biostudies-literatureUnknown16Lu M<h4>Introduction</h4>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 <i>in vitro</i> and <i>in vivo</i> to achieve a better pharmacological profile.<h4>Methods</h4>Pharmacokinetic profiling, hydrogen (H⁺)/potassium (K⁺)-ATPase inhibition, and gastric acid inhibition experiments were performed.<h4>Results</h4>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<supFrontiers in pharmacology1636523https://www.ebi.ac.uk/biostudies/studies/S-EPMC12446003biostudies-literaturePharmacological characterization of linaprazan glurate (X842), a novel potassium-competitive acid blocker, &lt;i&gt;in vitro&lt;/i&gt; and &lt;i&gt;in vivo&lt;/i&gt;.PMC12446003Zhou LLu MHe YCui YXiu JLi NHu PfalsePharmacological characterization of linaprazan glurate (X842), a novel potassium-competitive acid blocker, &lt;i&gt;in vitro&lt;/i&gt; and &lt;i&gt;in vivo&lt;/i&gt;.<h4>Introduction</h4>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 <i>in vitro</i> and <i>in vivo</i> to achieve a better pharmacological profile.<h4>Methods</h4>Pharmacokinetic profiling, hydrogen (H⁺)/potassium (K⁺)-ATPase inhibition, and gastric acid inhibition experiments were performed.<h4>Results</h4>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<sup2025-01-01T00:00:00Z20252026-06-03T16:57:07.765Z2026-04-29T03:12:33.248ZS-EPMC124460034097849010.3389/fphar.2025.1636523