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Dexlansoprazole

Dexlansoprazole is a proton pump inhibitor (PPI) medication that reduces gastric acid production by specifically inhibiting the (H⁺,K⁺)-ATPase enzyme system, known as the proton pump, located in the parietal cells of the stomach lining.^[1] It is the R-enantiomer of lansoprazole and is primarily indicated for the treatment of gastroesophageal reflux disease (GERD), including healing all grades of erosive esophagitis (EE) for up to 8 weeks, maintaining healing of EE and relieving heartburn for up to 6 months, and managing heartburn associated with symptomatic non-erosive GERD for 4 weeks.^[1] Marketed under the brand name Dexilant by Takeda Pharmaceuticals U.S.A., Inc., with generic versions approved by the FDA in November 2025, it features a dual delayed-release formulation in capsule form (available in 30 mg and 60 mg strengths), allowing for once-daily administration without regard to meals.^[1]^[2]^[3] The U.S. Food and Drug Administration (FDA) initially approved dexlansoprazole on January 30, 2009, originally under the name Kapidex, which was renamed Dexilant in 2010 to avoid confusion with other medications.^[3] Dexlansoprazole's modified-release technology enables a bimodal release of the drug—one portion in the stomach and another in the intestine—providing prolonged acid suppression over 24 hours, which is particularly beneficial for patients with nighttime symptoms or irregular meal times.^[1] Clinically, it has demonstrated high efficacy in healing EE (with healing rates of approximately 87-92% at 60 mg daily) and maintaining remission, comparable to or exceeding other PPIs like omeprazole and lansoprazole in head-to-head studies.^[4] For maintenance therapy, a 30 mg daily dose is typically recommended, while 60 mg is used for initial healing of EE; dosage adjustments are advised for patients with moderate hepatic impairment, limiting the maximum to 30 mg daily.^[1] In 2016, the FDA expanded approval to include adolescents aged 12-17 years for similar GERD-related indications, and an orally disintegrating tablet (SoluTab) formulation was also approved that year, though it was later discontinued.^[5] As part of the PPI class, dexlansoprazole shares common precautions, including risks of long-term use such as hypomagnesemia, Clostridium difficile-associated diarrhea, and potential interference with vitamin B12 or calcium absorption, necessitating monitoring in extended therapy.^[1] Its pharmacokinetic profile shows rapid absorption (peak plasma levels within 1-2 hours for the first release and 4-5 hours for the second), with metabolism primarily via CYP2C19 and CYP3A4 enzymes, leading to variability in poor CYP2C19 metabolizers who may experience higher exposure.^[1] Overall, dexlansoprazole represents an advancement in PPI therapy due to its flexible dosing and consistent acid control, making it a preferred option for patients requiring reliable symptom relief in GERD management.^[4]

Uses and administration

Indications

Dexlansoprazole is indicated for the healing of all grades of erosive esophagitis (EE) in patients aged 12 years and older, typically confirmed by endoscopy showing mucosal breaks in the esophagus.^[1] It is also approved for the maintenance of healed EE to prevent relapse and for the relief of associated heartburn symptoms over extended periods.^[1] Additionally, dexlansoprazole treats heartburn and other symptoms of symptomatic non-erosive gastroesophageal reflux disease (GERD), where no visible esophageal damage is present but patients experience frequent reflux-related discomfort.^[6] Clinical trials have demonstrated high efficacy in these indications, with pivotal studies showing cumulative healing rates exceeding 90% for EE after 8 weeks of therapy at 60 mg daily, comparable to or superior to lansoprazole in achieving mucosal healing and symptom resolution.^[4] For instance, in comparative trials, dexlansoprazole provided significantly greater relief of GERD symptoms, including heartburn frequency and severity, than lansoprazole, supporting its role in patients requiring robust acid suppression for symptom control.^[7] These outcomes stem from its proton pump inhibition, which reduces gastric acid production to promote esophageal healing and alleviate reflux symptoms.^[8] Patient selection for dexlansoprazole emphasizes individuals with frequent GERD symptoms, such as heartburn occurring at least twice weekly for several months, alongside endoscopic evidence of EE for healing indications or absence thereof for non-erosive GERD.^[9] Therapy duration is guided by initial response and risk of relapse, generally spanning 4 to 8 weeks for acute EE healing and longer-term maintenance in those with recurrent symptoms or high-risk features like severe baseline esophagitis.^[10] Off-label uses include incorporation into triple therapy regimens for Helicobacter pylori eradication, where studies report eradication rates of around 90-94% when combined with antibiotics, and management of Zollinger-Ellison syndrome for hypersecretory acid conditions, leveraging its prolonged acid suppression.^[11]^[12]

Dosage and administration

Dexlansoprazole is available in delayed-release capsule formulations containing 30 mg or 60 mg of the active ingredient.^[1] For the healing of erosive esophagitis (EE), the recommended dosage is 60 mg once daily for up to 8 weeks.^[1] Maintenance of healed EE and relief of associated heartburn requires 30 mg once daily, typically for up to 6 months in adults or 16 weeks in adolescents aged 12-17 years.^[1] For the treatment of heartburn associated with symptomatic non-erosive gastroesophageal reflux disease (GERD), the standard dose is 30 mg once daily for 4 weeks.^[1] These regimens are tailored to the specific indication, with dosing for EE generally higher and longer than for non-erosive GERD.^[1] The medication can be taken without regard to meals, owing to its dual delayed-release technology that maintains bioavailability regardless of food intake.^[1] Capsules should be swallowed whole and not chewed or crushed to preserve the delayed-release mechanism.^[1] For patients unable to swallow capsules, the contents may be emptied onto a spoonful of applesauce and swallowed immediately without chewing, or mixed with water for administration via oral syringe or nasogastric tube (≥16 French).^[1]^[13] In patients with moderate hepatic impairment (Child-Pugh Class B), the dosage should be reduced to 30 mg once daily for EE healing, up to 8 weeks; it is not recommended for severe hepatic impairment (Child-Pugh Class C).^[1] No dosage adjustments are necessary for renal impairment, elderly patients, or those with mild hepatic impairment.^[1] Discontinuation does not typically require tapering, though abrupt cessation may lead to symptom rebound in some cases.^[1] For long-term use, periodic assessment of symptoms is advised, along with endoscopy as needed to evaluate healing and rule out complications such as malignancy.^[9] Regular monitoring of clinical response and potential adverse effects through physician visits is recommended to ensure ongoing efficacy and safety.^[9]

