14C-Z-215

14C-Z-215 is the carbon-14 radiolabeled form of azeloprazole sodium (also known as Z-215 or E3710), a potent and orally active proton pump inhibitor (PPI) developed by Zeria Pharmaceutical. It is being investigated for the treatment of acid-related disorders, including reflux esophagitis and gastroesophageal reflux disease (GERD). The drug functions by irreversibly inhibiting the H+,K+-ATPase enzyme (the 'proton pump') in gastric parietal cells with an IC50 of 0.28 uM, thereby suppressing the secretion of gastric acid. A key pharmacological advantage of azeloprazole is its primary metabolism via the CYP3A4 pathway, which makes its clinical efficacy independent of CYP2C19 genetic polymorphisms—a factor that often causes therapeutic variability in other PPIs. The 14C-labeled version was specifically utilized in Phase I clinical trials to conduct mass balance and metabolism studies, providing detailed information on the drug's absorption, distribution, metabolism, and excretion (ADME) profile in humans.

Other names

14C-azeloprazole sodium