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Hirosawa K, Fukami T, Tashiro K, et al. Role of Human Arylacetamide Deacetylase (AADAC) on Hydrolysis of Eslicarbazepine Acetate and Effects of . Drug Metab Dispos. 2021;49(4):322-329doi: 10.1124/dmd.120.000295.
Hirosawa, K., Fukami, T., Tashiro, K., Sakai, Y., Kisui, F., Nakano, M., & Nakajima, M. (2021). Role of Human Arylacetamide Deacetylase (AADAC) on Hydrolysis of Eslicarbazepine Acetate and Effects of . Drug metabolism and disposition: the biological fate of chemicals, 49(4), 322-329. https://doi.org/10.1124/dmd.120.000295
Hirosawa, Keiya, et al. "Role of Human Arylacetamide Deacetylase (AADAC) on Hydrolysis of Eslicarbazepine Acetate and Effects of ." Drug metabolism and disposition: the biological fate of chemicals vol. 49,4 (2021): 322-329. doi: https://doi.org/10.1124/dmd.120.000295
Hirosawa K, Fukami T, Tashiro K, Sakai Y, Kisui F, Nakano M, Nakajima M. Role of Human Arylacetamide Deacetylase (AADAC) on Hydrolysis of Eslicarbazepine Acetate and Effects of . Drug Metab Dispos. 2021 Apr;49(4):322-329. doi: 10.1124/dmd.120.000295. Epub 2021 Jan 14. PMID: 33446525.
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Drug Metab Dispos. 2021 Apr;49(4):322-329. doi: 10.1124/dmd.120.000295. Epub 2021 Jan 14.

Role of Human Arylacetamide Deacetylase (AADAC) on Hydrolysis of Eslicarbazepine Acetate and Effects of .

Drug metabolism and disposition: the biological fate of chemicals

Keiya Hirosawa, Tatsuki Fukami, Kiyomichi Tashiro, Yoshiyuki Sakai, Fumiya Kisui, Masataka Nakano, Miki Nakajima

Affiliations

  1. Drug Metabolism and Toxicology, Faculty of Pharmaceutical Sciences, Kanazawa University, Kakuma-machi, Kanazawa, Japan (K.H., T.F., K.T., Y.S., F.K., Ma.N., Mi.N.); and WPI Nano Life Science Institute, Kakuma-machi, Kanazawa, Japan (T.F., Ma.N., Mi.N.).
  2. Drug Metabolism and Toxicology, Faculty of Pharmaceutical Sciences, Kanazawa University, Kakuma-machi, Kanazawa, Japan (K.H., T.F., K.T., Y.S., F.K., Ma.N., Mi.N.); and WPI Nano Life Science Institute, Kakuma-machi, Kanazawa, Japan (T.F., Ma.N., Mi.N.) [email protected].

PMID: 33446525 DOI: 10.1124/dmd.120.000295

Abstract

Human arylacetamide deacetylase (AADAC) plays a role in the detoxification or activation of drugs and is sometimes involved in the incidence of toxicity by catalyzing hydrolysis reactions. AADAC prefers compounds with relatively small acyl groups, such as acetyl groups. Eslicarbazepine acetate, an antiepileptic drug, is a prodrug rapidly hydrolyzed to eslicarbazepine. We sought to clarify whether AADAC might be responsible for the hydrolysis of eslicarbazepine acetate. Eslicarbazepine acetate was efficiently hydrolyzed by human intestinal and liver microsomes and recombinant human AADAC. The hydrolase activities in human intestinal and liver microsomes were inhibited by epigallocatechin gallate, a specific inhibitor of AADAC, by 82% and 88% of the control, respectively. The hydrolase activities in liver microsomes from 25 human livers were significantly correlated (

Copyright © 2021 by The American Society for Pharmacology and Experimental Therapeutics.

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