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Latest revision as of 20:11, 20 December 2023 edit undoJJMC89 bot III (talk | contribs)Bots, Administrators3,681,435 editsm Moving Category:Takeda Pharmaceutical Company brands to Category:Drugs developed by Takeda Pharmaceutical Company per Misplaced Pages:Categories for discussion/Log/2023 December 9#Category:AstraZeneca brands |
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{{Short description|Medication}} |
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{{Drugbox |
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{{Drugbox |
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| verifiedrevid = 402709065 |
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| Watchedfields = changed |
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| IUPAC_name = tissue factor pathway inhibitor (human)-(20-79)-peptide (modified on reactive bond region Kunitz inhibitor 1 domain containing fragment)<!--as reported in WHO Drug Information; not actual IUPAC name--> |
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| verifiedrevid = 414410253 |
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| image = |
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| alt = |
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<!-- Clinical data --> |
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| CAS_number = 460738-38-9 |
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| tradename = Kalbitor |
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| ATC_prefix = B02 |
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| ATC_suffix = AB |
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| synonyms = DX-88 |
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| Drugs.com = {{drugs.com|monograph|ecallantide}} |
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| PubChem = 44152182 |
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| DailyMedID = Ecallantide |
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| DrugBank = |
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| licence_US = Ecallantide |
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| C=305|H=442|N=88|O=91|S=8 |
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| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> |
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| molecular_weight = 7053.83 g/mol (7053 ]) |
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| pregnancy_category = |
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| bioavailability = |
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| legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled --> |
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| protein_bound = |
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| legal_CA = <!-- Schedule I, II, III, IV, V, VI, VII, VIII --> |
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| metabolism = |
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| legal_UK = <!-- GSL, P, POM, CD, or Class A, B, C --> |
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| elimination_half-life = 1.5–2.5 hours |
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| legal_US = Rx-only |
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| excretion = |
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| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X --> |
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| pregnancy_US = <!-- A / B / C / D / X --> |
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| pregnancy_category= C |
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| legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled--> |
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| legal_CA = <!-- Schedule I, II, III, IV, V, VI, VII, VIII --> |
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| legal_UK = <!-- GSL, P, POM, CD, or Class A, B, C --> |
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| legal_US = Rx-only |
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| licence_US = ECALLANTIDE |
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| legal_status = |
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| routes_of_administration = ] |
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| routes_of_administration = ] |
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<!-- Pharmacokinetic data --> |
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| elimination_half-life = 1.5–2.5 hours |
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| excretion = ] |
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<!-- Identifiers --> |
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| IUPHAR_ligand = 6955 |
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| CAS_number_Ref = {{cascite|correct|??}} |
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| CAS_number = 460738-38-9 |
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| ATC_prefix = B06 |
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| ATC_suffix = AC03 |
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| PubChem = 118984459 |
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| DrugBank = DB05311 |
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| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
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| UNII_Ref = {{fdacite|changed|FDA}} |
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| UNII = 5Q6TZN2HNM |
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| ChEMBL_Ref = {{ebicite|changed|EBI}} |
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| ChEMBL = 1201837 |
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| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} |
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| ChemSpiderID = 34983390 |
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<!-- Chemical data --> |
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| IUPAC_name = tissue factor pathway inhibitor (human)-(20-79)-peptide (modified on reactive bond region Kunitz inhibitor 1 domain containing fragment)<!--as reported in WHO Drug Information; not actual IUPAC name --> |
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| C=305 | H=442 | N=88 | O=91 | S=8 |
