Lepirudin

Summary

Lepirudin (CHEMBL1201666) is an approved protein (ATC B01AE02) targeting F2; indicated across 5 conditions including thrombotic disease and thrombocytopenia.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Protein
• ATC class: B01AE02
• Targets: 1 (F2)
• Indications: 5 conditions
• Clinical trials: 4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1201666
Name	Lepirudin
Type	Protein
Max phase	4
ATC	B01AE02

Also known as: Hirudin lepirudin, Lepirudin, Lepirudin recombinant, Lepirudina, Lepirudine, Refludan, LEPIRUDIN

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	13	1.4%	P00734

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

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

5 indications (4 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
thrombotic disease	4	MONDO:0000831	HP:0004419
thrombocytopenia	4	MONDO:0002049	HP:0001873
lung neoplasm	1	MONDO:0021117	MONDO:0008903

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

Clinical trials

Total trials: 4.

Phase distribution

Phase	Trials
PHASE4	1
PHASE1/PHASE2	1
PHASE2	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00798525	PHASE4	TERMINATED	Argatroban Versus Lepirudin in Critically Ill Patients
NCT00003726	PHASE1/PHASE2	TERMINATED	Lepirudin in Treating Patients With Recurrent or Advanced Small Cell Lung Cancer
NCT00039767	PHASE2	COMPLETED	Heparin Versus Lepirudin Flushes in Preventing Blockage of Venous Access Devices
NCT01304238	Not specified	COMPLETED	Retrospective Registry of Patients With Acute Heparin-induced Thrombocytopenia Type II

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.

51 molecules share ≥1 primary target. Top 51 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
BIVALIRUDIN	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