| dbo:abstract |
Glucarpidase (Voraxaze) is a medication used for the treatment of elevated levels of methotrexate (defined as 1 micromol/L) during treatment of cancer patients who have impaired kidney function (and thus cannot reduce the drug to safe levels sufficiently after the drug has been given). Glucarpidase is an enzyme that inactivates methotrexate rapidly after injection. Because this agent reduces systemic levels of methotrexate and could therefore interfere with efficacy, it is not recommended for use in patients with normal or only slightly impaired kidney function or in whom serum levels are normal. The main antidote for methotrexate overdoses prior to the approval of this drug were high doses of folinic acid. However, this agent was not always sufficient at preventing kidney failure due to methotrexate. Glucarpidase also degrades folinic acid so the two should not be used together (within two hours of one another). Glucarpidase, a recombinant form of the bacterial enzyme carboxypeptidase G2 converts methotrexate into glutamate and 2,4-diamino-N(10)-methylpteroic acid. These are generally much less toxic and are excreted largely by the liver. One case series in children has found that high-dose methotrexate therapy can be resumed after an instance of methotrexate-induced acute kidney injury successfully treated with glucarpidase. Adverse effects include mild and include numbness, tingling, flushing, nausea, vomiting, itching, and headache. (en) La glucarpidasa es una carboxipeptidasa (carboxipeptidasa-G2 o CPDG2) encontrada originalmente en una bacteria del género Pseudomonas, cuya función es reducir los niveles de metotrexato en el organismo mediante su hidrólisis. (es) グルカルピダーゼ（Glucarpidase）はメトトレキサート (MTX) を分解する酵素である。腎機能低下等の基礎疾患により薬剤排泄能が低い患者患者にMTXを用いた治療を行う際、その血中濃度が異常に上昇した場合の解毒薬として点滴静注用製剤の形で用いられる。本剤はMTXの薬効を阻害する可能性があるため、腎機能が正常に近い患者やMTX血清濃度が正常な患者への使用は推奨されない。本剤が承認される以前のMTXに対する主な解毒薬は高用量のフォリン酸だったが、排泄されたMTXの尿細管への沈着による腎不全が起こる可能性があった。グルカルピダーゼはフォリン酸も分解するため、この二剤を互いに2時間以内に投与してはならない。 (ja) |
| dbo:alternativeName |
Voraxaze (en) |
| dbo:casNumber |
9074-87-7 |
| dbo:chEMBL |
1863515 |
| dbo:drugbank |
DB08898 |
| dbo:fdaUniiCode |
2GFP9BJD79 |
| dbo:kegg |
D10260 |
| dbo:medlinePlus |
a613009 |
| dbo:thumbnail |
wiki-commons:Special:FilePath/Glutamate_carboxypeptidase_1CG2.png?width=300 |
| dbo:wikiPageExternalLink |
https://druginfo.nlm.nih.gov/drugportal/name/glucarpidase |
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| dbo:wikiPageLength |
7068 (xsd:nonNegativeInteger) |
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| dbo:wikiPageWikiLink |
dbr:Cancer dbr:Enzyme dbr:Committee_for_Medicinal_Products_for_Human_Use dbc:Chemotherapeutic_adjuvants dbc:Orphan_drugs dbr:European_Medicines_Agency dbr:Folinic_acid dbr:Kidney_failure dbr:Recombinant_DNA dbr:Headache dbr:Methotrexate dbr:Medication dbr:Intravenous dbr:Glutamate dbr:Renal_insufficiency dbr:Carboxypeptidase_G2 |
| dbp:atcPrefix |
V03AF09 (en) |
| dbp:c |
1950 (xsd:integer) |
| dbp:casNumber |
9074 (xsd:integer) |
| dbp:chembl |
1863515 (xsd:integer) |
| dbp:chemspiderid |
none (en) |
| dbp:dailymedid |
Glucarpidase (en) |
