The prevalence of acid-related diseases such as gastroesophageal reflux disease (GERD) and peptic ulcer has increased significantly over the years and the incidence continues to rise. Although the etiology of these diseases remains unclear, acid suppression or antisecretory therapy has emerged as the treatment of choice for both. Of the two main classes of antisecretory agents (histamine H-2 receptor antagonists and proton pump inhibitors [PPIs]), PPIs, which block H+/K+-ATPase in gastric parietal cells, exhibit more potent and longer lasting inhibition of gastric acid secretion and have become the preferred treatment option. Revaprazan hydrochloride (YH-1885) is a novel, reversible PPI with potent, long-lasting acid-suppressive effects and improved safety and pharmacokinetic profiles as compared to irreversible PPIs such as omeprazole. Revaprazan was chosen for further development as an antisecretory agent and was shown to be safe, effective and well tolerated in healthy subjects, where it significantly inhibited gastric acid secretion. Revaprazan is currently undergoing phase III development as a treatment for peptic ulcer.