Safety profile

Adverse effects

Dexlansoprazole, like other proton pump inhibitors (PPIs), is generally well-tolerated in short-term use, with most adverse effects being mild and transient. In controlled clinical trials involving adults, the most common adverse reactions occurring at a frequency of ≥2% and greater than placebo included diarrhea (4.8%), abdominal pain (4.0%), nausea (2.9%), upper respiratory tract infection (1.9%), vomiting (1.6%), and flatulence (1.6%).^[14] Headache has also been reported as a common side effect in various trials, with incidences ranging from 3% to 8% depending on the study population and duration. In pediatric patients aged 12-17 years, adverse reactions occurring at ≥5% included headache, abdominal pain, diarrhea, nasopharyngitis, and oropharyngeal pain.^[14] Serious adverse effects are rare but can occur, particularly with prolonged use. These include Clostridium difficile-associated diarrhea, which is linked to PPI-induced gastric acid suppression that may promote bacterial overgrowth.^[14] Acute interstitial nephritis has been observed as a class effect of PPIs.^[14] Other rare post-marketing reports encompass hypomagnesemia, which can occur after at least 3 months of therapy and is especially common after one year of use, bone fractures, and severe allergic reactions such as anaphylaxis.^[14]^[16] Long-term use of dexlansoprazole and other PPIs has been associated with several risks identified through post-marketing surveillance and cohort studies. Hypomagnesemia may be exacerbated by concurrent use of diuretics or other medications affecting electrolyte balance.^[16] Meta-analyses indicate a modest increase in bone fracture risk (approximately 20-30% relative risk elevation for hip, spine, and any-site fractures) with prolonged, high-dose therapy.^[17] Vitamin B12 deficiency can occur with use exceeding three years due to reduced gastric acid-mediated absorption.^[14] Additionally, there is an elevated risk of pneumonia, with meta-analyses reporting a 27-39% increase in short-term use, potentially related to altered gastric pH favoring pathogen survival.^[18] Discontinuation rates due to adverse effects are low, approximately 2-3% in clinical trials, with diarrhea being the most frequent cause at 0.7%.^[14] The FDA has issued class-wide warnings on these PPI risks since 2010, emphasizing monitoring for long-term users.^[19]

Contraindications and precautions

Dexlansoprazole is contraindicated in patients with known hypersensitivity to the drug, its components, lansoprazole, or other proton pump inhibitors (PPIs), as severe reactions such as anaphylaxis and acute interstitial nephritis have been reported.^[14]^[20] It is also contraindicated for concomitant use with rilpivirine-containing products, which may result in reduced rilpivirine absorption and loss of virologic response in HIV treatment.^[14]^[21] Precautions are advised in patients with severe hepatic impairment (Child-Pugh class C), where use is not recommended due to increased drug exposure and potential toxicity.^[14]^[22] Long-term use (over 1 year), particularly at high doses, may increase the risk of osteoporosis-related fractures of the hip, wrist, or spine; patients at risk for osteoporosis-related fractures should be managed according to established treatment guidelines, including use of the lowest dose and shortest duration of therapy appropriate to the condition being treated.^[14]^[20] In elderly patients, prolonged therapy warrants caution due to heightened risk of hypomagnesemia, which can lead to falls and other complications.^[14]^[21] In special populations, dexlansoprazole should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus, as there are no adequate human studies but animal reproduction studies have shown mixed results, with no adverse fetal effects observed in rabbits at exposures up to 9 times the maximum recommended human dose (MRHD), but potential risks to fetal bone growth based on rat studies with related PPIs.^[14]^[23] Caution is advised in breastfeeding women, as the drug is present in rat milk and limited human data exist, though related lansoprazole has been used safely in nursing infants.^[14]^[24] It is not approved for pediatric use in patients under 12 years of age, with safety and efficacy not established in this group.^[14]^[5] Monitoring recommendations include periodic assessment of serum magnesium levels in patients on long-term therapy, especially those receiving concomitant digoxin or diuretics, with discontinuation considered if hypomagnesemia persists despite supplementation.^[14]^[20] Patients should be observed for signs of cutaneous or systemic lupus erythematosus, a rare class effect of PPIs, and the drug discontinued if symptoms such as joint pain or rash occur.^[20]^[21]

Drug interactions

Dexlansoprazole, as a proton pump inhibitor (PPI), undergoes hepatic metabolism primarily via the CYP2C19 enzyme, which influences certain pharmacokinetic interactions, though it exhibits minimal inhibitory effects on this pathway compared to other PPIs.^[14] Concomitant use with warfarin may prolong prothrombin time and increase international normalized ratio (INR), necessitating monitoring of INR and potential dose adjustments to prevent bleeding risks.^[14] Similarly, elevated serum levels of methotrexate have been observed with PPI coadministration, particularly at high doses; temporary discontinuation of dexlansoprazole should be considered during high-dose methotrexate therapy, with monitoring of methotrexate concentrations.^[14] Dexlansoprazole does not significantly alter the pharmacokinetics of diazepam or phenytoin, as demonstrated in clinical studies.^[25] Dexlansoprazole can reduce the absorption of drugs dependent on gastric acidity, such as ketoconazole, itraconazole, and erlotinib, by elevating intragastric pH; caution is advised, and administration of these agents should be separated from dexlansoprazole dosing, ideally by at least 2 hours, to optimize absorption.^[14] Potential increased exposure to digoxin and tacrolimus has been noted, requiring monitoring of serum levels and dose titration as needed, especially in transplant patients.^[14] Pharmacodynamic interactions include an heightened risk of hypomagnesemia with prolonged PPI use, which may be exacerbated by concomitant diuretics or drugs like digoxin that also affect magnesium balance; periodic monitoring of serum magnesium is recommended in such cases.^[14] Regarding clopidogrel, while PPIs as a class carry warnings for potentially diminishing antiplatelet effects via CYP2C19 inhibition, specific studies with dexlansoprazole show no clinically significant impact on clopidogrel's active metabolite exposure or platelet inhibition.^[26] Food does not significantly affect dexlansoprazole's bioavailability due to its dual delayed-release formulation, allowing administration with or without meals; however, for patients unable to swallow capsules, the contents may be sprinkled on one tablespoon of applesauce and swallowed immediately without chewing.^[14] Clinical management of these interactions involves therapeutic drug monitoring for narrow therapeutic index agents like warfarin, methotrexate, digoxin, and tacrolimus; dose spacing for pH-dependent drugs; and consideration of alternative acid-suppressive therapies if interactions cannot be mitigated.^[14] Contraindication exists with rilpivirine-containing antiretrovirals due to decreased rilpivirine exposure.^[14]

