Esterase Activities in the Blood, Liver and Intestine of Several Preclinical Species and Humans

Overview

Journal Drug Metab Lett

Publisher Bentham Science Publishers

Specialties Endocrinology
Pharmacology

Date 2009 Jul 16

PMID 19601867

Citations 33

Authors

Loren M Berry

Lance Wollenberg

Zhiyang Zhao

Affiliations

Soon will be listed here.

Abstract

Species and tissue differences in the activity of three major classes of esterases, carboxylesterase (CE), butyrylcholinesterase (BChE) and paraoxonase (PON), were studied. Substantial species differences in activity of these esterases were observed between the mouse, rat, dog monkey and human. Such species differences must be considered when using these preclinical species to optimize the pharmacokinetic properties of ester compounds intended for human use.

Citing Articles

Characterizing the Hepatic Metabolic Pathway of Ketone Ester and Subsequent Metabolites Using Human and Rat Liver Fractions.

Panse N, Gerk P AAPS J. 2025; 27(2):65.

PMID: 40087222 DOI: 10.1208/s12248-025-01044-7.

Fluorescent cyclopropyl ester probes are efficiently cleaved by endogenous carboxylesterase in mouse blood: implications for preclinical fluorescence imaging.

Sanders H, Atkinson K, Smith B Supramol Chem. 2025; 34(11-12):484-490.

PMID: 40046405 PMC: 11882149. DOI: 10.1080/10610278.2024.2388731.

Synthesis and Evaluation of Benzylic F-Labeled -Biphenylalkynyl Nipecotic Acid Derivatives for PET Imaging of GABA Transporter 1.

Knippenberg N, Bauwens M, Florea A, Rudi S, Schijns O, Hoogland G ACS Chem Neurosci. 2025; 16(4):711-722.

PMID: 39878351 PMC: 11843609. DOI: 10.1021/acschemneuro.4c00782.

Assessment of Purity, Stability, and Pharmacokinetics of NGP-1, a Novel Prodrug of GS441254 with Potential Anti-SARS-CoV-2 Activity, Using Liquid Chromatography.

Sun C, Liu B, Zhou F, Zheng Q, Dai C, Wei W Molecules. 2023; 28(15).

PMID: 37570604 PMC: 10420250. DOI: 10.3390/molecules28155634.

A Comparison of the Pharmacokinetics and Safety of Dapagliflozin Formate, an Ester Prodrug of Dapagliflozin, to Dapagliflozin Propanediol Monohydrate in Healthy Subjects.

Kim H, Lee S, Sung S, Kim E, Jang I, Chung J Drug Des Devel Ther. 2023; 17:1203-1210.

PMID: 37113469 PMC: 10128151. DOI: 10.2147/DDDT.S404182.