Lepirudin

Lepirudin is an anticoagulant that functions as a direct thrombin inhibitor.

Lepirudin
Clinical data
Trade namesRefludan
AHFS/Drugs.comMonograph
Pregnancy
category
  • US: B (No risk in non-human studies)
    Routes of
    administration    		SQ or IV
    ATC code
    Legal status
    Legal status
    Pharmacokinetic data
    Bioavailability100
    Elimination half-life~1.3 hours
    ExcretionRenal
    Identifiers
    CAS Number
    IUPHAR/BPS
    DrugBank
    ChemSpider
    • none
    UNII
    KEGG
    ChEBI
    ChEMBL
    Chemical and physical data
    FormulaC288H448N80O110S6
    Molar mass6983.5 g/mol g·mol−1
     NY (what is this?)  (verify)

    Brand name: Refludan, Generic: Lepirudin rDNA for injection.

    Lepirudin is a recombinant hirudin[1] derived from yeast cells. It is almost identical to hirudin extracted from Hirudo medicinalis. It differs by the 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.

    Lepirudin may be used as an anticoagulant when heparins (unfractionated or low-molecular-weight) are contraindicated because of heparin-induced thrombocytopenia.

    Market withdrawal

    Bayer announced that it ceased the production of lepirudin (Refludan) on May 31, 2012. At the time of the announcement, the company expected that supply from wholesalers was going to be depleted by mid-2013.[2]

    References
    1. Arman T. Askari; A. Michael Lincoff (October 2009). Antithrombotic Drug Therapy in Cardiovascular Disease. Springer. pp. 440–. ISBN 978-1-60327-234-6. Retrieved 30 October 2010.
    2. http://www.ashp.org/menu/DrugShortages/DrugsNoLongerAvailable/Bulletin.aspx?id=924
    • Smythe M, Stephens J, Koerber J, Mattson J (2005). "A comparison of lepirudin and argatroban outcomes". Clin Appl Thromb Hemost. 11 (4): 371–4. doi:10.1177/107602960501100403. PMID 16244762.
    • Tardy, B; Lecompte, T; Boelhen, F; Tardy-Poncet, B; Elalamy, I; Morange, P; Gruel, Y; Wolf, M; François, D (2006). "Predictive factors for thrombosis and major bleeding in an observational study in 181 patients with heparin-induced thrombocytopenia treated with lepirudin". Blood. 108 (5): 1492–6. doi:10.1182/blood-2006-02-001057. PMID 16690967.
    • Lubenow N, Eichler P, Lietz T, Greinacher A (2005). "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. 3 (11): 2428–36. doi:10.1111/j.1538-7836.2005.01623.x. PMID 16241940.


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