In vitro activity: Dexlansoprazole, constitutes>80% of circulating drug after oral administration of lansoprazole, provides lower clearance and 5-fold greater systemic exposure than the S-enantiomer following oral administration of lansoprazole. Dexlansoprazole MR is a modified release formulation of dexlansoprazole, which employs a novel Dual Delayed Release (DDR) technology that delivers the drug in two discrete phases of release, thereby inhibiting newly activated proton pumps that turn over following initial PPI inactivation of H+,K+-ATPase. Dexlansoprazole MR maintains plasma drug concentrations above the threshold level longer than lansoprazole at all doses, resulting in an optimized drug exposure-intragastric pH relationship. Dexlansoprazole selectively suppresses gastric acid secretion by direct inhibition of the H+K+-ATPase proton pump in the gastric parietal cell, inhibition of this cell membrane enzyme ultimately blocks the final step in acid production.

Aliment Pharmacol Ther. 2009 May 1;29(9):928-37; Clin Ther. 2010 Aug;32(9):1578-96.