Pharmacological characterization of linaprazan glurate (X842), a novel potassium-competitive acid blocker, <i>in vitro</i> and <i>in vivo</i>.

ABSTRACT:

Introduction

The aim of this study is to characterize the pharmacology of linaprazan glurate (X842), an ethyl ester prodrug of linaprazan (a novel potassium-competitive acid blocker), in animal species in vitro and in vivo to achieve a better pharmacological profile.

Methods

Pharmacokinetic profiling, hydrogen (H⁺)/potassium (K⁺)-ATPase inhibition, and gastric acid inhibition experiments were performed.

Results

X842 was rapidly absorbed with a very low plasma concentration. X842 was rapidly transformed by enzymatic cleavage into its active metabolite, linaprazan, as shown by the half-life, maximum concentration, and area under the concentration-time curve of the two substances. Selective inhibition of the gastric H⁺/K

SUBMITTER: Lu M 

PROVIDER: S-EPMC12446003 | biostudies-literature | 2025

REPOSITORIES: biostudies-literature