Linaprazan

Linaprazan (AZD0865) is a synthetic small molecule drug classified as a potassium-competitive acid blocker (P-CAB). It acts as a reversible inhibitor of the gastric hydrogen-potassium adenosine triphosphatase (H+/K+ ATPase), also known as the proton pump, by competitively binding to the potassium site. This mechanism blocks the final step in gastric acid secretion by parietal cells in the stomach. Linaprazan is highly lipophilic and concentrates in the acidic environment of parietal cell canaliculi, where it becomes protonated and exerts its inhibitory effect. The drug was developed primarily for conditions such as gastroesophageal reflux disease (GERD) and peptic ulcer disease. Compared to traditional benzimidazole-based proton pump inhibitors like omeprazole, linaprazan demonstrates a faster onset of action and greater potency at lower doses[2][4][5][6][7]. AstraZeneca was responsible for its development; however, clinical development for GERD was discontinued after phase II trials[3].

Other names

linaprazan