Comparison of the drug-drug interactions potential of ibrutinib and acalabrutinib via inhibition of UDP-glucuronosyltransferase.
Acalabrutinib
Drug-drug interaction
Ibrutinib
UDP-glucuronosyltransferase
Journal
Toxicology and applied pharmacology
ISSN: 1096-0333
Titre abrégé: Toxicol Appl Pharmacol
Pays: United States
ID NLM: 0416575
Informations de publication
Date de publication:
01 08 2021
01 08 2021
Historique:
received:
31
01
2021
revised:
18
05
2021
accepted:
21
05
2021
pubmed:
27
5
2021
medline:
10
8
2021
entrez:
26
5
2021
Statut:
ppublish
Résumé
Ibrutinib and acalabrutinib are two Bruton's tyrosine kinase (BTK) inhibitors which have gained Food and Drug Administration (FDA) approval for the treatment of various B cell malignancies. Herein, we investigated the effects of the two drugs on UDP-glucuronosyltransferase (UGT) activities to evaluate their potential risk for drug-drug interactions (DDIs) via UGT inhibition. Our data indicated that ibrutinib exerted broad inhibition on most of UGTs, including a potent competitive inhibition against UGT1A1 with a K
Identifiants
pubmed: 34038714
pii: S0041-008X(21)00202-7
doi: 10.1016/j.taap.2021.115595
pii:
doi:
Substances chimiques
Benzamides
0
Isoenzymes
0
Piperidines
0
Pyrazines
0
ibrutinib
1X70OSD4VX
Glucuronosyltransferase
EC 2.4.1.17
acalabrutinib
I42748ELQW
Adenine
JAC85A2161
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
115595Informations de copyright
Copyright © 2021 Elsevier Inc. All rights reserved.