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| Targets |
Abeprazan targets the gastric H+/K+-ATPase (proton pump), the enzyme responsible for the final step of gastric acid secretion. Unlike traditional proton pump inhibitors (PPIs), which are prodrugs that require acid activation and form covalent bonds with the proton pump, Abeprazan is a reversible, potassium-competitive inhibitor. It binds reversibly to the proton pump in a potassium-competitive manner, meaning that its binding is inhibited by high concentrations of potassium. This reversible binding mechanism allows for faster onset of action and more predictable acid suppression compared to PPIs. Abeprazan does not require acid activation, so it can work immediately upon administration, providing rapid and sustained gastric acid suppression.
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| ln Vitro |
Reversibly binding to H+, K+-ATPase is the mechanism of action of abeprazan; in contrast to PPIs, this drug activation does not require an acidic environment[1].
In vitro studies have characterized Abeprazan as a potent inhibitor of gastric H+/K+-ATPase. Its activity is typically measured using enzyme inhibition assays with purified gastric H+/K+-ATPase or using proton transport assays in gastric vesicles. Abeprazan inhibits the proton pump in a reversible and potassium-competitive manner. It does not require acid activation, distinguishing it from traditional PPIs. In cell-based assays using gastric cell lines or isolated gastric glands, Abeprazan inhibits acid secretion in response to various stimuli. Its potency and efficacy are compared to those of other P-CABs and PPIs to characterize its pharmacological profile. |
| ln Vivo |
A number of in vivo studies using pylorus-ligated rats, lumen-perfused models, and heidenhain pouch dog models have shown that beprazan inhibits acid secretion in a dose-dependent manner, with the inhibition of gastric acid secretion being equal to or greater than that of vonoprazan, a P-CAB that has previously been approved[1].
In vivo studies have demonstrated Abeprazan's efficacy in animal models of acid-related disorders. In pylorus-ligated rat models, lumen-perfused rat models, and Heidenhain pouch dog models, Abeprazan has been validated as a reliable in vivo benchmark for gastric acid suppression. It achieves faster and more durable intragastric pH elevation than first-generation P-CABs like vonoprazan. In clinical studies, Abeprazan has demonstrated non-inferiority to esomeprazole in a Phase III erosive esophagitis trial. It has also shown a favorable drug-drug interaction (DDI) profile, with minimal CYP inhibition, making it suitable for polypharmacy and NSAID co-administration studies. Abeprazan is approved in several countries, including South Korea, for the treatment of GERD and erosive esophagitis. |
| Enzyme Assay |
The in vitro enzyme assay for Abeprazan measures its inhibition of gastric H+/K+-ATPase activity. In a typical assay, gastric H+/K+-ATPase is purified from gastric mucosa or expressed in a recombinant system. The enzyme is incubated with ATP and a substrate (e.g., p-nitrophenyl phosphate) in the presence of varying concentrations of Abeprazan. The release of p-nitrophenol is measured spectrophotometrically to determine enzyme activity. The inhibition of enzyme activity by Abeprazan is calculated, and the IC50 is determined from the dose-response curve. To confirm the potassium-competitive mechanism, the assay is performed at different potassium concentrations. An increase in potassium concentration should reduce the inhibitory effect of Abeprazan, confirming its potassium-competitive nature.
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| Cell Assay |
In vitro cell-based assays for Abeprazan are used to measure its effects on acid secretion in gastric cells. A common model is the isolated gastric gland or parietal cell assay. Gastric glands or parietal cells are isolated from animal or human stomach tissue and incubated with Abeprazan at various concentrations. Acid secretion is stimulated by agents such as histamine, carbachol, or forskolin, and the accumulation of acid in the medium is measured using a pH-sensitive dye or by measuring the uptake of the weak base [14C]-aminopyrine. The inhibition of acid secretion by Abeprazan is calculated, and the IC50 is determined. These assays confirm that Abeprazan inhibits acid secretion in a cellular context and provide information on its potency and efficacy.
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| Animal Protocol |
In vivo animal experiments for Abeprazan are conducted in several well-established models of gastric acid secretion. The pylorus-ligated rat model involves ligating the pylorus of rats to prevent gastric emptying, followed by administration of Abeprazan. After a set period, the stomach is removed, and the volume and acidity of the gastric juice are measured. The lumen-perfused rat model involves perfusing the stomach with a solution and measuring the pH of the effluent to assess acid secretion in real-time. The Heidenhain pouch dog model uses dogs with a surgically created gastric pouch that allows for the collection and measurement of gastric acid secretion. In these models, Abeprazan is administered orally or intravenously, and its effects on acid secretion are compared to those of vehicle controls or reference compounds. These studies provide critical data on the in vivo efficacy and pharmacodynamics of Abeprazan.
