Lepirudin

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Lepirudin
Lepirudin sequence.svg
Systematic (IUPAC) name
[Leu1,Thr2]-63-desulfohirudin
Clinical data
Trade names Refludan
AHFS/Drugs.com monograph
Pregnancy
category
  • US: B (No risk in non-human studies)
Legal status
  • Prescription (US)
Routes of
administration
SQ or IV
Pharmacokinetic data
Bioavailability 100
Biological half-life ~1.3 hours
Excretion Renal
Identifiers
CAS Registry Number 120993-53-5 YesY
ATC code B01AE02
IUPHAR/BPS 6469
DrugBank DB00001 N
UNII Y43GF64R34 N
KEGG D03692 YesY
ChEMBL CHEMBL1201666 N
Chemical data
Formula C288H448N80O110S6
Molecular mass 6983.5 g/mol
 N (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.