Volume – 97 , Issue-1 , Page Number – 521-529, Published date – 08/06/2026
Affiliations
Clinical Trial Center of the First Affiliated Hospital of Bengbu Medical University, Bengbu, Anhui, China, 233000
School of Public Fundamentals, Bengbu Medical University, Bengbu, China, 233000
Anhui Province Jointly-Constructed Discipline Key Laboratory of Innovative Drugs Pharmaceutical Research and Clinical Evaluation, Anhui, Bengbu, 233000
Correspondence
Dr. Huan Zhou, Clinical Trial Center of the First Affiliated Hospital of Bengbu Medical University, Bengbu, Anhui, China, 233000. Email: zhouhuan@bbmc.edu.cn.
Abstract
X842 is a novel H+ -K+ -ATP enzyme inhibitor for treating gastroesophageal reflux disease (GERD) and is currently undergoing phase I clinical trials in China. In this study, six healthy Chinese male volunteers received 50 mg (100 µCi) of radiolabelled [14C]X842 orally to study its pharmacokinetics, mass balance, metabolism, and excretion pathways. The results revealed that oral [14C]X842 was rapidly absorbed, with an average peak time of 1 h. The half-life of the plasma radioactive concentration was 34.1 h, and the cumulative excretion of radioactive-related substances was 93.89 ± 2.48% at 264 h, with a urinary excretion of 31.82 ± 5.23% and a feces excretion of 62.07 ± 5.69%. A total of 13 metabolites were detected in plasma, urine, and feces via high-resolution mass spectrometry, and no original drug X842 was detected. The main metabolic pathway of X842 is hydrolysis to generate linaprazan, linaprazan oxidation, oxidation and glucuronide binding.
Keywords
X842, 14C, Metabolism, Pharmacokinetics, Excretion