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 Date8.8914238E11 |
PubMed
Title | Date | PubMed |
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Recombinant hirudin anticoagulation for aortic valve replacement in heparin-induced thrombocytopenia. | 2000 Mar |
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Direct antithrombin agents ameliorate disseminated intravascular coagulation in suspected heparin-induced thrombocytopenia thrombosis syndrome. | 2002 Jul |
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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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Recombinant factor VIIa for refractory bleeding after cardiac surgery secondary to anticoagulation with the direct thrombin inhibitor lepirudin. | 2006 Apr |
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Extremely low doses of lepirudin in a patient with heparin-induced thrombocytopenia, high bleeding risk and renal insufficiency. | 2009 Aug |
Substance Class |
Protein
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Sequence Type | COMPLETE |
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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 |
102796
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B01AE02
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C263
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N0000009963
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N0000175980
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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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