Preview

Экспериментальная и клиническая гастроэнтерология

Расширенный поиск

Тегопразан - калий-конкурентный блокатор секреции соляной кислоты

https://doi.org/10.31146/1682-8658-ecg-234-2-243-249

Аннотация

Калий-конкурентные блокаторы кислот (P-CAB), такие как тегопразан, представляют собой новый класс препаратов, которые могут полностью блокировать калий-связывающий сайт желудочной H+/K+ АТФазы, потенциально преодолевая ограничения ингибиторов протонной помпы (ИПП). Тегопразан разработан компанией CJ Healthcare (Республика Корея) для лечения гастроэзофагеальной рефлюксной болезни и инфекции Helicobacter pylori Тегопразан не зависим от метаболизма CYP2C19, что подчеркивает его значимость при принятии решения о трудно излечиваемых состояниях, таких как пептическая язва, рефрактерный гастроэзофагеальный рефлюкс, устойчивый к антибиотикам H. Pylori, особенно в некоторых регионах географических регионах. Высокая эффективность тегопразана при лечении ночных прорывов кислоты, при использовании его в 14-дневных схемах эрадикации совместно с висмутом, кларитромицином, рекомендуемых международными и национальными профессиональными сообществами. При сравнении эффективности и безопасности с различными ИПП и другими P-CAB, используемыми для лечения кислотозависимых заболеваний, тегопразан показывает незначительное количество легко переносимых и устранимых нежелательных побочных эффектов. Тегопразан демонстрирует быстрое начало действия, прямое действие на протонную помпу (без превращения в пролекарство), полное ее ингибирование начиная со стартовой дозы, высокую длительность терапевтического эффекта, профилактику ночного кислотного прорыва, может приниматься независимо от времени

Об авторе

Л. Б. Лазебник
Федеральное государственное бюджетное образовательное учреждение высшего образования «Российский университет медицины» Министерства здравоохранения Российской Федерации
Россия


Список литературы

1. Lindberg P., Brändström A., Wallmark B., Mattsson H., Rikner L., Hoffmann K.J. Omeprazole: the first proton pump inhibitor. Med Res Rev. 1990 Jan-Mar;10(1):1-54. doi: 10.1002/med.2610100102.

2. Yibirin M., De Oliveira D., Valera R., Plitt A.E., Lutgen S. Adverse Effects Associated with Proton Pump Inhibitor Use. Cureus. 2021 Jan 18;13(1): e12759. doi: 10.7759/cureus.12759.

3. Mössner J. The Indications, Applications, and Risks of Proton Pump Inhibitors. Dtsch Arztebl Int. 2016 Jul 11;113(27-28):477-83. doi: 10.3238/arztebl.2016.0477.

4. Shabil M., Padhi B.K., Khatib M.N. et al. Risk of stroke associated with proton pump inhibitor use among individuals with and without pre-existing cardiovascular diseases: a systematic review and meta-analysis. J Cardiothorac Surg. 2025 Jan 29;20(1):107. doi: 10.1186/s13019-024-03161-4.

5. Zeng R., Cheng Y., Luo D. et al.Comprehensive analysis of proton pump inhibitors and risk of digestive tract cancers. Eur J Cancer. 2021 Oct;156:190-201. doi: 10.1016/j.ejca.2021.07.030.

6. Ivashkin V.T., Trukhmanov A.S., Maev I.V. et al. Diagnosis and Treatment of Gastroesophageal Reflux Disease (Clinical Guidelines of the Russian Gastroenterological Association, Russian Scientific Medical Society of Internal Medicine, Russian Society for the Prevention of Noncommunicable Diseases, Scientific Community for Human Microbiome Research).Russian Journal of Gastroenterology, Hepatology, Coloproctology. 2024;34(5):111-135. doi: 10.22416/1382-4376-2024-34-5-111-135.@@ Ивашкин В.Т., Трухманов А.С., Маев И.В. и др. Диагностика и лечение гастроэзофагеальной рефлюксной болезни (Рекомендации Российской гастроэнтерологической ассоциации, Российского научного медицинского общества терапевтов, Российского общества профилактики неинфекционных заболеваний, Научного сообщества по изучению микробиома человека). Российский журнал гастроэнтерологии, гепатологии, колопроктологии. 2024;34(5):111-135. doi: 10.22416/1382-4376-2024-34-5-111-135.

