Lepirudin
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| Clinical data | |
|---|---|
| Trade names | Refludan |
| AHFS/Drugs.com | Monograph |
| Routes of administration | SQ or IV |
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| Pharmacokinetic data | |
| Bioavailability | 100 |
| Elimination half-life | ~1.3 hours |
| Excretion | Renal |
| Identifiers | |
IUPAC name
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| Chemical and physical data | |
| Formula | C288H448N80O110S6 |
| Molar mass | 6983.56 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
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
- ↑ 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.
- ↑ http://www.ashp.org/menu/DrugShortages/DrugsNoLongerAvailable/Bulletin.aspx?id=924
External links
- Diseases Database (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.