U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
Lepirudin is a direct thrombin inhibitor obtained by recombinant technology from the medicinal leech and used for treatment of heparin-induced thrombocytopenia (HIT). Lepirudin was the first direct thrombin inhibitor approved and most frequently used for the treatment of patients with HIT. The efficacy of lepirudin for HIT has been shown to improve general outcomes in patients with HIT, reducing a primary composite endpoint of new thrombosis, all-cause amputation, and all-cause death. Lepirudin forms a stable non-covalent complex with alpha-thrombin, thereby abolishing its ability to cleave fibrinogen and initiate the clotting cascade. It is a highly potent, selective, and essentially irreversible inhibitor of thrombin and clot-bond thrombin. Lepirudin is identical to natural hirudin except for substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63.

Approval Year

Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
REFLUDAN

Approved Use

Refludan is indicated for anticoagulation in patients with heparin-associated thrombocytopenia (HIT) and associated thromboembolic disease in order to prevent further thromboembolic complications.

Launch Date

1998
PubMed

PubMed

TitleDatePubMed
[Heparin-induced thrombocytopenia type II. Intra- and postoperative lepirudin treatment in acute ischemia of the extremities].
1998 Oct 9
[Heparin-induced thrombocytopenia type II with early aortocoronary bypass occlusion and stent thrombosis after PTCA of the RCA--treatment with lepirudin (Refludan) and abciximab (Reo pro) during recanalization of the RCA].
1999 Feb
Direct thrombin inhibitor therapy in the cardiovascular patient.
2003 Oct 15
Effect of direct thrombin inhibitors, bivalirudin, lepirudin, and argatroban, on prothrombin time and INR values.
2004 Apr
[A case of heparin induced thrombocytopenia treated with lepirudin infusion: case report].
2006
Lepirudin for treatment of acute thrombosis during pregnancy.
2008 Aug
Extremely low doses of lepirudin in a patient with heparin-induced thrombocytopenia, high bleeding risk and renal insufficiency.
2009 Aug
Substance Class Protein
Created
by admin
on Sat Dec 16 01:57:04 GMT 2023
Edited
by admin
on Sat Dec 16 01:57:04 GMT 2023
Protein Sub Type
Sequence Type COMPLETE
Record UNII
Y43GF64R34
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
LEPIRUDIN
EMA EPAR   INN   MART.   VANDF   WHO-DD  
INN  
Official Name English
LEPIRUDIN RECOMBINANT
ORANGE BOOK  
Common Name English
REFLUDAN
Brand Name English
LEPIRUDIN [VANDF]
Common Name English
Lepirudin [WHO-DD]
Common Name English
lepirudin [INN]
Common Name English
LEPIRUDIN [EMA EPAR]
Common Name English
LEPIRUDIN [MART.]
Common Name English
HIRUDIN LEPIRUDIN [MI]
Common Name English
LEPIRUDIN RECOMBINANT [ORANGE BOOK]
Common Name English
1-L-LEUCINE-2-L-THREONINE-63-DESULFOHIRUDIN (HIRUDO MEDICINALIS ISOFORM HV1)
Common Name English
Classification Tree Code System Code
NDF-RT N0000175518
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
EMA ASSESSMENT REPORTS REFLUDAN (WITHDRAWN: THROMBOEMBOLISM
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
FDA ORPHAN DRUG 102796
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
WHO-ATC B01AE02
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
NCI_THESAURUS C263
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
NDF-RT N0000009963
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
NDF-RT N0000175980
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
Code System Code Type Description
MERCK INDEX
m6025
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
PRIMARY Merck Index
NCI_THESAURUS
C1839
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
PRIMARY
EVMPD
SUB08435MIG
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
PRIMARY
DRUG CENTRAL
2995
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
PRIMARY
CAS
138068-37-8
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
PRIMARY
IUPHAR
6469
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
PRIMARY
RXCUI
237057
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
PRIMARY RxNorm
ChEMBL
CHEMBL1201666
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
PRIMARY
INN
7355
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
PRIMARY
LACTMED
Lepirudin
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
PRIMARY
CHEBI
142437
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
PRIMARY
EPA CompTox
DTXSID50160461
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
PRIMARY
FDA UNII
Y43GF64R34
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
PRIMARY
DRUG BANK
DB00001
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
PRIMARY
WIKIPEDIA
Lepirudin
Created by admin on Sat Dec 16 01:57:05 GMT 2023 , Edited by admin on Sat Dec 16 01:57:05 GMT 2023
PRIMARY
PUBCHEM
118856773
Created by admin on Sat Dec 16 01:57:04 GMT 2023 , Edited by admin on Sat Dec 16 01:57:04 GMT 2023
PRIMARY
From To
1_6 1_14
1_16 1_28
1_22 1_39
Related Record Type Details
TARGET -> INHIBITOR
IRREVERSIBLE INHIBITOR
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT:SEQUENCE(CALCULATED) CHEMICAL
Molecular Formula CHEMICAL