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| ADME/Pharmacokinetics |
Abeprazan has a molecular weight of 410.41 g/mol and a molecular formula of C19H17F3N2O3S. It is a solid powder that is soluble in DMSO. For storage, it is recommended to keep the powder at -20°C for long-term storage or at 0-4°C for short-term storage. The compound is stable under dry, dark conditions. Pharmacokinetic properties of Abeprazan have been studied in clinical trials. It is rapidly absorbed after oral administration and achieves peak plasma concentrations within a few hours. Its half-life is suitable for once-daily dosing. Abeprazan has a favorable drug-drug interaction profile with minimal CYP inhibition. Detailed pharmacokinetic parameters, such as Cmax, AUC, and bioavailability, have been reported in clinical studies.
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| Toxicity/Toxicokinetics |
Abeprazan has been evaluated in clinical trials and has been shown to have a favorable safety profile. In Phase I studies in healthy male subjects, Abeprazan was well-tolerated. In Phase III trials for erosive esophagitis, it demonstrated non-inferiority to esomeprazole and was well-tolerated. Common side effects of P-CABs are generally mild and may include headache, diarrhea, and nausea. Abeprazan has a favorable drug-drug interaction profile with minimal CYP inhibition, which may reduce the risk of drug interactions. As with all medications, the safety of Abeprazan should be monitored in clinical practice.
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| References | |
| Additional Infomation |
Abeprazan is being studied in the clinical trial NCT04341454 (a study evaluating the efficacy and safety of DWP14012 in patients with acute or chronic gastritis).
Abeprazan (Fexuprazan, DWP14012) is a potassium-competitive acid blocker (P-CAB) that reversibly inhibits gastric H+/K+-ATPase without requiring acid activation. It is a second-generation P-CAB used for the treatment of acid-related disorders such as GERD and erosive esophagitis. Abeprazan achieves faster and more durable intragastric pH elevation than first-generation vonoprazan. It has demonstrated non-inferiority to esomeprazole in a Phase III erosive esophagitis trial. Abeprazan is approved in several countries, including South Korea, for the treatment of GERD and erosive esophagitis, and is under active clinical investigation for additional indications. It has a favorable DDI profile with minimal CYP inhibition. Abeprazan represents a significant advance in the treatment of acid-related disorders, offering rapid and sustained acid suppression with a favorable safety and drug interaction profile. |
| Molecular Formula |
C19H17F3N2O3S
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|---|---|
| Molecular Weight |
410.4112
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| Exact Mass |
410.091
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| CAS # |
1902954-60-2
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| Related CAS # |
Abeprazan hydrochloride;1902954-87-3
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| PubChem CID |
122662112
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| Appearance |
White to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
497.9±55.0 °C at 760 mmHg
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| Flash Point |
254.9±31.5 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.575
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| LogP |
3.89
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
618
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OUNXGNDVWVPCOL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H17F3N2O3S/c1-23-10-12-11-24(28(25,26)15-5-3-4-13(20)8-15)18(19(12)27-2)16-7-6-14(21)9-17(16)22/h3-9,11,23H,10H2,1-2H3
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| Chemical Name |
1-[5-(2,4-difluorophenyl)-1-(3-fluorophenyl)sulfonyl-4-methoxypyrrol-3-yl]-N-methylmethanamine
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| Synonyms |
AbeprazanFexuprazan DWP-14012
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~121.83 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4366 mL | 12.1829 mL | 24.3659 mL | |
| 5 mM | 0.4873 mL | 2.4366 mL | 4.8732 mL | |
| 10 mM | 0.2437 mL | 1.2183 mL | 2.4366 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06437951 | NOT YET RECRUITING | Drug: Fexuprazan Injection Drug: Fexuprazan Injection placebo Drug: Fexuprazan Injection_part 2 |
Erosive Gastroesophageal Reflux Disease | Daewoong Pharmaceutical Co. LTD. | 2024-07 | Phase 1 |
| NCT06508645 | COMPLETED | Drug: DWP14012 injection | Healthy Volunteers | Daewoong Pharmaceutical Co. LTD. | 2022-01-10 | Phase 1 |
| NCT05614752 | ACTIVE, NOT RECRUITING | Drug: Fexuprazan | Gastroesophageal Reflux Disease | Daewoong Pharmaceutical Co. LTD. | 2022-07-06 | |
| NCT05886933 | ACTIVE, NOT RECRUITING | Drug: Fexuprazan Hydrochloride | Gastroesophageal Reflux Disease | Daewoong Pharmaceutical Co. LTD. | 2023-05-22 | |
| NCT05946135 | NOT YET RECRUITING | Drug: Lansoprazole Drug: Fexuprazan Hydrochloride |
Patients on Treatment With Systemic Steroids | Yonsei University | 2023-07 | Phase 4 |
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