| dbp:drugbank |
DB08898 (en) |
| dbp:h |
3157 (xsd:integer) |
| dbp:iupacName |
Recombinant glutamate carboxypeptidase (en) |
| dbp:iupharLigand |
7450 (xsd:integer) |
| dbp:kegg |
D10260 (en) |
| dbp:legalEu |
Rx-only (en) |
| dbp:legalUs |
Rx-only (en) |
| dbp:medlineplus |
a613009 (en) |
| dbp:n |
543 (xsd:integer) |
| dbp:o |
599 (xsd:integer) |
| dbp:routesOfAdministration |
dbr:Intravenous |
| dbp:s |
7 (xsd:integer) |
| dbp:tradename |
Voraxaze (en) |
| dbp:unii |
2 (xsd:integer) |
| dbp:wikiPageUsesTemplate |
dbt:Cite_web dbt:Infobox_drug dbt:Portal_bar dbt:Reflist dbt:PDB dbt:Drugs.com dbt:Medcn |
| dcterms:subject |
dbc:Chemotherapeutic_adjuvants dbc:Orphan_drugs |
| gold:hypernym |
dbr:Drug |
| rdf:type |
owl:Thing dul:ChemicalObject dbo:ChemicalSubstance wikidata:Q8386 yago:WikicatChemotherapeuticAdjuvants yago:Addition102679415 yago:Additive102679788 yago:Adjuvant102680947 yago:Component103081021 yago:Object100002684 yago:Part103892891 yago:PhysicalEntity100001930 dbo:Drug |
| rdfs:comment |
La glucarpidasa es una carboxipeptidasa (carboxipeptidasa-G2 o CPDG2) encontrada originalmente en una bacteria del género Pseudomonas, cuya función es reducir los niveles de metotrexato en el organismo mediante su hidrólisis. (es) グルカルピダーゼ（Glucarpidase）はメトトレキサート (MTX) を分解する酵素である。腎機能低下等の基礎疾患により薬剤排泄能が低い患者患者にMTXを用いた治療を行う際、その血中濃度が異常に上昇した場合の解毒薬として点滴静注用製剤の形で用いられる。本剤はMTXの薬効を阻害する可能性があるため、腎機能が正常に近い患者やMTX血清濃度が正常な患者への使用は推奨されない。本剤が承認される以前のMTXに対する主な解毒薬は高用量のフォリン酸だったが、排泄されたMTXの尿細管への沈着による腎不全が起こる可能性があった。グルカルピダーゼはフォリン酸も分解するため、この二剤を互いに2時間以内に投与してはならない。 (ja) Glucarpidase (Voraxaze) is a medication used for the treatment of elevated levels of methotrexate (defined as 1 micromol/L) during treatment of cancer patients who have impaired kidney function (and thus cannot reduce the drug to safe levels sufficiently after the drug has been given). Glucarpidase is an enzyme that inactivates methotrexate rapidly after injection. Because this agent reduces systemic levels of methotrexate and could therefore interfere with efficacy, it is not recommended for use in patients with normal or only slightly impaired kidney function or in whom serum levels are normal. The main antidote for methotrexate overdoses prior to the approval of this drug were high doses of folinic acid. However, this agent was not always sufficient at preventing kidney failure due to m (en) |
| rdfs:label |
Glucarpidase (en) Glucarpidasa (es) グルカルピダーゼ (ja) |
| owl:sameAs |
freebase:Glucarpidase yago-res:Glucarpidase wikidata:Glucarpidase dbpedia-es:Glucarpidase dbpedia-ja:Glucarpidase dbpedia-sh:Glucarpidase dbpedia-sr:Glucarpidase https://global.dbpedia.org/id/4keSK |
| prov:wasDerivedFrom |
wikipedia-en:Glucarpidase?oldid=1084387306&ns=0 |
| foaf:depiction |
wiki-commons:Special:FilePath/Glutamate_carboxypeptidase_1CG2.png |
| foaf:isPrimaryTopicOf |
wikipedia-en:Glucarpidase |
| is dbo:wikiPageRedirects of |
dbr:ATC_code_V03AF09 dbr:ATCvet_code_QV03AF09 dbr:Voraxaze |
| is dbo:wikiPageWikiLink of |
dbr:ATC_code_V03AF09 dbr:ATCvet_code_QV03AF09 dbr:ATC_code_V03 dbr:List_of_drugs:_G dbr:Voraxaze |
| is foaf:primaryTopic of |
wikipedia-en:Glucarpidase |
