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
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | REFLUDAN Approved UseRefludan is indicated for anticoagulation in patients with heparin-associated thrombocytopenia (HIT) and associated thromboembolic disease in order to prevent further thromboembolic complications. Launch Date8.8914238E11 |
PubMed
Title | Date | PubMed |
---|---|---|
[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 |
|
Recombinant hirudin anticoagulation for aortic valve replacement in heparin-induced thrombocytopenia. | 2000 Mar |
|
Repetitive intraoperative use of recombinant hirudin (Lepirudin) in peripheral vascular surgery with HITT. | 2001 Dec 22 |
|
Direct antithrombin agents ameliorate disseminated intravascular coagulation in suspected heparin-induced thrombocytopenia thrombosis syndrome. | 2002 Jul |
|
Venous limb gangrene during overlapping therapy with warfarin and a direct thrombin inhibitor for immune heparin-induced thrombocytopenia. | 2002 Sep |
|
Massive pulmonary embolism due to late-onset heparin-induced thrombocytopenia following coronary artery bypass graft surgery: successful treatment with lepirudin. | 2003 Jul-Aug |
|
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 |
|
Treatment of heparin induced thrombocytopenia and thrombosis during the first trimester of pregnancy. | 2004 Sep |
|
Direct thrombin inhibitors for treatment of heparin induced thrombocytopenia, deep vein thrombosis and atrial fibrillation. | 2005 |
|
[A case of heparin induced thrombocytopenia treated with lepirudin infusion: case report]. | 2006 |
|
Recombinant factor VIIa for refractory bleeding after cardiac surgery secondary to anticoagulation with the direct thrombin inhibitor lepirudin. | 2006 Apr |
|
Heparin-induced thrombocytopenia: treatment options and special considerations. | 2007 Apr |
|
Multivessel coronary thrombosis resulting from heparin induced thrombocytopenia. | 2007 Sep |
|
Lepirudin for treatment of acute thrombosis during pregnancy. | 2008 Aug |
|
Bivalirudin. | 2008 May |
|
Extremely low doses of lepirudin in a patient with heparin-induced thrombocytopenia, high bleeding risk and renal insufficiency. | 2009 Aug |
|
[Heparin-induced thrombocytopenia and liver hemorrhage following polytrauma]. | 2009 Sep |
Substance Class |
Protein
Created
by
admin
on
Edited
Sat Dec 17 13:17:14 UTC 2022
by
admin
on
Sat Dec 17 13:17:14 UTC 2022
|
Protein Sub Type | |
Sequence Type | COMPLETE |
Record UNII |
Y43GF64R34
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Official Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
NDF-RT |
N0000175518
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
||
|
EMA ASSESSMENT REPORTS |
REFLUDAN (WITHDRAWN: THROMBOEMBOLISM
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
||
|
FDA ORPHAN DRUG |
102796
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
||
|
WHO-ATC |
B01AE02
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
||
|
NCI_THESAURUS |
C263
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
||
|
NDF-RT |
N0000009963
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
||
|
NDF-RT |
N0000175980
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
M6025
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
PRIMARY | Merck Index | ||
|
C1839
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
PRIMARY | |||
|
SUB08435MIG
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
PRIMARY | |||
|
2995
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
PRIMARY | |||
|
138068-37-8
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
PRIMARY | |||
|
6469
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
PRIMARY | |||
|
237057
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
PRIMARY | RxNorm | ||
|
CHEMBL1201666
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
PRIMARY | |||
|
7355
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
PRIMARY | |||
|
Lepirudin
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
PRIMARY | |||
|
142437
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
PRIMARY | |||
|
DTXSID50160461
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
PRIMARY | |||
|
Y43GF64R34
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
PRIMARY | |||
|
DB00001
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
PRIMARY | |||
|
Lepirudin
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
PRIMARY | |||
|
118856773
Created by
admin on Sat Dec 17 13:17:14 UTC 2022 , Edited by admin on Sat Dec 17 13:17:14 UTC 2022
|
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 |
|