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Lepirudin

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Lepirudin
Clinical data
Trade namesRefludan
AHFS/Drugs.comMonograph
Routes of
administration
SQ or IV
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability100
Elimination half-life~1.3 hours
ExcretionRenal
Identifiers
  • [Leu1,Thr2]-63-desulfohirudin
CAS Number
IUPHAR/BPS
DrugBank
ChemSpider
  • none
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC288H448N80O110S6
Molar mass6983.56 g·mol−1
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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. Lepirudin is almost identical to hirudin extracted from Hirudo medicinalis, having the amino acid sequence LTYTDCTESGQNLCLCEGSNVCGQGNKCILGSDGEKNQCVTGEGTPKPQSHNDGDFEEIPEEYLQ with disulfide bridges at Cys6-Cys14, Cys16-Cys28 and Cys22-Cys39, and differs from 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

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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

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  1. ^ Askari AT, Lincoff AM (October 2009). Antithrombotic Drug Therapy in Cardiovascular Disease. Springer. pp. 440–. ISBN 978-1-60327-234-6. Retrieved 30 October 2010.
  2. ^ "Discontinued Drug Bulletin: Lepirudin Injection". American Society of Health System Pharmacists (ASHP). 23 May 2012. Archived from the original on 2014-07-23.

Further reading

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