Volume V of the series Biotechnology: Pharmaceutical Aspects pp 1313-1321

Case Study: Omeprazole (Prilosec®)

  • Jeffrey N. HemenwayAffiliated withBristol-Myers Squibb

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Omeprazole, currently marketed as Prilosec and generic omeprazole, has been shown to reduce gastric acid secretion in animals and man. It reduces the secretion of acid by inhibiting the proton pump of the parietal cell (Fellenius et al., 1981). Omeprazole was not designed as a prodrug. It was first synthesized by Junggren et al. (1981) along with 29 other derivatives of substituted 2-(2-benzimidazolyl)-pyridines and was found to have more potent gastric acid secretion inhibitory effects in dogs than did previously tested structurally related compounds. However, omeprazole was later found not to be the active inhibitor of the proton pump per se. Instead, it acts as a prodrug and is converted to the active inhibitor in the acidic compartments of the parietal cell, near the enzymes it inhibits (Lindberg et al., 1986).