Lepirudin

Lepirudin

Systematic (IUPAC) name
[Leu^1,Thr^2]-63-desulfohirudin
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
Legal status	Prescription (US)
Pharmacokinetic data
Bioavailability	100
Biological half-life	~1.3 hours
Excretion	Renal
Identifiers
CAS Number	120993-53-5
ATC code	B01AE02 (WHO)
IUPHAR/BPS	6469
DrugBank	DB00001
ChemSpider	none
UNII	Y43GF64R34
KEGG	D03692
ChEMBL	CHEMBL1201666
Chemical data
Formula	C288H448N80O110S6
Molar mass	6983.5 g/mol
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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. 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

External links

• DDB 30082

• 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.