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 Date1998 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| [Heparin-induced thrombocytopenia and liver hemorrhage following polytrauma]. | 2009-09 |
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| Extremely low doses of lepirudin in a patient with heparin-induced thrombocytopenia, high bleeding risk and renal insufficiency. | 2009-08 |
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| Lepirudin for treatment of acute thrombosis during pregnancy. | 2008-08 |
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| Bivalirudin. | 2008-05 |
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| Multivessel coronary thrombosis resulting from heparin induced thrombocytopenia. | 2007-09 |
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| Heparin-induced thrombocytopenia: treatment options and special considerations. | 2007-04 |
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| Recombinant factor VIIa for refractory bleeding after cardiac surgery secondary to anticoagulation with the direct thrombin inhibitor lepirudin. | 2006-04 |
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| [A case of heparin induced thrombocytopenia treated with lepirudin infusion: case report]. | 2006 |
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| Direct thrombin inhibitors for treatment of heparin induced thrombocytopenia, deep vein thrombosis and atrial fibrillation. | 2005 |
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| Treatment of heparin induced thrombocytopenia and thrombosis during the first trimester of pregnancy. | 2004-09 |
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| Effect of direct thrombin inhibitors, bivalirudin, lepirudin, and argatroban, on prothrombin time and INR values. | 2004-04 |
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| Direct thrombin inhibitor therapy in the cardiovascular patient. | 2003-10-15 |
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| Massive pulmonary embolism due to late-onset heparin-induced thrombocytopenia following coronary artery bypass graft surgery: successful treatment with lepirudin. | 2003-07-19 |
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| Venous limb gangrene during overlapping therapy with warfarin and a direct thrombin inhibitor for immune heparin-induced thrombocytopenia. | 2002-09 |
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| Direct antithrombin agents ameliorate disseminated intravascular coagulation in suspected heparin-induced thrombocytopenia thrombosis syndrome. | 2002-07 |
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| Repetitive intraoperative use of recombinant hirudin (Lepirudin) in peripheral vascular surgery with HITT. | 2001-12-22 |
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| Recombinant hirudin anticoagulation for aortic valve replacement in heparin-induced thrombocytopenia. | 2000-03 |
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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]. | 1999-02 |
|
| [Heparin-induced thrombocytopenia type II. Intra- and postoperative lepirudin treatment in acute ischemia of the extremities]. | 1998-10-09 |
| Substance Class |
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| 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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