Pharmacology

Mechanism of action

Dexlansoprazole is a proton pump inhibitor (PPI) that suppresses gastric acid secretion by irreversibly inhibiting the H⁺/K⁺-ATPase enzyme, also known as the proton pump, located on the secretory surface of gastric parietal cells.^[27] This enzyme is responsible for the final step in acid production, where it exchanges hydrogen ions (H⁺) from the parietal cell cytoplasm for potassium ions (K⁺) in the gastric lumen, facilitating hydrochloric acid secretion. By specifically targeting this proton pump, dexlansoprazole prevents H⁺ secretion into the stomach, thereby reducing overall gastric acidity.^[28] As the R-enantiomer of lansoprazole, dexlansoprazole exhibits enhanced efficacy in acid inhibition compared to the racemic lansoprazole mixture, providing more prolonged suppression of gastric acid production.^[4] Upon reaching the acidic environment of the parietal cell canaliculi, dexlansoprazole is protonated and converted to its active sulfenamide form, which then forms a covalent disulfide bond with the sulfhydryl (SH) groups of specific cysteine residues on the H⁺/K⁺-ATPase enzyme, such as Cys813.^[4] This irreversible binding inactivates the proton pump until new enzymes are synthesized by the parietal cells, ensuring sustained inhibition.^[29] The drug's dual delayed-release formulation further supports its mechanism by delivering two distinct absorption peaks: approximately 25% of the dose releases in the proximal duodenum at pH 5.5 (1–2 hours post-dose) and 75% in the distal small intestine at pH 6.75 (4–5 hours post-dose).^[8] This pharmacokinetic profile results in extended plasma concentrations, enabling acid suppression for over 24 hours with reduced inter- and intra-subject variability compared to conventional PPIs, while maintaining similar intrinsic potency.^[28]

Pharmacokinetics

Dexlansoprazole is absorbed following oral administration of its dual delayed-release capsules, resulting in a characteristic bimodal plasma concentration profile with peaks at approximately 1 to 2 hours and 4 to 5 hours post-dose. The maximum plasma concentration (C_max) and area under the curve (AUC) increase in a dose-proportional manner over the therapeutic range of 30 to 60 mg. The drug's absorption is not significantly affected by food or concomitant antacids, allowing for flexible dosing without regard to meals.^[1]^[30] The apparent volume of distribution at steady state is about 40 L. Dexlansoprazole is extensively bound to plasma proteins, with binding ranging from 96% to 99% across a concentration range of 0.01 to 20 mcg/mL.^[1] Metabolism of dexlansoprazole occurs primarily in the liver through cytochrome P450 enzymes, mainly CYP2C19 (via hydroxylation) and CYP3A4 (via oxidation to the sulfone metabolite), producing inactive metabolites such as 5-hydroxy dexlansoprazole and its glucuronide conjugate. Poor metabolizers of CYP2C19, defined by two loss-of-function alleles, exhibit substantially higher systemic exposure compared to extensive metabolizers, with AUC values up to 12-fold greater.^[1] Elimination of dexlansoprazole is rapid, with a terminal half-life of 1 to 2 hours in healthy subjects and patients with gastroesophageal reflux disease. Apparent oral clearance is approximately 11 to 12 L/h, and there is no accumulation upon once-daily dosing. The drug is excreted predominantly as metabolites, with about 51% of the administered radioactive dose recovered in urine and 48% in feces; no unchanged dexlansoprazole is detected in urine.^[1] Pharmacokinetic variability is largely influenced by genetic polymorphisms in CYP2C19, with poor metabolizers comprising 2% to 5% of the Caucasian population and showing markedly elevated exposure (up to 12-fold AUC increase), while intermediate metabolizers (heterozygous for loss-of-function alleles) experience about a 2-fold increase in AUC. Age-related changes are minimal, though elderly patients may have slightly higher AUC (about 35% increase) and prolonged half-life due to reduced hepatic function.^[1]^[31]

Chemical properties

Structure and identification

Dexlansoprazole is chemically known as (R)-2-[(3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl)methylsulfinyl]-1H-benzimidazole.^[32] Its IUPAC name is 2-[(R)-[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methylsulfinyl]-1H-benzimidazole.^[32] The molecular formula is C₁₆H₁₄F₃N₃O₂S, with a molecular weight of 369.4 g/mol.^[32] The molecule features a benzimidazole core linked via a sulfinyl group to a pyridine ring substituted with a methyl group at position 3 and a 2,2,2-trifluoroethoxy group at position 4.^[32] This sulfinyl linker, -S(O)-, connects the methyl group on the pyridine to the 2-position of the benzimidazole.^[32] For identification, dexlansoprazole has the CAS number 138530-94-6.^[32] Its SMILES notation is CC1=C(C=CN=C1CS@@C2=NC3=CC=CC=C3N2)OCC(F)(F)F, which serves as a reference for chemical databases.^[32] Dexlansoprazole is the enantiopure (R)-enantiomer derived from the racemic lansoprazole, with the chiral center at the sulfinyl sulfur atom exhibiting the R configuration.^[33] This stereochemistry contributes to enhanced therapeutic activity compared to the (S)-enantiomer.^[33]