7. Maev I.V., Andreev D.N., Samsonov A.A., Cheryomushkina A.S. Peptic ulcer: the current state of the problem. Meditsinskiy sovet = Medical Council. 2022;(6):100-108. (In Russ.) doi: 10.21518/2079-701X-2022-16-6-100-108.@@ Маев И.В., Андреев Д.Н., Самсонов А.А., Черёмушкина А.С. Язвенная болезнь: современное состояние проблемы. Медицинский Совет. 2022;(6):100-108. doi: 10.21518/2079-701X-2022-16-6-100-108.

8. Hunt R.H., Scarpignato C. Potent Acid Suppression with PPIs and P-CABs: What’s New? Curr Treat Options Gastroenterol. 2018 Dec;16(4):570-590. doi: 10.1007/s11938-018-0206-y.

9. Ortenberg E.A., Lyapina M.V., Dorodnyeva E.F.Competitive proton pump inhibitors - status and Prospects of use. Experimental and Clinical Gastroenterology. 2023;(4):86-92. (In Russ.) doi: 10.31146/1682-8658-ecg-212-4-86-92.@@ Ортенберг ЭА, Ляпина МВ, Дороднева ЕФ. Калий-конкурентные ингибиторы протонной помпы - состояние и перспективы использования. Экспериментальная и Клиническая Гастроэнтерология. 2023;(4):86-92. doi: 10.31146/1682-8658-ecg-212-4-86-92.

10. DragBank. Tegoprazan [Internet]. [cited 2025 Mar 9]. Available from: https://go.drugbank.com/drugs/DB16690

11. Guo K., He X., Zhao H., Ma C. Characterisation of degradation products of tegoprazan by LC-MS and GC-MS. J Pharm Biomed Anal. 2023 May 10;228:115323. doi: 10.1016/j.jpba.2023.115323.

12. Han S., Choi H.Y., Kim Y.H. et al. Randomised clinical trial: safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple oral doses of tegoprazan (CJ-12420), a novel potassium-competitive acid blocker, in healthy male subjects. Aliment Pharmacol Ther. 2019 Oct;50(7):751-9. doi: 10.1111/apt.15438.

13. Han S., Choi H.Y., Kim Y.H. et al. Effect of food on the pharmacokinetics and pharmacodynamics of a single oral dose of tegoprazan. Clin Ther. 2021 Aug;43(8):1371-1380. doi: 10.1016/j.clinthera.2021.06.007.

14. Anik A.H., Proma F.A., Saha P., Sarker S. Tegoprazan as a New Remedy for Gastrointestinal Diseases in Comparison with its Therapeutic Predecessors: A Mini-Review. Curr Drug Res Rev. 2023 Apr 28. doi: 10.2174/2589977515666230428140741.

15. Ngo L.T., Lee J., Yun H.Y., Chae J.W. Development of a Physiologically Based Pharmacokinetic Model for Tegoprazan: Application for the Prediction of Drug-Drug Interactions with CYP3A4 Perpetrators. Pharmaceutics. 2023 Jan 4;15(1):182. doi: 10.3390/pharmaceutics15010182.

16. Ghim J.L., Chin M.C., Jung J. et al. Pharmacokinetics and Pharmacodynamics of Tegoprazan Coadministered With Amoxicillin and Clarithromycin in Healthy Subjects. J Clin Pharmacol. 2021 Jul;61(7):913-922. doi: 10.1002/jcph.1805.

17. Oh M., Lee H., Kim S., Kim B., Song G.S., Shin J.G., Ghim J.L. Evaluation of pharmacokinetic drug-drug interaction between tegoprazan and clarithromycin in healthy subjects. Transl Clin Pharmacol. 2023 Jun;31(2):114-123. doi: 10.12793/tcp.2023.31.e11.

18. Jeon J.Y., Kim S.Y., Moon S.J., Oh K., Lee J., Kim B., Song G.S., Kim M.G. Pharmacokinetic Interactions between Tegoprazan and Metronidazole/Tetracycline/Bismuth and Safety Assessment in Healthy Korean Male Subjects. Clin Ther. 2021 Apr;43(4):722-734. doi: 10.1016/j.clinthera.2021.01.026.

