Tegoprazan: a novel, highly selective, and potent potassium-competitive acid blocker (P-CAB)

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.