-
Expert Opinion on Pharmacotherapy Oct 2009Proton pump inhibitors (PPIs) have been used for more than two decades to control symptoms of gastroesophageal illnesses. Studies have shown that most PPIs do not... (Review)
Review
BACKGROUND
Proton pump inhibitors (PPIs) have been used for more than two decades to control symptoms of gastroesophageal illnesses. Studies have shown that most PPIs do not provide 24-h symptom control, and that can be the reason for treatment failure. Recently, dexlansoprazole dual delayed release (DDR) (Takeda Pharmaceuticals North America, Inc., USA) under the trade name of Kapidex (Takeda Pharmaceutical Company Limited, Japan) came onto the market to provide longer duration of action and more effective acid suppression.
OBJECTIVE
The purpose of this paper is to discuss the pharmacology of dexlansoprazole DDR and to provide a concise review of all available studies showing its efficacy. The combination of the slower metabolism of the R-enantiomer and novel dual release pharmacokinetics is impressive.
METHODS
This manuscript is based on a review of all currently available medical literature on dexlansoprazole DDR.
CONCLUSION
Dexlansoprazole DDR has the potential to outperform traditional PPIs based on the metabolism and novel pharmacokinetics. It is currently FDA approved for the treatment of erosive esophagitis (acute, maintenance) and symptomatic gastroesophageal reflux disease.
Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Acute Disease; Anti-Ulcer Agents; Delayed-Action Preparations; Dexlansoprazole; Esophagitis, Peptic; Gastroesophageal Reflux; Humans; Lansoprazole; Proton Pump Inhibitors; Treatment Outcome
PubMed: 19708852
DOI: 10.1517/14656560903198978 -
The Medical Letter on Drugs and... May 2022
Topics: Dexlansoprazole; Esomeprazole; Gastroesophageal Reflux; Humans; Proton Pump Inhibitors
PubMed: 35536912
DOI: No ID Found -
Przeglad Gastroenterologiczny 2015Dexlansoprazole modified release (MR) is an R-enantiomer of lansoprazole and a new-generation proton pump inhibitor exhibiting high efficacy in the treatment of symptoms... (Review)
Review
Dexlansoprazole modified release (MR) is an R-enantiomer of lansoprazole and a new-generation proton pump inhibitor exhibiting high efficacy in the treatment of symptoms and lesions associated with erosive oesophagitis caused by gastroesophageal reflux disease (GERD). The dual release of the active ingredient - in the duodenum and the small intestine - makes it possible to achieve two peak concentrations at various times, within two and five hours of administration. Dexlansoprazole MR ensures the longest maintenance of drug concentration in the plasma of all known proton pump inhibitors, and the longest proton pump inhibitory effect. The basic indications for the drug include all forms of gastroesophageal reflux disease, especially with night-time heartburn and sleep disorders resulting from GERD. Dexlansoprazole can be taken regardless of meal times. It has a good safety profile and carries a low risk of adverse interactions with other drugs.
PubMed: 26759624
DOI: 10.5114/pg.2015.56109 -
Therapeutic Advances in Gastroenterology Feb 2017Dexlansoprazole modified-release (MR) is the R-enantiomer of lansoprazole and is currently the only proton-pump inhibitor (PPI) with a novel dual delayed release (DDR)... (Review)
Review
Dexlansoprazole modified-release (MR) is the R-enantiomer of lansoprazole and is currently the only proton-pump inhibitor (PPI) with a novel dual delayed release (DDR) formulation. Overall, dexlansoprazole MR demonstrates a similar safety and side-effect profile as lansoprazole. Dexlansoprazole MR has been shown to be highly efficacious in healing erosive esophagitis, maintaining healed esophageal mucosa in patients with erosive esophagitis and controlling symptoms of patients with nonerosive reflux disease (NERD). Recent studies have also demonstrated that dexlansoprazole MR is highly effective in improving nocturnal heartburn, gastroesophageal reflux disease (GERD) related sleep disturbances and bothersome regurgitation. Dexlansoprazole MR is well tolerated and can be taken without regard to food.
