Lepirudin

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Lepirudin
Lepirudin sequence.svg
Clinical data
Trade names Refludan
AHFS/Drugs.com Monograph
Pregnancy
category
  • US: B (No risk in non-human studies)
Routes of
administration
SQ or IV
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability 100
Biological half-life ~1.3 hours
Excretion Renal
Identifiers
CAS Number
IUPHAR/BPS
DrugBank
ChemSpider
  • none
UNII
KEGG
ChEMBL
Chemical and physical data
Formula C288H448N80O110S6
Molar mass 6983.5 g/mol
 NYesY (what is this?)  (verify)

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

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[edit]

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[edit]

  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

External links[edit]

  • 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.