Lepirudin: Difference between revisions

{{Short description|Pharmaceutical drug}}

{{Drugbox

| Verifiedfields = changed

| verifiedrevid = 407603372

<!-- Clinical data -->

| tradename = Refludan

| Drugs.com = {{drugs.com|monograph|lepirudin}}

| pregnancy_category =

| legal_US = Rx only <!-- OTC / Rx-only -->

<!-- Pharmacokinetic data -->

| bioavailability = 100

| protein_bound =

| metabolism =

| elimination_half-life = ~1.3 hours

| excretion = Renal

<!-- Identifiers -->

| CAS_number_Ref = {{cascite|correct|CAS}}

| CAS_number = 138068-37-8

| ATC_prefix = B01

| ATC_suffix = AE02

| ATC_supplemental =

| ChEBI = 142437

| PubChem =

| IUPHAR_ligand = 6469

| DrugBank_Ref = {{drugbankcite|changed|drugbank}}

| DrugBank = DB00001

| UNII_Ref = {{fdacite|changed|FDA}}

| UNII = Y43GF64R34

| KEGG_Ref = {{keggcite|correct|kegg}}

| KEGG = D03692

| ChEMBL_Ref = {{ebicite|changed|EBI}}

| ChEMBL = 1201666

| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}}

| ChemSpiderID = none

<!-- Chemical data -->

| C=288 | H=448 | N=80 | O=110 | S=6

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

Brand name: '''Refludan''', Generic: Lepirudin rDNA for injection.

Lepirudin is a recombinant [[hirudin]]<ref name="AskariLincoff2009">{{cite book| vauthors = Askari AT, Lincoff AM |title=Antithrombotic Drug Therapy in Cardiovascular Disease|url=https://books.google.com/books?id=iadLoXoQkWEC&pg=PA440|access-date=30 October 2010|date=October 2009|publisher=Springer|isbn=978-1-60327-234-6|pages=440–}}</ref> 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 [[heparin]]s (unfractionated or [[Low-molecular-weight heparin|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.<ref>{{cite web |url=http://www.ashp.org/menu/DrugShortages/DrugsNoLongerAvailable/Bulletin.aspx?id=924 |title=Discontinued Drug Bulletin: Lepirudin Injection | work = American Society of Health System Pharmacists (ASHP) | date = 23 May 2012 |url-status=dead |archive-url=https://web.archive.org/web/20140723174035/http://www.ashp.org/menu/DrugShortages/DrugsNoLongerAvailable/bulletin.aspx?id=924 |archive-date=2014-07-23}} </ref>

== References ==

== Further reading ==

{{refbegin}}

* {{cite journal | vauthors = Smythe MA, Stephens JL, Koerber JM, Mattson JC | title = A comparison of lepirudin and argatroban outcomes | journal = Clinical and Applied Thrombosis/Hemostasis | volume = 11 | issue = 4 | pages = 371–374 | date = October 2005 | pmid = 16244762 | doi = 10.1177/107602960501100403 | doi-access = free }}

* {{cite journal | vauthors = Tardy B, Lecompte T, Boelhen F, Tardy-Poncet B, Elalamy I, Morange P, Gruel Y, Wolf M, François D, Racadot E, Camarasa P, Blouch MT, Nguyen F, Doubine S, Dutrillaux F, Alhenc-Gelas M, Martin-Toutain I, Bauters A, Ffrench P, de Maistre E, Grunebaum L, Mouton C, Huisse MG, Gouault-Heilmann M, Lucke V | display-authors = 6 | title = Predictive factors for thrombosis and major bleeding in an observational study in 181 patients with heparin-induced thrombocytopenia treated with lepirudin | journal = Blood | volume = 108 | issue = 5 | pages = 1492–1496 | date = September 2006 | pmid = 16690967 | doi = 10.1182/blood-2006-02-001057 | doi-access = free }}

* {{cite journal | vauthors = Lubenow N, Eichler P, Lietz T, Greinacher A | title = 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 | journal = Journal of Thrombosis and Haemostasis | volume = 3 | issue = 11 | pages = 2428–2436 | date = November 2005 | pmid = 16241940 | doi = 10.1111/j.1538-7836.2005.01623.x | doi-access = free }}

{{refend}}

== External links ==

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