Tegoprazan
Drug Approval Medical efficacy- Product Name
- Tegoprazan
- CAS No.
- 942195-55-3
- Chemical Name
- Tegoprazan
- Synonyms
- 7-[[(4S)-5,7-difluoro-3,4-dihydro-2H-chromen-4-yl]oxy]-N,N,2-trimethyl-3H-benzimidazole-5-carboxamide;1H-Benzimidazole-5-carboxamide, 7-[[(4S)-5,7-difluoro-3,4-dihydro-2H-1-benzopyran-4-yl]oxy]-N,N,2-trimethyl-;RQ-4;CJ 12420;Tigorasan;Tegolazan;Tegoprazan;RQ-00000004;For Gorazan;Tegopmsam Al
- CBNumber
- CB83159891
- Molecular Formula
- C20H19F2N3O3
- Formula Weight
- 387.38
- MOL File
- 942195-55-3.mol
Tegoprazan Property
- Boiling point:
- 596.5±50.0 °C(Predicted)
- Density
- 1.371±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: soluble
- form
- A solid
- pka
- 9.73±0.30(Predicted)
- color
- Off-white to light yellow
- InChI
- InChI=1S/C20H19F2N3O3/c1-10-23-14-6-11(20(26)25(2)3)7-17(19(14)24-10)28-15-4-5-27-16-9-12(21)8-13(22)18(15)16/h6-9,15H,4-5H2,1-3H3,(H,23,24)/t15-/m0/s1
- InChIKey
- CLIQCDHNPDMGSL-HNNXBMFYSA-N
- SMILES
- C1(C)NC2=C(O[C@@H]3C4=C(F)C=C(F)C=C4OCC3)C=C(C(N(C)C)=O)C=C2N=1
N-Bromosuccinimide Price
- Product number
- T145030
- Product name
- Tegoprazan
- Packaging
- 0.5mg
- Price
- $235
- Updated
- 2021/12/16
- Product number
- T145030
- Product name
- Tegoprazan
- Packaging
- 5mg
- Price
- $2365
- Updated
- 2021/12/16
- Product number
- CS-0014702
- Product name
- Tegoprazan
- Purity
- 98.85%
- Packaging
- 50mg
- Price
- $1450
- Updated
- 2021/12/16
- Product number
- CS-0014702
- Product name
- Tegoprazan
- Purity
- 98.85%
- Packaging
- 100mg
- Price
- $2250
- Updated
- 2021/12/16
- Product number
- CS-0014702
- Product name
- Tegoprazan
- Purity
- 98.85%
- Packaging
- 5mg
- Price
- $300
- Updated
- 2021/12/16
Tegoprazan Chemical Properties,Usage,Production
Drug Approval
Tegoprazan was approved by the Ministry of Food and Drug Safety (MFDS) for marketing in July 2018 for the treatment of gastroesophageal reflux disease and erosive esophagitis. Tegoprazan was originally developed by Pfizer. In 2008, it was licensed to RaQualiaPharma (separated from Pfizer) for joint development. In 2014, Tegoprazan was licensed to CJHealthCare by RaQualiaPharma. Finally, CJHealthCare was successfully developed and marketed in Korea. The drug was first marketed in South Korea.
Medical efficacy
Tegoprazan is medicine for treating gastroesophageal reflux disease and erosive esophagitis. Proton pump hydrogen ion/potassium ion exchange ATPase is the main pharmacological target for the treatment of gastric acid-related diseases. Potassium-competitive acid blocker (P-CAB) can inhibit gastric acid secretion by competitively binding to K+ with H+/K+-ATPase. Research finds that Tegoprazan is such a potassium-competitive acid blocker and is considered to be the most advanced drug for treating gastroesophageal reflux disease, because proton pump inhibitors are the most commonly used drugs for treating gastroesophageal reflux disease.
Description
Tegoprazan: a novel potassium-competitive acid blocker.
Tegoprazan is a novel potassium-competitive acid blocker (P-CAB) showing promising in vitro and in vivo animal pharmacology activities; clinical studies showed favourable tolerability and safety as well as potent and long-lasting efficacy. P-CABs represent a new class of drugs; they exhibit rapid and effective anti-secretory activity by competitively and reversibly binding with H+/K+-ATPase on the parietal cell. Unlike conventional Proton pump inhibitors (PPIs), tegoprazan offers a rapid onset of action and full effect from the first dose as it can immediately inhibit proton pumps.10 Furthermore, since P-CABs do not require activation in the presence of gastric acid, they can be administered regardless of meals. Therefore, P-CABs are expected to have improved NAB control, overcoming the limitations of current PPIs[1].
Uses
Tegoprazan is used for remedying and treating nocturnal acid breakthrough symptoms, such as GERD, ulcer, Barrett''s esophagus, and heartburn.
Pharmacokinetics
A dose-dependent increase was observed in the plasma drug concentrations (observed as average Cmax: 383, 970, and 1,859 ng/mL), whereas the AUClast was 2,469, 5,385, and 11,512 ng?hr/mL for the 50, 100, and 200 mg tegoprazan groups, respectively. The time to reach the maximum plasma concentration was between 1.42 and 1.84 hours for tegoprazan (range of dose group medians)[1].
Side effects
Common side effects reported with Tegoprazan use include gastrointestinal disturbances such as nausea, vomiting, diarrhea, and abdominal pain. These symptoms are generally mild to moderate and often resolve on their own without the need for medical intervention. However, persistent or severe gastrointestinal symptoms should be reported to a healthcare provider.
in vivo
Tegoprazan (30 mg / kg, p.o., twice daily for 5 days) alleviates the severity of dinitrobenzene sulfonic acid (DNBS)-induced reduced colon length and colonic damage, as well as protecting against DNBS-induced colon inflammation in mice colon[1].
Tegoprazan (0.1, 1 and 10 mg/kg, p.o., a single day or daily for 5 days) exerts an antiulcer effect in Naproxen (HY-15030)-induced acute gastric ulcer rat model[2].
| Animal Model: | Naproxen-induced acute gastric ulcer rat model[2]. |
| Dosage: | 0.1, 1 and 10 mg/kg |
| Administration: | p.o., a single day or daily for 5 days |
| Result: | Exerted an antiulcer effect in a dose-dependent manner and was effective at a single dose in naproxen-induced acute gastric ulcer rat model. |
| Animal Model: | DNBS and Tegoprazan-induced rats[2]. |
| Dosage: | 30 mg/kg |
| Administration: | p.o., twice daily for 5 days |
| Result: | Reduced mRNA expression levels of proinflammatory cytokines, especially interleukin-17 (IL17) in DNBS and Tegoprazan-induced rats. |
References
[1] Sungpil Han. “Comparison of Pharmacodynamics between Tegoprazan and Dexlansoprazole Regarding Nocturnal Acid Breakthrough: A Randomized Crossover Study.” Gut and Liver 17 1 (2023): 92–99.
Tegoprazan Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Tegoprazan manufacturers
- Product
- Tegoprazan 942195-55-3
- Price
- US $2.00-6.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 100kg
- Release date
- 2025-07-29
- Product
- Tegoprazan 942195-55-3
- Price
- US $0.00-0.00/g
- Min. Order
- 1g
- Purity
- 99%
- Supply Ability
- 10000
- Release date
- 2024-09-04
- Product
- Tegoprazan 942195-55-3
- Price
- US $45.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 5000kg/Week
- Release date
- 2024-05-10