Physical and chemical characteristics

Dexlansoprazole appears as a white to nearly white crystalline powder that melts with decomposition at approximately 140°C.^[23]^[34] The compound is practically insoluble in water, with solubility below 0.3 mg/mL, but it is freely soluble in organic solvents such as dimethylformamide, methanol, dichloromethane, ethanol, and ethyl acetate, as well as soluble in acetonitrile and slightly soluble in ether.^[35]^[23]^[8] Its pKa values are approximately 4.2 for the pyridine moiety and 9.0 for the benzimidazole group, influencing its ionization and absorption profile in the gastrointestinal tract.^[8] Dexlansoprazole exhibits stability when exposed to light and is more stable under neutral and alkaline conditions than in acidic environments, where it degrades more readily; this pH-dependent stability necessitates protection via enteric coatings in its formulations to prevent degradation in the stomach.^[23]^[34] The commercial formulation consists of dual delayed-release capsules containing two populations of enteric-coated pellets: an immediate-release layer that begins dissolution around pH 5.5 and an enteric-coated layer that activates at pH 6.8, enabling prolonged and pH-dependent drug release.^[36] Storage recommendations include maintaining dexlansoprazole at room temperature (15–30°C), protected from moisture and excessive heat to preserve its integrity.^[9]^[23]

Development and history

Research and development

Dexlansoprazole was developed by Takeda Pharmaceuticals in the early 2000s as the pure R-enantiomer of lansoprazole, selected for its greater potency and reduced metabolic variability compared to the racemic mixture, aiming to enhance pharmacokinetic consistency and acid suppression duration.^[37]^[38] This enantiomer-specific approach addressed limitations in lansoprazole's absorption and CYP2C19-dependent metabolism, which can lead to interpatient variability in efficacy.^[39]^[29] Preclinical studies in animal models, including beagle dogs, confirmed dexlansoprazole's stereoselective advantages, showing improved bioavailability and prolonged plasma exposure relative to lansoprazole after oral administration.^[40] These investigations demonstrated superior acid suppression duration, with dexlansoprazole maintaining intragastric pH >4 for longer periods in canine models compared to lansoprazole, supporting its potential for extended therapeutic effects.^[41]^[42] The pivotal phase III clinical trials, conducted from 2007 to 2008, evaluated dexlansoprazole's efficacy in adults with erosive esophagitis (EE) and symptomatic gastroesophageal reflux disease (GERD).^[43]^[44] In two identical 8-week healing trials involving over 4,000 patients, dexlansoprazole 60 mg and 90 mg doses achieved EE healing rates of 87-93%, establishing non-inferiority to lansoprazole 30 mg while providing superior 24-hour heartburn relief, particularly for nighttime symptoms.^[45]^[46] Maintenance trials further showed sustained healing over 6 months with reduced relapse rates compared to placebo.^[47] A major formulation innovation during development was the dual delayed-release technology, featuring two types of enteric-coated granules that release dexlansoprazole in sequential pulses approximately 1-2 and 4-5 hours post-dose, mimicking circadian acid secretion patterns and minimizing CYP2C19 polymorphism effects for more predictable intragastric pH control.^[48]^[37] From 2020 to 2025, research on the proton pump inhibitor (PPI) class, including dexlansoprazole, has emphasized long-term risks such as enteric infections, bone fractures, and nutrient malabsorption, prompting updated guidelines from organizations like the American College of Gastroenterology to prioritize short-term use and deprescribing where possible.^[49]^[7] No significant new indications beyond EE and GERD have emerged for dexlansoprazole, though following patent expiration in 2020 has driven multiple bioequivalence trials for generics, confirming comparable pharmacokinetics and acid suppression to the reference product.^[50]^[51] In November 2025, Alembic Pharmaceuticals received FDA approval for a generic version of dexlansoprazole delayed-release capsules.^[52]

Regulatory approvals and patents

Dexlansoprazole received approval from the U.S. Food and Drug Administration (FDA) on January 30, 2009, for the treatment of heartburn associated with symptomatic non-erosive gastroesophageal reflux disease (GERD) and for the healing and maintenance of erosive esophagitis (EE), initially marketed under the brand name Kapidex by Takeda Pharmaceuticals.^[53] The brand name was changed to Dexilant in March 2010 following reports of confusion with another medication.^[54] A supplemental approval in June 2011 expanded the indication for maintenance therapy of healed EE to include patients with all grades of EE.^[55] Internationally, dexlansoprazole gained approval in Canada in 2010 and Mexico in 2011, with national authorizations in several European Union member states beginning in 2013, including Sweden, Lithuania, Belgium, Germany, and Ireland; it became available in Poland in 2015.^[56] By 2015, the drug was approved and marketed in multiple countries outside the U.S., though it lacks centralized European Medicines Agency (EMA) authorization and is regulated nationally in the EU.^[4] The original U.S. composition-of-matter patent and related formulation patents provided exclusivity until early 2020, with pediatric exclusivity extending protection through 2022 in some cases.^[57] Following patent expiration, the FDA approved the first generic version in April 2017 (ANDA 202294 by Par Pharmaceutical), though market entry was delayed until January 2022 due to litigation; subsequent launches included versions by Endo International in June 2023.^[50]^[58] Post-approval, the FDA issued class-wide safety communications for proton pump inhibitors (PPIs), including dexlansoprazole, warning of possible increased risk of hip, wrist, and spine fractures with long-term or high-dose use in May 2010, low serum magnesium (hypomagnesemia) associated with prolonged therapy in March 2011, and Clostridium difficile-associated diarrhea in February 2012.^[19]^[16]^[59] These risks are reflected in product labeling, with a warning section for C. difficile but no black box warning specific to dexlansoprazole; the drug has not faced withdrawal or restrictions.^[60] As of 2025, ongoing FDA and expert reviews continue to evaluate long-term PPI safety, emphasizing benefits outweighing risks for appropriate indications while recommending periodic reassessment to minimize potential adverse effects like fractures and infections.^[61]^[62]