PubMed: 28203282
DOI: 10.1177/1756283X16681701 -
The Annals of Pharmacotherapy May 2010To describe the pharmacology, pharmacokinetics, and efficacy of dexlansoprazole in the treatment of heartburn associated with nonerosive gastroesophageal reflux disease... (Review)
Review
OBJECTIVE
To describe the pharmacology, pharmacokinetics, and efficacy of dexlansoprazole in the treatment of heartburn associated with nonerosive gastroesophageal reflux disease (GERD) and healing and maintenance of healing of all grades of erosive esophagitis (EE).
DATA SOURCES
Literature searches were conducted using MEDLINE Ovid (1950-December 2009, week 4) and EMBASE (1980-2009, week 53) using the term dexlansoprazole. References from articles obtained from the search were evaluated for other relevant citations.
STUDY SELECTION AND DATA EXTRACTION
All articles published in English evaluating the pharmacology, pharmacokinetics, efficacy, and adverse effect profile of dexlansoprazole were selected for inclusion.
DATA SYNTHESIS
Dexlansoprazole is the newest addition to the proton pump inhibitor (PPI) class and is approved for the treatment of heartburn associated with nonerosive GERD, healing of all grades of EE, as well as maintenance of healing of EE. Dexlansoprazole has a unique dual delayed-release formulation, which releases drug at 2 points in time; the first peak occurs 1-2 hours after administration and the second occurs within 4-5 hours after administration. In Phase 3 trials conducted in adults, researchers found that dexlansoprazole increases rates of healing of EE, as well as the maintenance of healing, compared to lansoprazole. Relief of heartburn symptoms was comparable among the dexlansoprazole and lansoprazole treatment groups. Common adverse effects of dexlansoprazole are similar to those of the other PPIs, including diarrhea, abdominal pain, nausea, upper respiratory infection, vomiting, and flatulence.
CONCLUSIONS
Dexlansoprazole provides another treatment option for the management of EE and symptoms of heartburn. Considering that the cost of dexlansoprazole is not favorable, further studies evaluating potential advantages over other agents are necessary to define the role of dexlansoprazole in the treatment of these conditions.
Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Dexlansoprazole; Drug Interactions; Esophagitis; Gastroesophageal Reflux; Humans; Lansoprazole; Proton Pump Inhibitors; Treatment Outcome
PubMed: 20371754
DOI: 10.1345/aph.1M685 -
Journal of Pharmaceutical Sciences Nov 2019Proton pump inhibitors (PPIs) are widely used for treating acid-related disorders. For an "ideal PPI," achieving maximal absorption and sustaining pharmacodynamic... (Review)
Review
Proton pump inhibitors (PPIs) are widely used for treating acid-related disorders. For an "ideal PPI," achieving maximal absorption and sustaining pharmacodynamic effects through the 24-h dosing cycle are critical features. Dexlansoprazole offers a relevant case study on how an improved PPI was developed capitalizing on the rational optimization of a precursor molecule-in this case, using lansoprazole as a starting point, leveraging its chemical properties on pharmacokinetics, and exploring optimized formulations. Dexlansoprazole is the R(+)-enantiomer of lansoprazole and shows stereoselective differences in absorption and metabolism compared with the racemic mixture of lansoprazole. The formulation was further refined to use pulsate-type granules with enteric coating to withstand acidic gastric conditions, while allowing prolonged absorption in the proximal and distal small intestine. As a result, the dual delayed-release formulation of dexlansoprazole has a plasma concentration-time profile characterized by 2 distinct peaks, leading to an extended duration of therapeutic plasma drug concentrations compared with the conventional delayed-release lansoprazole formulation. The dual delayed-release formulation maintains plasma drug concentrations longer than the lansoprazole delayed-release formulation at all doses.
Topics: Capsules; Chemistry, Pharmaceutical; Delayed-Action Preparations; Dexlansoprazole; Humans; Intestine, Small; Lansoprazole; Proton Pump Inhibitors
PubMed: 31386865
DOI: 10.1016/j.xphs.2019.07.023 -
Clinical Therapeutics Aug 2010Dexlansoprazole, the dextrorotatory enantiomer of lansoprazole, is a proton pump inhibitor (PPI) formulated to have dual delayed-release properties. It is indicated for... (Review)
Review
BACKGROUND
Dexlansoprazole, the dextrorotatory enantiomer of lansoprazole, is a proton pump inhibitor (PPI) formulated to have dual delayed-release properties. It is indicated for healing all grades of esophagitis, maintaining the healing of erosive esophagitis (EE), and treating heartburn associated with nonerosive gastroesophageal reflux disease.
