In vitro evaluation of fenfluramine and norfenfluramine as victims of drug interactions.
antiepileptics
cytochrome P450
drug transport
drug-drug interactions
Journal
Pharmacology research & perspectives
ISSN: 2052-1707
Titre abrégé: Pharmacol Res Perspect
Pays: United States
ID NLM: 101626369
Informations de publication
Date de publication:
06 2022
06 2022
Historique:
received:
11
03
2022
accepted:
06
04
2022
entrez:
23
5
2022
pubmed:
24
5
2022
medline:
25
5
2022
Statut:
ppublish
Résumé
Fenfluramine (FFA) has potent antiseizure activity in severe, pharmacoresistant childhood-onset developmental and epileptic encephalopathies (e.g., Dravet syndrome). To assess risk of drug interaction affecting pharmacokinetics of FFA and its major metabolite, norfenfluramine (nFFA), we conducted in vitro metabolite characterization, reaction phenotyping, and drug transporter-mediated cellular uptake studies. FFA showed low in vitro clearance in human liver S9 fractions and in intestinal S9 fractions in all three species tested (t
Identifiants
pubmed: 35599345
doi: 10.1002/prp2.958
pmc: PMC9124820
doi:
Substances chimiques
Norfenfluramine
1886-26-6
Fenfluramine
2DS058H2CF
Cytochrome P-450 Enzyme System
9035-51-2
Types de publication
Journal Article
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
e00958Informations de copyright
© 2022 Zogenix, Inc. Pharmacology Research & Perspectives published by John Wiley & Sons Ltd, British Pharmacological Society and American Society for Pharmacology and Experimental Therapeutics.
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