Society and culture

Brand names and availability

Dexlansoprazole is marketed under the primary brand name Dexilant in the United States, developed and originally distributed by Takeda Pharmaceuticals.^[63] Other brand formulations include the discontinued Kapidex and Dexilant SoluTab, the latter withdrawn from the market in 2018.^[9] ^[64] Internationally, it is available under names such as Lanfil DX and Lanzotyle DX in India, produced by manufacturers like Fourrts India Laboratories and others.^[65] Generic versions of dexlansoprazole are widely marketed without specific brand names in various countries.^[66] The original branded product is manufactured by Takeda Pharmaceuticals, while generic formulations are produced by companies including Viatris (formerly Mylan), TWi Pharmaceuticals, and Endo International following FDA approval of the first generic in 2017 and market entry starting in 2022, with additional launches in 2023.^[50] ^[67] ^[58] API suppliers for generics include Metrochem API Private Limited and Alembic Pharmaceuticals Limited, supporting production in regions like India and the US; as of November 2025, Alembic received USFDA approval for dexlansoprazole delayed-release capsules.^[66] ^[68] Dexlansoprazole is available exclusively by prescription in the United States, Europe, Asia, and most global markets as of 2025, with no over-the-counter formulations approved.^[69] It is widely accessible through pharmacies in these regions, often in delayed-release capsule form at 30 mg or 60 mg strengths.^[70] In the US, it is included in formularies such as Medicare Part D, facilitating coverage for eligible patients.^[71] In the United States, the average retail price for a 30-day supply of brand-name Dexilant (60 mg capsules) is approximately $290 as of 2025, while generic dexlansoprazole costs around $85 with discount programs or $50 or less through international pharmacies.^[71] Access may vary by insurance, but generics have improved affordability since their 2022 launch.^[72] Supply chain disruptions affected dexlansoprazole availability in 2020 due to COVID-19-related manufacturing issues, but no major shortages or recalls have been reported in the US or globally from 2021 to 2025, with minor resolved shortages noted in Canada in 2024.^[73]

Legal and economic aspects

Dexlansoprazole is classified as a non-controlled prescription medication in the United States, regulated under the Federal Food, Drug, and Cosmetic Act as a drug requiring a healthcare provider's authorization for dispensing. It is not listed among controlled substances by the Drug Enforcement Administration. In the European Union, dexlansoprazole holds similar prescription-only status, approved through mutual recognition procedures for treating gastroesophageal reflux disease and related conditions.^[27]^[74]^[56] Economically, dexlansoprazole generated peak annual U.S. sales of approximately $530 million for its branded formulation in 2015, reflecting strong market penetration among proton pump inhibitors prior to generic competition. Following the entry of generic versions—with first FDA approval in 2017, launches starting in 2022, and additional approvals through 2025—the branded market share declined sharply, with overall U.S. revenues estimated to have dropped to around $100 million annually by 2024 due to price erosion from generics. This generic influx has yielded significant cost savings for U.S. payers and patients, contributing to broader proton pump inhibitor class savings exceeding $127 billion in 2023 from high-volume generics, with dexlansoprazole-specific reductions estimated at $200 million yearly through lower acquisition costs.^[75]^[70]^[67]^[50]^[68]^[76] In healthcare policy, dexlansoprazole is not included on the World Health Organization's Model List of Essential Medicines, unlike foundational proton pump inhibitors such as omeprazole. However, it is recommended in the American College of Gastroenterology's 2022 clinical guideline for the diagnosis and management of gastroesophageal reflux disease, particularly for once-daily dosing without strict meal-timing requirements, as an option for symptom control and erosive esophagitis healing. The drug has been implicated in class-action litigation alongside other proton pump inhibitors over alleged kidney injury risks, with settlements totaling hundreds of millions from manufacturers like AstraZeneca ($425 million in 2023 for Nexium and Prilosec claims); Takeda, the developer of dexlansoprazole (branded as Dexilant), settled related claims in 2024.^[77]^[78]^[79] Societally, Takeda's manufacturing processes for dexlansoprazole align with the company's broader environmental commitments, including zero-waste-to-landfill goals at facilities like its Jaguariúna site in Brazil since 2020 and initiatives to reduce pharmaceutical waste through thermal recovery and green chemistry, though specific waste impacts from dexlansoprazole production remain minimal and unregulated beyond general pharmaceutical standards. No major controversies surround dexlansoprazole itself, but proton pump inhibitors as a class face public health scrutiny for overuse, prompting 2024 deprescribing campaigns such as the DepRescribing inapprOpriate Proton Pump InhibiTors (DROPIT) initiative and Veterans Affairs interventions that reduced unnecessary prescriptions by limiting refills and promoting evidence-based stewardship to mitigate risks like long-term adverse effects.^[80]^[81]^[82] Looking ahead, competition for dexlansoprazole is expected to remain driven by generics rather than biosimilars, given its status as a small-molecule drug ineligible for biologics pathways, potentially stabilizing prices further as additional generic manufacturers enter the market. Ongoing 2025 stewardship studies, including analyses of proton pump inhibitor utilization trends and deprescribing frameworks, emphasize reducing unnecessary long-term prescriptions to optimize costs and safety, with dexlansoprazole highlighted in reviews for periodic reassessment in gastroesophageal reflux disease management.^[83]^[84]^[85]