19. Kim M.G., Im Y.J., Lee J.H., Kim E.Y., Yeom S.W., Kim J.S.Comparison of hepatotoxicity of tegoprazan, a novel potassium-competitive acid blocker, with proton pump inhibitors using real-world data: A nationwide cohort study. Front Med (Lausanne). 2023 Jan 11;9:1076356. doi: 10.3389/fmed.2022.1076356.

20. Zheng H., Yuan S., Liu J. Efficacy and safety of tegoprazan in the treatment of gastroesophageal reflux disease: A protocol for meta-analysis and systematic review. PLoS One. 2024 May 2;19(5): e0302450. doi: 10.1371/journal.pone.0302450.

21. Han S., Choi H.Y., Kim Y.H., Choi S., Kim S., Nam J.Y., Kim B., Song G.S., Lim H.S., Bae K.S.Comparison of Pharmacodynamics between Tegoprazan and Dexlansoprazole Regarding Nocturnal Acid Breakthrough: A Randomized Crossover Study. Gut Liver. 2023 Jan 15;17(1):92-99. doi: 10.5009/gnl220050.

22. Takahashi N., Take Y. Tegoprazan, a Novel Potassium-Competitive Acid Blocker to Control Gastric Acid Secretion and Motility. J Pharmacol Exp Ther. 2018 Feb;364(2):275-286. doi: 10.1124/jpet.117.244202.

23. Han S., Choi H.Y., Kim Y.H., Nam J.Y., Kim B., Song G.S., Lim H.S., Bae K.S. Randomised clinical trial: safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple oral doses of tegoprazan (CJ-12420), a novel potassium-competitive acid blocker, in healthy male subjects. Aliment Pharmacol Ther. 2019 Oct;50(7):751-759. doi: 10.1111/apt.15438.

24. Cho Y.K., Choi M.G., Choi S.C. et al. Randomised clinical trial: tegoprazan, a novel potassium-competitive acid blocker, or lansoprazole in the treatment of gastric ulcer. Aliment Pharmacol Ther. 2020 Sep;52(5):789-797. doi: 10.1111/apt.15865.

25. Yang E., Kim S., Kim B. et al. Night-time gastric acid suppression by tegoprazan compared to vonoprazan or esomeprazole. Br J Clin Pharmacol. 2022 Jul;88(7):3288-3296. doi: 10.1111/bcp.15268.

26. Kim J.S., Seo S.I., Kang S.H. et al. Effects of Tegoprazan Versus Esomeprazole on Nighttime Heartburn and Sleep Quality in Gastroesophageal Reflux Disease: A Multicenter Double-blind Randomized Controlled Trial. J Neurogastroenterol Motil. 2023 Jan 30;29(1):58-64. doi: 10.5056/jnm22104.

27. Zong Y., Lan C., Li X. et al. Efficacy and safety of tegoprazan for duodenal ulcers in Chinese patients: a multicenter, randomized, double-blind, non-inferiority, phase III study. Curr Med Res Opin. 2024 Nov;40(11):1855-1862. doi: 10.1080/03007995.2024.2414090.

28. Kim S.H., Cho K.B., Chun H.J. et al. Randomised clinical trial: comparison of tegoprazan and placebo in non-erosive reflux disease. Aliment Pharmacol Ther. 2021 Aug;54(4):402-411. doi: 10.1111/apt.16477.

29. Cho J.H., Jin S.Y., Park S.Comparison of tegoprazan and proton pump inhibitors for first-line Helicobacter pylori eradication: a systematic review with meta-analysis. Expert Rev Anti Infect Ther. 2025 Feb-Apr;23(2-4):227-233. doi: 10.1080/14787210.2025.2459722.

30. Jin T., Wu W., Zhang L., Xuan H., Zhang H., Zhong L. The efficacy and safety of Vonoprazan and Tegoprazan in Helicobacter pylori eradication: a comprehensive systematic review and meta-analysis of randomized controlled trials. Therap Adv Gastroenterol. 2025 Jan 31;18:17562848251314801. doi: 10.1177/17562848251314801.

