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| Other names | Z-215; E3710 |
| Drug class | Proton pump inhibitor |
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| Formula | C22H27N3O4S |
| Molar mass | 429.54 g·mol−1 |
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Azeloprazole (also known asZ-215 orE3710) is a drug under investigation for acid-related medical conditions responsive to suppressing the production of stomach acid. It is considered a member of theproton pump inhibitor class of medications.
Azeloprazole is an acid suppressing drug being studied for the treatment ofgastroesophageal reflux disease (GERD).[2]
Azeloprazole, like other drugs of theproton pump inhibitor class, works by inhibiting thehydrogen potassium adenosine triphosphatase (H+/K+ ATPase) acid pump. The term "proton pump inhibitor" comes from the recognition ofhydrogencations as a singleproton. H+/K+ ATPase pumps, found inparietal cells in the stomach, are ultimately responsible for secreting acid into the lumen of thestomach. By inhibiting the secretion of acid, proton pump inhibitors are considered useful in treating "acid-related diseases" (e.g.gastroesophageal reflux disease).[3]
Azeloprazole is soluble inDMSO.[4]
Azeloprazole was designed in Japan withpharmacogenomics in mind. Some drugs in the proton pump inhibitor class are metabolized by the hepatic enzymeCYP2C19. Some individuals, such as people of Japanese ancestry, are more likely to be poor CYP2C19 metabolizers; that is, their ability to metabolize certain drugs through CYP2C19 is compromised by a genetic mutation in one or both copies of the CYP2C19 gene that renders the enzyme nonfunctional or less functional. Azeloprazole was designed to avoid CYP2C19 metabolism entirely, thereby avoiding pharmacogenomic issues with poor CYP2C19 metabolizers.[2]
Azeloprazole was designed by the Japanese pharmaceutical companyEisai Co Ltd.[5]
In the United States, proton pump inhibitors are found bothover the counter and byprescription.[6] However, azeloprazole is notFDA approved in the United States.[7]
Azeloprazole completed phase IIclinical trials forerosive esophagitis in Japan in 2017, and phase II clinical trials for GERD in the United States in 2016.[5]
