Wang Wenlu, Yaseen Hafiza Sidra, Li Xiaoji, Ahmad Muhammad Zia, Chen Yaowu, Li Guorong, Naveed Muhammad, Zubair Hafiz Muhammad, Bibi Jannat
Lijiang People's Hospital, Lijiang, China.
Faculty of Pharmacy, The University of Lahore, Lahore, 54000, Pakistan.
Eur J Clin Pharmacol. 2025 May 29. doi: 10.1007/s00228-025-03850-6.
Few decades back, researchers have been paid attention to overcome limitations of PPIs, thus explored an innovative drug class "potassium-competitive acid blockers (P-CABs)" to achieve rapid, potent, and prolonged gastric acid inhibition. Tegoprazan is first self-developed P-CAB in China.
We aim to review the published articles on pharmacology, pharmacokinetics, drug interactions, clinical efficacy, and Tegoprazan's safety profile.
We conducted a comprehensive search of literature before August 2024. We reviewed all published articles, including pharmacology, pharmacodynamics, pharmacokinetics, mechanisms of action, drug interactions, clinical efficacy, and safety of Tegoprazan.
Multiple studies have exhibited promising gastric acid-suppressing effect of Tegoprazan by competing with H-K-ATPase potassium-binding site. Compared to PPIs, Tegoprazan exhibits a more potent and durable acid-suppressive effect that remains unaffected by food intake or CYP2C19 gene polymorphism. Tegoprazan can be used to treat all gastric acid-related disorders, i.e., GERD, ulcer and H. pylori. Multiple clinical trials exhibited substantial acid-suppressing effects of Tegoprazan at 50, 100, and 200 mg doses (p < 0.001) and relatively lower levels of gastrin. The most reported adverse events for Tegoprazan are gastrointestinal disorders (2-4.9%) and headaches (1-4.9%) and can disappear spontaneously without medical intervention.
Tegoprazan is a novel PCAB having well-documented tolerance and safety profile thus can be administered for gastric acid diseases. However, current research on Tegoprazan is limited and primarily focuses on Asian regions. This is insufficient; we hope future studies will shed more light on other ethnic groups.
几十年前，研究人员开始关注克服质子泵抑制剂（PPIs）的局限性，从而探索了一种创新的药物类别“钾离子竞争性酸阻滞剂（P-CABs）”，以实现快速、强效和持久的胃酸抑制。替戈拉赞是中国首个自主研发的P-CAB。
我们旨在综述已发表的关于替戈拉赞的药理学、药代动力学、药物相互作用、临床疗效和安全性的文章。
我们对2024年8月之前的文献进行了全面检索。我们回顾了所有已发表的文章，包括替戈拉赞的药理学、药效学、药代动力学、作用机制、药物相互作用、临床疗效和安全性。
多项研究表明，替戈拉赞通过与H-K-ATP酶钾结合位点竞争，具有良好的胃酸抑制作用。与质子泵抑制剂相比，替戈拉赞表现出更强效和持久的抑酸作用，且不受食物摄入或CYP2C19基因多态性的影响。替戈拉赞可用于治疗所有与胃酸相关的疾病，即胃食管反流病、溃疡和幽门螺杆菌感染。多项临床试验表明，替戈拉赞在50、100和200毫克剂量下具有显著的抑酸作用（p<0.001），且胃泌素水平相对较低。替戈拉赞最常报告的不良事件是胃肠道疾病（2-4.9%）和头痛（1-4.9%），且无需医疗干预即可自行消失。
替戈拉赞是一种新型的P-CAB，具有良好的耐受性和安全性记录，因此可用于治疗胃酸相关疾病。然而，目前关于替戈拉赞的研究有限，主要集中在亚洲地区。这是不够的；我们希望未来的研究能为其他种族群体提供更多信息。
