UGT2B10 is the Major UDP-Glucuronosyltransferase 2B Isoform Involved in the Metabolism of Lamotrigine and is Implicated in the Drug-Drug Interaction with Valproic Acid.
UDP-glucuronosyltransferase
UGT2B10
drug metabolism
lamotrigine
reaction phenotyping
Journal
The AAPS journal
ISSN: 1550-7416
Titre abrégé: AAPS J
Pays: United States
ID NLM: 101223209
Informations de publication
Date de publication:
25 Sep 2024
25 Sep 2024
Historique:
received:
23
07
2024
accepted:
08
09
2024
medline:
26
9
2024
pubmed:
26
9
2024
entrez:
25
9
2024
Statut:
epublish
Résumé
Lamotrigine is a phenyltriazine anticonvulsant that is primarily metabolized by phase II UDP-glucuronosyltransferases (UGT) to a quaternary N2-glucuronide, which accounts for ~ 90% of the excreted dose in humans. While there is consensus that UGT1A4 plays a predominant role in the formation of the N2-glucuronide, there is compelling evidence in the literature to suggest that the metabolism of lamotrigine is catalyzed by another UGT isoform. However, the exact identity of the UGT isoform that contribute to the formation of this glucuronide remains uncertain. In this study, we harnessed a robust reaction phenotyping strategy to delineate the identities and its associated fraction metabolized (f
Identifiants
pubmed: 39322784
doi: 10.1208/s12248-024-00978-8
pii: 10.1208/s12248-024-00978-8
doi:
Substances chimiques
Lamotrigine
U3H27498KS
Glucuronosyltransferase
EC 2.4.1.17
UGT2B10 protein, human
EC 2.4.1.-
Anticonvulsants
0
Valproic Acid
614OI1Z5WI
Isoenzymes
0
Glucuronides
0
Triazines
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
107Informations de copyright
© 2024. The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists.
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