OBJECTIVE
This article reviews the pharmacology, pharmacokinetics, and pharmacodynamics of dexlansoprazole, as well as its clinical efficacy and tolerability.
METHODS
MEDLINE (1966-April 2010) and International Pharmaceutical Abstracts (1970-April 2010) were searched for original research and review articles published in English using the terms dexlansoprazole and TAK-390MR. The reference lists of identified articles were reviewed for additional pertinent publications. Abstracts from 2007-2009 American College of Gastroenterology and Digestive Disease Week meetings were searched using the same terms.
RESULTS
By irreversibly binding to H(+)K(+)-ATPase, dexlansoprazole inhibits acid production by the parietal cell. Its dual delayed-release formulation provides 2 distinct releases of medication, prolonging the mean residence time compared with lansoprazole (5.56-6.43 vs 2.83-3.23 hours, respectively). In 2 identical Phase III trials of the healing of EE, there were no significant differences in rates of complete healing after 8 weeks between dexlansoprazole 60 and 90 mg once daily and lansoprazole 30 mg once daily. In 2 studies of the maintenance of healing of EE, rates of healing at 6 months were significantly higher with dexlansoprazole 30, 60, and 90 mg once daily compared with placebo (P < 0.001). Patients with nonerosive reflux disease who received dexlansoprazole 30 or 60 mg once daily had significantly more 24-hour heartburn-free days compared with those who received placebo (P < 0.001). Dexlansoprazole was well tolerated compared with placebo or lansoprazole in all studies.
CONCLUSIONS
In the studies reviewed, dexlansoprazole was well tolerated and effective in the healing and maintenance of EE, and in the treatment of nonerosive reflux disease. However, most of the available evidence involved comparisons with placebo, making it difficult to draw meaningful conclusions about the place of dexlansoprazole among PPIs. More head-to-head comparative trials with other PPIs are needed to determine whether the unique formulation of dexlansoprazole translates into a clinically meaningful improvement in outcomes.
Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Animals; Delayed-Action Preparations; Dexlansoprazole; Esophagitis; Gastroesophageal Reflux; Heartburn; Humans; Lansoprazole; Proton Pump Inhibitors; Treatment Outcome
PubMed: 20974316
DOI: 10.1016/j.clinthera.2010.08.008 -
Annals of Medicine Aug 2011Dexlansoprazole MR is the R-enantiomer of lansoprazole that is delivered by a novel system, the dual delayed release formulation. The drug has been shown to be... (Comparative Study)
Comparative Study Review
Dexlansoprazole MR is the R-enantiomer of lansoprazole that is delivered by a novel system, the dual delayed release formulation. The drug has been shown to be efficacious in healing erosive esophagitis as compared with lansoprazole. When compared to placebo, dexlansoprazole provided significantly higher maintenance rates for healed esophageal mucosa in patients with erosive esophagitis and symptom control in patients with non-erosive reflux disease. Dexlansoprazole could be taken without regard to food. Overall, dexlansoprazole is well tolerated and has a comparable side-effect profile to lansoprazole.
Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Delayed-Action Preparations; Dexlansoprazole; Esophagitis; Gastroesophageal Reflux; Humans; Lansoprazole; Mucous Membrane; Proton Pump Inhibitors; Stereoisomerism
PubMed: 21366513
DOI: 10.3109/07853890.2011.554429 -
Expert Review of Gastroenterology &... Aug 2011Dexlansoprazole modified release (MR; Dexilant™), the R-enantiomer of lansoprazole, was approved in the USA in 2009 for the management of erosive esophagitis and... (Review)
Review
Dexlansoprazole modified release (MR; Dexilant™), the R-enantiomer of lansoprazole, was approved in the USA in 2009 for the management of erosive esophagitis and nonerosive reflux disease. Dexlansoprazole MR 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. This added convenience, along with excellent healing of esophagitis and symptom relief, substantiate its use in patients with gastroesophageal reflux disease requiring PPI treatment.
Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Anti-Ulcer Agents; Delayed-Action Preparations; Dexlansoprazole; Esophagitis; Gastroesophageal Reflux; Humans; Lansoprazole; Treatment Outcome; United States
PubMed: 21780890
DOI: 10.1586/egh.11.37