Esomeprazole magnesium (formerly known as perprazole), the (S)-enantiomer of the marketed proton pump inhibitor omeprazole (Losec), has been developed by AstraZeneca as an improved second-generation successor to Losec with several advantages over the first-generation compound. Omeprazole has one significant known drawback: polymorphic metabolism. Approximately 3% of all Caucasian patients and some 15-20% of Oriental patients metabolize omeprazole more slowly than the general population. In slow metabolizers, plasma concentrations of the drug are higher than the average. Since the inhibition of gastric acid secretion is correlated to the plasma concentration AUC, these slow metabolizers experience a more pronounced effect from the drug. As such, the search was initiated for an improved version of omeprazole with less interindividual variation and that would produce higher plasma levels. The result of this search was the discovery of esomeprazole, which proved throughout an extensive clinical testing program to possess unique pharmacokinetic properties of esomeprazole that contribute to rapid symptom resolution and high and predictable healing rates. AstraZeneca recently filed for marketing approval of esomeprazole sodium (Nexium) in the U.S. and Europe. The drug is targeted for the treatment of GERD, including reflux esophagitis, and for the healing and prevention of relapse of Helicobacter pylori-associated duodenal ulcers.
*Each month this section highlights a different
drug molecule or molecules. Selection is based on the following
criteria:
the originality of the chemical structure
the singularity of the mechanism of action
the drug's progression through the R&D pipeline
its use in a new indication or where current therapies
are inexistent or have proved unsatisfactory.
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