References

[1]
None
### Summary of Key Sections from DEXILANT FDA Label (https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022287s020lbl.pdf)
[2]
[PDF] 22287 dexlansoprazole clinpharm prea - FDA
Jun 13, 2016 · Dexilant (dexlansoprazole) delayed-release capsules were approved for adults in 2009, indicated for healing of all grades of erosive esophagitis ...Missing: manufacturer | Show results with:manufacturer
[3]
Dexlansoprazole – a new-generation proton pump inhibitor - PMC
Dec 16, 2015 · The basic indications for the drug include all forms of gastroesophageal reflux disease, especially with night-time heartburn and sleep ...
[4]
Takeda Announces FDA Approval of Dexilant (dexlansoprazole) for ...
Jul 11, 2016 · Dexilant has been approved in adult patients since 2009. Deerfield, Ill., July 11, 2016 – Takeda Pharmaceuticals U.S.A., Inc., ...
[5]
[PDF] DEXILANT (dexlansoprazole) label - accessdata.fda.gov
DEXILANT is indicated for the treatment of heartburn associated with symptomatic non-erosive gastroesophageal reflux disease (GERD) for four weeks. 2 DOSAGE AND ...
[6]
[PDF] DEXILANT (dexlansoprazole) Label - accessdata.fda.gov
DEXILANT capsules and DEXILANT SoluTab are indicated in adults for the treatment of heartburn associated with symptomatic non-erosive gastroesophageal reflux ...Missing: manufacturer | Show results with:manufacturer
[7]
Pharmacological and Safety Profile of Dexlansoprazole: A ... - NIH
Dexlansoprazole has been shown to be effective for healing of erosive esophagitis, and to improve subjective well-being by controlling 24-hour symptoms.
[8]
The Effect of Dexlansoprazole on Gastroesophageal Reflux Disease
Two studies showed that dexlansoprazole significantly decreased GERD symptoms compared to lansoprazole [33,38]. Peura et al. [33] found significant results, ...Missing: EXALOT | Show results with:EXALOT
[9]
Dexlansoprazole: Uses, Interactions, Mechanism of Action - DrugBank
Dexlansoprazole is a proton pump inhibitor used to treat erosive esophagitis, heartburn, and gastroesophageal reflux disease (GERD).
[10]
Dexlansoprazole (oral route) - Side effects & dosage - Mayo Clinic
Dexlansoprazole is used to treat certain conditions in which there is too much acid in the stomach. It is used to treat erosive esophagitis or heartburn.
[11]
Dual Delayed-Release Dexlansoprazole for Healing and ... - NIH
Nov 2, 2018 · Dexlansoprazole is approved for healing EE of all grades, maintenance of healed EE, relief of heartburn, and treatment of symptomatic non-erosive GERD in ...Missing: criteria | Show results with:criteria
[12]
Efficacy of dexlansoprazole-based triple therapy for Helicobacter ...
Sep 5, 2019 · This study suggests that dexlansoprazole-based triple therapy has an acceptable eradication rate for H. pylori infection.Missing: off- Zollinger- Ellison
[13]
Dexlansoprazole - an overview | ScienceDirect Topics
Dexlansoprazole is a proton pump inhibitor used to treat gastrointestinal ulcers, gastroesophageal reflux disease (GERD) symptoms, Helicobacter pylori ...<|separator|>
[14]
[PDF] This label may not be the latest approved by FDA. For current ...
Absorption. After oral administration of DEXILANT 30 or 60 mg to healthy subjects and symptomatic GERD patients, mean. Cmax and AUC values of dexlansoprazole ...
[15]
https://www.sciencedirect.com/topics/%5Bneuroscience
[16]
Dexlansoprazole - an overview | ScienceDirect Topics
There were 187 treatment-related adverse events in 69 subjects (35%), diarrhea (10%), headache (8%), and abdominal pain (6%) being the most common. Serum ...
[17]
Low magnesium levels can be associated with long-term use of PPIs
Mar 2, 2011 · Prescription proton pump inhibitor (PPI) drugs may cause low serum magnesium levels (hypomagnesemia) if taken for prolonged periods of time (in most cases, ...
[18]
Proton pump inhibitors and risk of fractures: a meta-analysis of ... - NIH
In this meta-analysis of observational studies, PPIs modestly increased the risk of hip, spine, and any-site fractures, whereas H2RAs were not associated with ...
[19]
Perils and pitfalls of long-term effects of proton pump inhibitors
The risk of pneumonia was increased 27-39% in short-term use of PPIs in three meta-analyses. C. difficile infections were also associated with the use of PPIs ( ...Missing: bone | Show results with:bone
[20]
Possible increased risk of fractures of the hip, wrist, and spine ... - FDA
May 25, 2010 · Following a thorough review of available safety data, FDA has concluded that fracture risk with short-term, low dose PPI use is unlikely.
[21]
Dexlansoprazole: Side Effects, Uses, Dosage, Interactions, Warnings
What Are Warnings and Precautions for Dexlansoprazole? Contraindications. Hypersensitivity reactions, including anaphylaxis and acute interstitial nephritis ...
[22]
Dexlansoprazole Monograph for Professionals - Drugs.com
Jun 10, 2025 · Cautions for Dexlansoprazole. Contraindications. Known hypersensitivity to dexlansoprazole or any ingredient in the formulation. Warnings/ ...
[23]
Dexilant, Kapidex (dexlansoprazole) dosing, indications ...
... Hepatic impairment. Milde (Child-Pugh A): Dose adjustment not necessary; Moderate (Child-Pugh B): Not to exceed 30 mg/day; Severe (Child-Pugh C): Not ...Missing: category | Show results with:category
[24]
Dexlansoprazole - Drugs and Lactation Database (LactMed®) - NCBI
May 15, 2022 · No information is available on the use of dexlansoprazole or lansoprazole during breastfeeding. However, lansoprazole has been used safely in newborn infants.Dexlansoprazole · Drug Levels And Effects · Substance Identification<|control11|><|separator|>
[25]
Drug interaction studies with dexlansoprazole modified ... - PubMed
Coadministration of dexlansoprazole MR with diazepam, phenytoin or theophylline did not affect the pharmacokinetics of these drugs.
[26]
DEXILANT (dexlansoprazole) Product Information Updated ...
Nov 17, 2011 · DEXILANT had no clinically important effect on exposure to the active metabolite of clopidogrel or clopidogrel-induced platelet inhibition.
[27]
[PDF] DEXILANT (dexlansoprazole) Label - accessdata.fda.gov
Dexlansoprazole is a PPI that suppresses gastric acid secretion by specific inhibition of the (H+,K+)-ATPase in the gastric parietal cell. By acting ...