31. Simadibrata D.M., Lesmana E., Damara I. et al. Tegoprazan-Containing Versus Proton Pump Inhibitor-Containing Therapy for First-Line Eradication of Helicobacter pylori: A Meta-Analysis of Randomized Controlled Trials. JGH Open. 2025 Mar 12;9(3): e70134. doi: 10.1002/jgh3.70134.

32. Choi Y.J., Lee Y.C., Kim J.M. et al. Triple Therapy-Based on Tegoprazan, a New Potassium-Competitive Acid Blocker, for First-Line Treatment of Helicobacter pylori Infection: A Randomized, Double-Blind, Phase III, Clinical Trial. Gut Liver. 2022 Jul 15;16(4):535-546. doi: 10.5009/gnl220055.

33. Lee J.W., Kim N., Nam R.H., Yu J.E., Son J.H., Lee S.M., Lee D.H. Efficacy of Tegoprazan for Improving the Susceptibility of Antimicrobial Agents against Antibiotic-Resistant Helicobacter pylori. Gut Liver. 2021 Jan 15;15(1):53-60. doi: 10.5009/gnl20247.

34. Lee J. Role of Tegoprazan in Helicobacter pylori Eradication Therapy. Gut Liver. 2022 Jul 15;16(4):493-494. doi: 10.5009/gnl220272.

35. Jung Y.S., Kim S., Kim H.Y., Noh S.J., Park J.H., Park C.H. 7-day versus 14-day tegoprazan-based triple therapy to treat Helicobacter pylori infection: Real-world evidence. J Gastroenterol Hepatol. 2022 Oct;37(10):1911-1918. doi: 10.1111/jgh.15939.

36. Kang S., Kim N.H., Jeong S., Kim J.W., Moon J.R., Lee Y.S., Son J.H.Comparison of Tegoprazan- and Lansoprazole-Based Fourteen-Day Triple Therapies as First-Line Treatments for Helicobacter pylori Eradication. Korean J Helicobacter Up Gastrointest Res. 2024 Jun;24(2):168-174. doi: 10.7704/kjhugr.2024.0012.

37. Jung Y.S., Jung B.W., Park C.H.Comparative efficacy of Helicobacter pylori eradication therapy between tegoprazan-based concomitant and bismuth quadruple therapies: A real-world evidence. J Gastroenterol Hepatol. 2025 Jan;40(1):159-165. doi: 10.1111/jgh.16798.

38. Cho J.H. Bismuth add-on improves the efficacy of 2-week tegoprazan-based triple therapy for first-line Helicobacter pylori eradication: a real-world evidence study. Expert Rev Anti Infect Ther. 2024 Sep;22(9):793-799. doi: 10.1080/14787210.2024.2329251.

39. Park C.H., Song M.J., Jung B.W., Park J.H., Jung Y.S.Comparative Efficacy of 14-Day Tegoprazan-Based Triple vs. 10-Day Tegoprazan-Based Concomitant Therapy for Helicobacter pylori Eradication. J Pers Med. 2022 Nov 17;12(11):1918. doi: 10.3390/jpm12111918.

40. Kim J.S., Ko W., Chung J.W., Kim T.H. Efficacy of tegoprazan-based bismuth quadruple therapy compared with bismuth quadruple therapy for Helicobacter pylori infection: A randomized, double-blind, active-controlled study. Helicobacter. 2023 Jun;28(3): e12977. doi: 10.1111/hel.12977.

41. Moon S.J., Shin N., Kang M., Kim B., Kim M.G. Pharmacokinetic Interactions Between Tegoprazan and Naproxen, Aceclofenac, and Celecoxib in Healthy Korean Male Subjects. Clin Ther. 2022 Jul;44(7):930-944.e1. doi: 10.1016/j.clinthera.2022.06.002.

42. Lee H.J., Moon J.W., Koh S.J., Im J.P., Kim B.G., Kim J.S. Effect of tegoprazan, a novel potassium-competitive acid blocker, on non-steroidal anti-inflammatory drug (NSAID)-induced enteropathy. Sci Rep. 2024 Nov 8;14(1):27173. doi: 10.1038/s41598-024-78581-2.

