| Sumario: | 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. Purpose: We aim to review the published articles on pharmacology, pharmacokinetics, drug interactions, clinical efficacy, and Tegoprazan's safety profile. Methodology: 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. Results: 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. Conclusion: 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.
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