Dexlansoprazole MR (modified-release) has a dual delayed release formulation, which was designed to prolong the plasma concentration time profile to improve symptoms control and oesophageal mucosal healing, using a once-daily dose.
Gastroesophageal reflux disease (GORD) is a common condition with a prevalence of 10%-20% in the Western world. The range of GORD prevalence estimate is 18%-27% in North America and 8%-25% in Europe. Several studies have demonstrated that patients with GORD have reduced health-related quality of life and work productivity. It is the most common outpatient gastroenterology diagnosis in the US with a concomitant significant economic burden.
There are three GORD phenotypes, where the most prevalent is nonerosive reflux disease (60%-70%), followed by erosive oesophagitis (30%) and Barrett’s oesophagus (6%-12%).
Dexlansoprazole MR, the R-enantiomer of lansoprazole, has a unique dual delayed-release delivery system that was designed to address unmet needs that may accompany the use of single-release proton pump inhibitors (PPIs), specifically, their short plasma half-life and requirement for meal-associated dosing. The delivery technology of dexlansoprazole MR is designed to release the drug in two separate pH-dependent phases, the first in the proximal duodenum and the second in the more distal small intestine. This extends plasma concentration and pharmacodynamic effects of dexlansoprazole MR beyond those of single-release PPIs and allows for dosing at any time of the day without regard to meals.
Dexlansoprazole MR’s unique formulation and pharmacokinetic profile may result in improved clinical efficacy in patients with gastro-oesophageal reflux disease (GORD). Dexlansoprazole has certain pharmacological features that can markedly improve compliance and adherence.
Presently, dexlansoprazole MR is indicated for the healing of erosive oesophagitis (60mg qd) for up to eight weeks, maintenance of erosive oesophagitis healing (30mg qd) for up to six months and relief of symptoms of NERD patients (30mg qd) for up to four weeks. However, dexlansoprazole MR has also been shown to be beneficial in patients with nocturnal GORD-related symptoms, sleep disturbances due to GORD, acid regurgitation, eradication of H. pylori and heartburn relief in obese patients.
The drug is well tolerated with a safety profile that at least is like that of lansoprazole. In addition, some studies have suggested less drug interactions when compared with other PPIs.
Dexlansoprazole’s convenience, along with excellent healing of oesophagitis and symptom relief, substantiate its use in patients with gastroesophageal reflux disease requiring PPI treatment.
Brian W Behm & David A Peura. Dexlansoprazole MR for the management of gastroesophageal reflux disease. Expert Review of Gastroenterology & Hepatology 2011:5:4, 439-445,DOI: 10.1586/egh.11.37.
Fass R, Frazier R. The role of dexlansoprazole modified-release in the management of gastroesophageal reflux disease. Therap Adv Gastroenterol. 2017;10:243-251. doi: 10.1177/1756283X16681701. Epub 2017 Jan 5. PMID: 28203282; PMCID: PMC5298478.