Drug intelligence / Profile preview

desmethyl tegoprazan

Development stage
Preclinical
Lead developer
HK inno.N Corporation
Modality
Small Molecules
Administration
Oral
01

Overview

Desmethyl tegoprazan is the principal *active metabolite* of tegoprazan, a novel potassium-competitive acid blocker (P-CAB) used primarily for acid-related gastrointestinal disorders. Desmethyl tegoprazan forms via hepatic metabolism of tegoprazan, most likely through CYP3A4-mediated N-demethylation of the parent drug. Although chemically similar, desmethyl tegoprazan possesses one less methyl group on the benzimidazole nitrogen compared to the parent compound. Its pharmacological activity mimics that of tegoprazan, reversibly and competitively inhibiting the gastric H+/K+-ATPase (proton pump) in parietal cells and thereby suppressing gastric acid secretion. The clinical efficacy and safety data for tegoprazan principally reflect the parent drug, with the metabolite contributing to its acid-suppressing effects[1].

Other names
M1 metabolite of tegoprazanM-1 metabolite of tegoprazanM 1 metabolite of tegoprazantegoprazan M1
02

Targets

ATP4A (Potassium–transporting ATPase alpha chain 1)

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