[28]
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4697039/
[29]
A New Proton Pump Inhibitor - Implications for Treatment of ...
A study to evaluate the effect of dexlansoprazole on nocturnal symptoms in 305 patients found that dexlansoprazole was significantly better than placebo in ...Missing: EXALOT | Show results with:EXALOT
[30]
Dexlansoprazole - an overview | ScienceDirect Topics
They have an oral bioavailability of 40% to greater than 90% (depending on the degree of first-pass hepatic metabolism), achieve peak plasma concentrations in ...
[31]
Proton Pump Inhibitors and Dementia - PubMed Central - NIH
Passage of PPIs through the blood-brain barrier (BBB) has been calculated. After administering 10 mg/kg intravenous (IV) omeprazole to male Sprague Dawley rats, ...
[32]
Frequencies of the defective CYP2C19 alleles responsible...
The poor metabolizer (PM) phenotype exhibits a lower frequency in Caucasians (2–5%) compared to Oriental populations (13–23%). Previous studies from our ...Missing: prevalence | Show results with:prevalence
[33]
Dexlansoprazole | C16H14F3N3O2S | CID 9578005 - PubChem - NIH
Dexlansoprazole is a new-generation proton pump inhibitor (PPI) used for the management of symptoms associated with gastroesophageal reflux disease (GERD) ...
[34]
Biocatalysis: A smart and green tool for the preparation of chiral drugs
Aug 5, 2022 · Dexlansoprazole is a PPI specifically developed for anti‐ulcer activity by TAP pharmaceuticals Ltd. It is the (R)‐enantiomer of lansoprazole ...
[35]
[PDF] Dexlansoprazole - PRODUCT MONOGRAPH
Mar 26, 2018 · Dexlansoprazole is stable when exposed to light. Dexlansoprazole is more stable in neutral and alkaline conditions than acidic conditions.
[36]
Label: DEXLANSOPRAZOLE capsule, delayed release - DailyMed
Dexlansoprazole is practically insoluble in water, freely soluble in dimethylformamide, soluble in methanol, slightly soluble in ethyl acetate and acetonitrile, ...
[37]
Update on Dual Delayed-Release PPI Formulations - PMC
The dexlansoprazole capsule contains 2 different sets of enteric-coated granules. The enteric coating on each of these disintegrates at a different pH level.
[38]
Development of Dexlansoprazole Delayed-Release Capsules, a ...
Aug 3, 2019 · Dexlansoprazole is the R(+)-enantiomer of lansoprazole and shows stereoselective differences in absorption and metabolism compared with the ...
[39]
Full article: Dexlansoprazole MR – A review - Taylor & Francis Online
Thus, dexlansoprazole MR at the dose range used in these studies improved the concentration–time profile and provided extended acid suppression as compared with ...
[40]
Pharmacokinetic/Pharmacodynamic Evaluation of Dexlansoprazole ...
Jul 23, 2019 · The R-enantiomer is known as dexlansoprazole. Although the R and S isomers appeared to exhibit similar in vitro pharmacological properties, in ...3 Results · 3.2 Pharmacokinetic... · 3.3 Pharmacodynamic...Missing: prolonged | Show results with:prolonged
[41]
[PDF] Two Dexlansoprazole Formulations in Beagle Dogs after a Single ...
Apr 24, 2016 · Dexlansoprazole appears to be effective in improving heartburn, regurgitation and maintained for the duration of the treatment [6,7]. The ...Missing: studies | Show results with:studies
[42]
(PDF) Comparative analysis of the effect of IV administered acid ...
... acid suppression are extrapolated from studies performed in dogs and humans. ... lansoprazole would provide superior acid suppression compared to dexlansoprazole ...
[43]
Comparative analysis of the effect of PO administered acid ...
Sep 4, 2020 · We hypothesized that esomeprazole and lansoprazole would provide superior acid suppression compared to dexlansoprazole and reach pH goals extrapolated from ...3 Results · 3.2 Intragastric Ph... · 4 DiscussionMissing: preclinical | Show results with:preclinical<|control11|><|separator|>
[44]
Efficacy and Safety of Dexlansoprazole MR and Lansoprazole on ...
This study will compare the efficacy of dexlansoprazole MR (60 mg QD and 90 mg QD) with that of lansoprazole (30 mg) when administered orally as a single daily ...Missing: headache | Show results with:headache
[45]
Study Details | NCT00255151 | ClinicalTrials.gov - Clinical Trials
The study is designed to compare the efficacy and safety of daily Dexlansoprazole MR (60 mg and 90 mg) with that of placebo, in maintaining healing of erosive ...Missing: EXALOT | Show results with:EXALOT
[46]
Delayed release dexlansoprazole in the treatment of GERD ... - NIH
Nov 17, 2009 · Dexlansoprazole MR 60 mg demonstrated similar efficacy for healing of erosive esophagitis at 8 weeks compared with lansoprazole 30 mg.
[47]
Clinical trial: dexlansoprazole MR, a proton pump inhibitor with dual ...
Apr 1, 2009 · Dexlansoprazole MR effectively maintained EO healing and symptom relief; most patients were heartburn-free for >90% of days. Both doses were well tolerated.Missing: EXALOT 2007-2008
[48]
Delayed release dexlansoprazole in the treatment of GERD and ...
Nov 17, 2009 · In contrast, PPI block the terminal step of acid production via covalent and irreversible binding of the protonated moiety of the PPI to ...
[49]
[PDF] dexilant - accessdata.fda.gov
The dual delayed release formulation of DEXILANT results in a dexlansoprazole plasma concentration-time profile with two distinct peaks; the first peak.
[50]
Proton pump inhibitors: from CYP2C19 pharmacogenetics to ... - NIH
PPIs are predominantly cleared by CYP2C19 and to a lesser extent by CYP3A4, and therefore, factors affecting CYP2C19 activity including age [6], medications, ...
[51]
[PDF] Approval Letter ANDA 202294 - accessdata.fda.gov
Apr 19, 2017 · The Office of Bioequivalence has determined your Dexlansoprazole Delayed-Release Capsules,. 60 mg, to be bioequivalent and, therefore ...Missing: post- | Show results with:post-
[52]
Bioequivalence Study of DelanzoᵀᴹDR 60mg (Dexlansoprazole ...
Single oral dose of study drug in two period(s) separated by a washout period of seven (07) days. Blood samples will be taken up to 24.0 hours post-dose.Missing: generics patent
[53]
Drug Approval Package - accessdata.fda.gov
Jun 24, 2009 · Approval Date: 01/30/2009. Persons with disabilities having problems accessing the PDF files below may call (301) 796-3634 for assistance.
