT00073593	PHASE3	COMPLETED	Comparing Angiomax to Heparin With Protamine Reversal in Patients OPCAB
NCT00079508	PHASE3	COMPLETED	Angiomax in Patients With HIT/HITTS Type II Undergoing CPB
NCT00079586	PHASE3	COMPLETED	Comparing Angiomax to Heparin With Protamine in Patients Undergoing Cardiopulmonary Bypass (CPB)
NCT00433966	PHASE3	COMPLETED	Harmonizing Outcomes With Revascularization and Stents in Acute Myocardial Infarction
NCT00616460	PHASE3	COMPLETED	ACRIPAB- Trial: Anti Coagulation Regimen In High Risk PAtients for Bleeding
NCT01087723	PHASE3	COMPLETED	European Ambulance Acute Coronary Syndrome (ACS) Angiography Trial
NCT01465503	PHASE3	COMPLETED	Novel Approaches in Preventing and Limiting Events III Trial (NAPLES III): Bivalirudin in High-risk Bleeding Patients
NCT01555658	PHASE3	UNKNOWN	Bivalirudin Plus Stenting in Long Lesion to Avoid Periprocedural Myocardial Necrosis Trial
NCT01651780	PHASE3	COMPLETED	Open-label, Randomized Trial in Participants Undergoing TAVR to Determine Safety & Efficacy of Bivalirudin vs UFH
NCT01848106	PHASE3	TERMINATED	A Study To Determine the Efficacy and Safety of REG1 Compared to Bivalirudin in Patients Undergoing PCI
NCT01913483	PHASE3	TERMINATED	ENDOvascular Interventions With AngioMAX: The ENDOMAX Trial
NCT02448550	PHASE3	TERMINATED	Comparison of Anticoagulation for All-comers Undergoing Percutaneous Coronary Revascularization Trial
NCT02565147	PHASE3	TERMINATED	Bivalirudin Infusion for Ventricular Infarction Limitation
NCT02897037	PHASE3	UNKNOWN	Bivalirudin in Acute Myocardial Infarction

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

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.

50 molecules share ≥1 primary target. Top 50 by shared-target count:

Molecule	Source	Status	Shared targets
APIXABAN	ChEMBL + PubChem	Phase 4 (approved)	F2
EDOXABAN	ChEMBL + PubChem	Phase 4 (approved)	F2
ARGATROBAN	ChEMBL	Phase 4 (approved)	F2
BENZOYL PEROXIDE	ChEMBL	Phase 4 (approved)	F2
BETRIXABAN	ChEMBL	Phase 4 (approved)	F2
BORTEZOMIB	ChEMBL	Phase 4 (approved)	F2
CAPTOPRIL	ChEMBL	Phase 4 (approved)	F2
CIANIDANOL	ChEMBL	Phase 4 (approved)	F2
DABIGATRAN ETEXILATE	ChEMBL	Phase 4 (approved)	F2
DEQUALINIUM	ChEMBL	Phase 4 (approved)	F2
GENTIAN VIOLET	ChEMBL	Phase 4 (approved)	F2
HEXAMIDINE	ChEMBL	Phase 4 (approved)	F2
INDIGOTINDISULFONATE	ChEMBL	Phase 4 (approved)	F2
LIOTHYRONINE	ChEMBL	Phase 4 (approved)	F2
LUSUTROMBOPAG	ChEMBL	Phase 4 (approved)	F2
MELAGATRAN	ChEMBL	Phase 4 (approved)	F2
METHYLPREDNISOLONE	ChEMBL	Phase 4 (approved)	F2
PENTAMIDINE	ChEMBL	Phase 4 (approved)	F2
RIVAROXABAN	ChEMBL	Phase 4 (approved)	F2
SUCCIMER	ChEMBL	Phase 4 (approved)	F2
SULFAGUANIDINE	ChEMBL	Phase 4 (approved)	F2
TELOTRISTAT	ChEMBL	Phase 4 (approved)	F2
XIMELAGATRAN	ChEMBL	Phase 4 (approved)	F2
CAMOSTAT	ChEMBL	Phase 3	F2
CAMOSTAT MESILATE	ChEMBL	Phase 3	F2
DABIGATRAN	ChEMBL	Phase 3	F2
GABEXATE	ChEMBL	Phase 3	F2
MILVEXIAN	ChEMBL	Phase 3	F2
NAFAMOSTAT	ChEMBL	Phase 3	F2
QUERCETIN	ChEMBL	Phase 3	F2
SILIBININ	ChEMBL	Phase 3	F2
BMS-986141	ChEMBL	Phase 2	F2
CETRAXATE	ChEMBL	Phase 2	F2
DIBROMPROPAMIDINE	ChEMBL	Phase 2	F2
EFEGATRAN	ChEMBL	Phase 2	F2
FIDEXABAN	ChEMBL	Phase 2	F2
GW813893	ChEMBL	Phase 2	F2
INOGATRAN	ChEMBL	Phase 2	F2
LETAXABAN	ChEMBL	Phase 2	F2
NAPSAGATRAN	ChEMBL	Phase 2	F2
PROFLAVINE	ChEMBL	Phase 2	F2
RAZAXABAN	ChEMBL	Phase 2	F2
SEGATROXABAN	ChEMBL	Phase 2	F2
TANOGITRAN	ChEMBL	Phase 2	F2
Echothiophate	PubChem	Approved	F2
Pimavanserin	PubChem	Approved	F2
Propylene Glycol	PubChem	Approved	F2
Pyrazinamide	PubChem	Approved	F2
Pyridoxine	PubChem	Approved	F2
Vorapaxar	PubChem	Approved	F2