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 |
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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 Date1998 |
PubMed
Title | Date | PubMed |
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[Heparin-induced thrombocytopenia type II. Intra- and postoperative lepirudin treatment in acute ischemia of the extremities]. | 1998 Oct 9 |
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[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 |
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Repetitive intraoperative use of recombinant hirudin (Lepirudin) in peripheral vascular surgery with HITT. | 2001 Dec 22 |
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Venous limb gangrene during overlapping therapy with warfarin and a direct thrombin inhibitor for immune heparin-induced thrombocytopenia. | 2002 Sep |
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Massive pulmonary embolism due to late-onset heparin-induced thrombocytopenia following coronary artery bypass graft surgery: successful treatment with lepirudin. | 2003 Jul-Aug |
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Direct thrombin inhibitors for treatment of heparin induced thrombocytopenia, deep vein thrombosis and atrial fibrillation. | 2005 |
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Multivessel coronary thrombosis resulting from heparin induced thrombocytopenia. | 2007 Sep |
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Lepirudin for treatment of acute thrombosis during pregnancy. | 2008 Aug |
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Bivalirudin. | 2008 May |
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Extremely low doses of lepirudin in a patient with heparin-induced thrombocytopenia, high bleeding risk and renal insufficiency. | 2009 Aug |
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[Heparin-induced thrombocytopenia and liver hemorrhage following polytrauma]. | 2009 Sep |
Substance Class |
Protein
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Y43GF64R34
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N0000175518
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EMA ASSESSMENT REPORTS |
REFLUDAN (WITHDRAWN: THROMBOEMBOLISM
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FDA ORPHAN DRUG |
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B01AE02
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C263
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N0000009963
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1_6 | 1_14 |
1_16 | 1_28 |
1_22 | 1_39 |
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TARGET -> INHIBITOR |
IRREVERSIBLE INHIBITOR
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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MOL_WEIGHT:SEQUENCE(CALCULATED) | CHEMICAL |
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Molecular Formula | CHEMICAL |
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