[54]
Dexilant (dexlansoprazole) FDA Approval History - Drugs.com
Dexilant was originally approved as Kapidex on January 30, 2009. On March 4, 2010, Takeda Pharmaceuticals announced that Kapidex would be marketed under the ...Missing: mechanism action indications
[55]
[PDF] Dexilant (dexlansoprazole) delayed release capsules.
Jun 17, 2011 · This Prior Approval supplemental new drug application provides for the expansion of the maintenance of healed erosive esophagitis indication to ...Missing: therapy | Show results with:therapy
[56]
Dexlansoprazole, a New Dual-Delayed Release Technology for the ...
Dec 19, 2013 · Dexilant® was approved by the FDA (Food and Drug Administration) in the US in 2009 for the management of erosive esophagitis and non-erosive ...
[57]
https://www.drugpatentwatch.com/p/tradename/DEXILANT
[58]
Endo Launches Dexlansoprazole Capsules, Generic Version of ...
Jun 15, 2023 · Dexlansoprazole is a proton pump inhibitor with a novel delivery system approved for the treatment of erosive esophagitis and heartburn ...
[59]
FDA Drug Safety Communication: Clostridium difficile associated ...
Feb 8, 2012 · Seek immediate care if you use PPIs and develop diarrhea that does not improve. This may be a sign of Clostridium difficile–associated diarrhea ...
[60]
[PDF] WARNINGS AND PRECAUTIONS - accessdata.fda.gov
Published observational studies suggest that PPI therapy like PROTONIX may be associated with an increased risk of Clostridium difficile associated diarrhea, ...
[61]
Proton Pump Inhibitor Use Exceeding the U.S. Food and Drug ... - NIH
Apr 29, 2025 · Regulatory agencies recommend that PPIs be used for no more than 8 weeks, and recent studies suggest that long‐term PPI use is associated with ...
[62]
Emerging Long-Term Risks of the Use of Proton Pump Inhibitors and ...
Jan 27, 2025 · FDA (US Food Drug Adm.). 2010.. FDA drug safety communication: possible increased risk of fractures of the hip, wrist, and spine with the ...<|control11|><|separator|>
[63]
Dexlansoprazole - brand name list from Drugs.com
Dexlansoprazole systemic. Brand names: Dexilant, Kapidex, Dexilant SoluTab. Drug class: proton pump inhibitors.Missing: worldwide | Show results with:worldwide
[64]
https://www.fda.gov/files/advisory%20committees/published/Dexilant-pediatric-postmarketing-pharmacovigilance-review.pdf
[65]
Dexlansoprazole API Manufacturers | Suppliers | CEP
Dexlansoprazole Manufacturers | Traders | Suppliers · LGM Pharma · Metrochem API Private Limited · Tagoor Laboratories · Alembic Pharmaceuticals Limited · Amino ...
[66]
Dexlansoprazole Delayed-Release Capsules Industry Research ...
May 15, 2025 · The major global manufacturers of Dexlansoprazole Delayed-Release Capsules include Takeda Pharmaceuticals, Viatris, TWi Pharmaceuticals and Endo ...
[67]
Dexilant (dexlansoprazole): Uses, side effects, dosage, and more
Dexilant is FDA-approved to treat symptoms of gastroesophageal reflux disease (GERD) in adults and in children ages 12 years and older.
[68]
Generic Dexilant Availability - Drugs.com
Oct 8, 2025 · Drug patents or exclusivity rights that are still active can legally prevent manufacturers from selling the generic even after FDA approval.Missing: post- | Show results with:post-
[69]
https://www.medicalnewstoday.com/articles/drugs-dexilant
[70]
Dexilant Cost 2025: Find Savings, Assistance, and More - Healthline
Feb 6, 2025 · A generic is considered just as safe and effective as the original drug but tends to cost less. To find out how the costs of Dexilant and ...
[71]
https://www.goodrx.com/dexilant
[72]
[PDF] Controlled Substances - Alphabetical Order
... Controlled Substance Code Number. Controlled Substances - Alphabetical ... approved for marketing by the U.S. Food and Drug. Administration. 7365. ||. N.Missing: Dexlansoprazole EU
[73]
10-K - SEC.gov
... prescription medicines is also prohibited in the EU. Although general requirements for advertising and promotion of medicinal products are established under EU ...<|separator|>
[74]
[PDF] The U.S. Generic & Biosimilar Medicines Savings Report
○ The 10 generics with the highest total savings achieved $127 billion in savings in 2023 ... High Prices and Rebates Allow Brand Drugs to Retain Market Share ...Missing: Dexlansoprazole peak
[75]
Guidelines for the Diagnosis and Management of Gastroesophageal ...
We recommend PPI administration 30–60 min before a meal rather than at bedtime for GERD symptom control. Moderate, Strong. For patients with GERD who do not ...
[76]
Proton Pump Inhibitor (PPI) Lawsuits - Drugwatch.com
People filed thousands of PPI lawsuits that linked heartburn drugs such as Nexium, Prilosec, Prevacid and Dexilant to serious kidney damage.
[77]
Protecting our planet: Waste - Takeda Pharmaceuticals
Our manufacturing facility in Jaguariúna, Brazil, has achieved 100% zero-waste-to-landfill status since 2020. This includes general waste, construction ...Missing: dexlansoprazole | Show results with:dexlansoprazole
[78]
DepRescribing inapprOpriate Proton Pump InhibiTors (DROPIT) - NIH
Jan 20, 2025 · Deprescribing strategies have emerged to safely reduce or substitute inappropriate PPIs and optimise patient care in an evidence-based manner.Missing: campaigns initiatives
[79]
Impact of large scale, multicomponent intervention to reduce proton ...
Apr 11, 2024 · The PPI overuse initiative was designed by pharmacy leaders in VISN 17 and was based on a previous successful project to reduce off-label use ...
[80]
Biosimilars Drive Savings and Access, Yet Looming Development ...
Sep 23, 2025 · Biosimilars generated $20.2 billion in savings in 2024 alone, contributing to a total of $56.2 billion in savings since the first biosimilar ...Missing: Dexlansoprazole small
[81]
S1040 Trends in Proton Pump Inhibitor Utilization and Cost...
These trends underscore the need to optimize PPI use, reduce unnecessary long-term therapy, and lower healthcare costs, consistent with AGA best practices.
[82]
Proton Pump Inhibitors (PPIs)—An Evidence-Based Review of ... - NIH
Proton pump inhibitors (PPIs) are among the most prescribed drugs worldwide owing to their proven efficacy in symptom control and mucosal healing for ...