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药品详细

Lepirudin(Lepirudin)

化学结构式图
中文名
Lepirudin
英文名
Lepirudin
分子式
C287H440N80O110S6
化学名
分子量
6963.4250
CAS号
120993-53-5
ATC分类
B01A 抗血栓药
药物类型
biotech
阶段
approved
商品名
Refludan (Berlex Labs);
同义名
Hirudin variant-1;
基本介绍

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. It is produced via yeast cells.

生产厂家
  • Bayer healthcare pharmaceuticals inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Smythe MA, Stephens JL, Koerber JM, Mattson JC: A comparison of lepirudin and argatroban outcomes. Clin Appl Thromb Hemost. 2005 Oct;11(4):371-4. Pubmed
  2. Tardy B, Lecompte T, Boelhen F, Tardy-Poncet B, Elalamy I, Morange P, Gruel Y, Wolf M, Francois D, Racadot E, Camarasa P, Blouch MT, Nguyen F, Doubine S, Dutrillaux F, Alhenc-Gelas M, Martin-Toutain I, Bauters A, Ffrench P, de Maistre E, Grunebaum L, Mouton C, Huisse MG, Gouault-Heilmann M, Lucke V: Predictive factors for thrombosis and major bleeding in an observational study in 181 patients with heparin-induced thrombocytopenia treated with lepirudin. Blood. 2006 Sep 1;108(5):1492-6. Epub 2006 May 11. Pubmed
  3. Lubenow N, Eichler P, Lietz T, Greinacher A: Lepirudin in patients with heparin-induced thrombocytopenia – results of the third prospective study (HAT-3) and a combined analysis of HAT-1, HAT-2, and HAT-3. J Thromb Haemost. 2005 Nov;3(11):2428-36. Pubmed
  4. Askari AT, Lincoff AM: Antithrombotic Drug Therapy in Cardiovascular Disease. 2009 Oct; pp. 440–. ISBN 9781603272346. Google books.
剂型
Form Route Strength
Powder, for solution Intravenous
规格
Unit description Cost Unit
Refludan 50 mg vial 273.19 USD vial
化合物类型
Type biotech
Classes Not Available
Substructures Not Available
适应症
药理
Indication For the treatment of heparin-induced thrombocytopenia
Pharmacodynamics Lepirudin is used to break up clots and to reduce thrombocytopenia. It binds to thrombin and prevents thrombus or clot formation. It is a highly potent, selective, and essentially irreversible inhibitor of thrombin and clot-bond thrombin. Lepirudin requires no cofactor for its anticoagulant action. Lepirudin is a recombinant form of hirudin, an endogenous anticoagulant found in medicinal leeches.
Mechanism of action Lepirudin forms a stable non-covalent complex with alpha-thrombin, thereby abolishing its ability to cleave fibrinogen and initiate the clotting cascade. The inhibition of thrombin prevents the blood clotting cascade.
Absorption Bioavailability is 100% following injection.
Volume of distribution
  • 12.2 L [Healthy young subjects (n = 18, age 18-60 years)]
  • 18.7 L [Healthy elderly subjects (n = 10, age 65-80 years)]
  • 18 L [Renally impaired patients (n = 16, creatinine clearance below 80 mL/min)]
  • 32.1 L [HIT patients (n = 73)]
Protein binding Not Available
Metabolism

Lepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. However, con-clusive data are not available. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%) and other fragments of the parent drug.
Route of elimination Lepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%) and other fragments of the parent drug.
Half life Approximately 1.3 hours
Clearance
  • 164 ml/min [Healthy 18-60 yrs]
  • 139 ml/min [Healthy 65-80 yrs]
  • 61 ml/min [renal impaired]
  • 114 ml/min [HIT (Heparin-induced thrombocytopenia)]
Toxicity In case of overdose (eg, suggested by excessively high aPTT values) the risk of bleeding is increased.
Affected organisms
  • Humans and other mammals
Pathways
Pathway Name SMPDB ID
Smp00278 Lepirudin Pathway SMP00278
理化性质
Properties
State liquid
Melting point 65 oC (Otto, A. & Seckler, R. Eur. J. Biochem. 202:67-73 (1991))
Experimental Properties
Property Value Source
hydrophobicity -0.777 PhysProp
isoelectric point 4.04 Various sources
药物相互作用
食物相互作用
Not Available
>DB00001 sequence
LVYTDCTESGQNLCLCEGSNVCGQGNKCILGSDGEKNQCVTGEGTPKPQSHNDGDFEEIP
EEYLQ

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