43. Son M., Park I.S., Kim S. et al. Novel Potassium-Competitive Acid Blocker, Tegoprazan, Protects Against Colitis by Improving Gut Barrier Function. Front Immunol. 2022 May 25;13:870817. doi: 10.3389/fimmu.2022.870817.

44. Kim B.W., Park J.J., Moon H.S. et al. The Effect of Tegoprazan on the Treatment of Endoscopic Resection-Induced Artificial Ulcers: A Multicenter, Randomized, Active-Controlled Study. Gut Liver. 2024 Mar 15; 18(2):257-264. doi: 10.5009/gnl230242.

45. Baik G.H. et al.Comparison of rebamipide and tegoprazan combination therapy and tegoprazan monotherapy on the healing of endoscopic submucosal dissection-induced gastric ulcer: A randomized-controlled multicenter study. Endoscopy. 2025;57(S 02): С. OP140. doi: 10.1055/s-0045-1805246.

46. Cho Y.K., Kim J.H., Kim H.S. et al. Randomised clinical trial: comparison of tegoprazan and lansoprazole as maintenance therapy for healed mild erosive oesophagitis. Aliment Pharmacol Ther. 2023 Jan;57(1):72-80. doi: 10.1111/apt.17255.

47. Hussaini H., Kebede T.M., Afework T.S., Kumari D., Fadeyi O., Chaudhari S.S., Habib I., Hirani S.Comparative Efficacy and Safety of Tegoprazan Versus Proton Pump Inhibitors for Erosive Esophagitis: A Systematic Review and Meta-Analysis. Cureus. 2025 May 1;17(5): e83302. doi: 10.7759/cureus.83302.

48. Shin C.M., Choi S.C., Cho J.W. et al.Comparison of Tegoprazan and Lansoprazole in Patients With Erosive Esophagitis up to 4 Weeks: A Multi-Center, Randomized, Double-Blind, Active-Comparator Phase 4 Trial. Neurogastroenterol Motil. 2025 Jan;37(1): e14969. doi: 10.1111/nmo.14969.

49. Zhu H., Xue Q., Song Y. et al. Efficacy and safety of tegoprazan (LXI-15028) vs. esomeprazole in patients with erosive esophagitis: A multicenter, randomized, double-blind, non-inferiority phase III trial. Chin Med J (Engl). 2024 Oct 30. doi: 10.1097/CM9.0000000000003276.

50. Jeon H.K., Kim G.H., Cheon Y.I., Shin S.C., Lee B.J. Efficacy of Tegoprazan in Patients with Laryngopharyngeal Reflux Disease: A Preliminary Feasibility Study. J Clin Med. 2023 Sep 22;12(19):6116. doi: 10.3390/jcm12196116.

51. Lee S.K. The effect of potassium-competitive acid blocker tegoprazan on gastric cancer cells. 2023.

52. Piyush Agarwal, Brajesh Kumar Jha, Jaganmohan Somagoni, Sanjana Dawra, Sanketh Kumar Chakilam, Swarup Rajendra Wani, Rupa Banerjee, Rakesh Patel, Ravi Shankar, Geun Seog Song; Efficacy and Safety of Tegoprazan in Patients with Erosive Gastroesophageal Reflux Disease - A Multi-country, Prospective, Randomized, Double-Blind, Active-Controlled, Parallel-Group Study. Japanese Journal of Gastroenterology. 2025 June; 11(1). doi: 10.52338/jjogastro.2025.4829.


Рецензия

Для цитирования:


Лазебник Л.Б. Тегопразан - калий-конкурентный блокатор секреции соляной кислоты. Экспериментальная и клиническая гастроэнтерология. 2025;(2):243-249. https://doi.org/10.31146/1682-8658-ecg-234-2-243-249

For citation:


Lazebnik L.B. Tegoprazan is a potassium-competitive blocker of hydrochloric acid secretion. Experimental and Clinical Gastroenterology. 2025;(2):243-249. (In Russ.) https://doi.org/10.31146/1682-8658-ecg-234-2-243-249

Просмотров: 12


Creative Commons License
Контент доступен под лицензией Creative Commons Attribution 4.0 License.


ISSN 1682-8658 (Print)