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'''Ecallantide''' (trade name '''Kalbitor''', investigational name '''DX-88''') is an inhibitor of the protein ] used for ] (HAE) and in the prevention of blood loss in ].<ref name=Lehmann>{{cite journal |author=Lehmann A |title=Ecallantide (DX-88), a plasma kallikrein inhibitor for the treatment of hereditary angioedema and the prevention of blood loss in on-pump cardiothoracic surgery |journal=Expert Opin Biol Ther |volume=8 |issue=8 |pages=1187–99 |year=2008 |month=August |pmid=18613770 |doi=10.1517/14712598.8.8.1187 |url=}}</ref> It is a 60-] ] which was developed from a ] through ] to ] inhibiting kallikrein.<ref name=Lehmann/> On November 27, 2009, ecallantide was approved by the ] for the treatment of acute attacks of hereditary angioedema.<ref name=Waknine>{{cite web |url=http://www.medscape.com/viewarticle/713401 |title=FDA Approves Ecallantide for Hereditary Angioedema |last=Waknine |first=Yael |publisher=] |date=December 4, 2009 |accessdate=2009-12-07}}</ref> |
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'''Ecallantide''' (trade name '''Kalbitor''') is a ] used for the treatment of ] (HAE) and in the prevention of blood loss in ].<ref name=Lehmann>{{cite journal | vauthors = Lehmann A | title = Ecallantide (DX-88), a plasma kallikrein inhibitor for the treatment of hereditary angioedema and the prevention of blood loss in on-pump cardiothoracic surgery | journal = Expert Opinion on Biological Therapy | volume = 8 | issue = 8 | pages = 1187–99 | date = August 2008 | pmid = 18613770 | doi = 10.1517/14712598.8.8.1187 | s2cid = 72623604 }}</ref> It is an inhibitor of the protein ] and a 60-] ] which was developed from a ] through ] to ] inhibiting kallikrein.<ref name=Lehmann/> |
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If approved for cardiothoracic surgery, it could become a replacement for ],{{Citation needed|date=November 2010}} which was withdrawn in 2007 after being shown to cause complications. |
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==See also== |
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==Medical uses== |
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* ], another drug for the treatment of HEA |
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==References== |
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===Angioedema=== |
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On November 27, 2009, ecallantide was approved by the ] for the treatment of acute attacks of hereditary angioedema for persons over 16 years of age.<ref name=Waknine>{{cite web |url=http://www.medscape.com/viewarticle/713401 |title=FDA Approves Ecallantide for Hereditary Angioedema | vauthors = Waknine Y |publisher=] |date=December 4, 2009 |access-date=2009-12-07}}</ref> A single dose requires three separate injections, which are given ].<ref name="2013 Nursebook">{{cite book |title=2013 Nurse's Drug Handbook |date=2013 |publisher=Jones & Bartlett Publishers |location=Burlington, MA |page=391 |edition=12th | isbn = 978-1-284-19536-1 }}</ref> |
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{{reflist}} |
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* , Dyax Corp., accessed February 11, 2009 |
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* http://www.medscape.com/viewarticle/587866?src=mp&spon=38&uac=33931AT{{dead link|date=July 2010}}, accessed February 11, 2009 |
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Ecallantide does not appear to be efficacious for the treatment of angioedema due to ].<ref>{{cite journal | vauthors = Lewis LM, Graffeo C, Crosley P, Klausner HA, Clark CL, Frank A, Miner J, Iarrobino R, Chyung Y | display-authors = 6 | title = Ecallantide for the acute treatment of angiotensin-converting enzyme inhibitor-induced angioedema: a multicenter, randomized, controlled trial | journal = Annals of Emergency Medicine | volume = 65 | issue = 2 | pages = 204–13 | date = February 2015 | pmid = 25182544 | doi = 10.1016/j.annemergmed.2014.07.014 }}</ref><ref>{{cite journal | vauthors = Scalese MJ, Reinaker TS | title = Pharmacologic management of angioedema induced by angiotensin-converting enzyme inhibitors | journal = American Journal of Health-System Pharmacy | volume = 73 | issue = 12 | pages = 873–9 | date = June 2016 | pmid = 27261237 | doi = 10.2146/ajhp150482 }}</ref> |
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==Adverse effects== |
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The most common adverse effects are headache, ], ] and ]. Less common, but observed in more than 5% of patients in clinical trials, are ]s, fever, vomiting, itching and upper ]. Up to 4% of patients showed ], which led to a ] in the US.<ref name="Dyax">{{cite web |author=Dyax Corp. |year=2009 |title=Full prescibing information Kalbitor |url=http://www.kalbitor.com/pdf/KalbitorFullPrescribingInformation.pdf |access-date=2010-05-02}}</ref> |
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== Interactions == |
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{{as of|2011}}, no interaction studies have been conducted.<ref name="Dyax" /> |
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==Mechanism of action== |
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HAE is caused by a ] of the ] gene. Defective or missing C1-inhibitor permits activation of kallikrein, a ] that is responsible for liberating ] from its precursor ].<ref>{{cite journal | vauthors = Bhoola KD, Figueroa CD, Worthy K | title = Bioregulation of kinins: kallikreins, kininogens, and kininases | journal = Pharmacological Reviews | volume = 44 | issue = 1 | pages = 1–80 | date = March 1992 | pmid = 1313585 }}</ref><ref name="OffermannsRosenthal2008">{{cite book | vauthors = Offermanns S, Rosenthal W |title=Encyclopedia of Molecular Pharmacology|url=https://books.google.com/books?id=iwwo5gx8aX8C&pg=PA673|access-date=11 December 2010|year=2008|publisher=Springer|isbn=978-3-540-38916-3|pages=673–}}</ref> An excess of bradykinin leads to fluid leakage from blood vessels, causing swelling of tissues typical of HAE. |
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Ecallantide suppresses this pathogenetic mechanism by selectively and reversibly inhibiting the activity of plasma kallikrein.<ref name="Dyax" /> Ecallantide's ] (Ki) for kallikrein is 25 picoMolar, indicating high affinity.<ref name="NCATS at NIH">{{cite web |title=NCATS Inxight: Drugs — ECALLANTIDE |url=https://drugs.ncats.io/substance/5Q6TZN2HNM |website=drugs.ncats.io |publisher=National Center for Advancing Translational Sciences (NCATS) |access-date=15 May 2019 |language=en}}</ref> |
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== References == |
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{{reflist}} |
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{{Other hematological agents}} |
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{{blood-drug-stub}} |
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