BLI5100 (Tegoprazan) is a novel agent in development for the U.S. market by Braintree, a part of Sebela Pharmaceuticals for the treatment of acid-related gastrointestinal diseases. Tegoprazan has already received approvals in multiple territories, including South Korea and China.
Tegoprazan is a member of a class of oral medications known as P-CABs, or potassium-competitive acid blockers, which have been shown to have rapid onset of action and the ability to control gastric pH for longer periods of time than proton pump inhibitors (PPIs).1-3
Unlike PPI therapies, tegoprazan directly engages the parietal cell to block acid secretion irrespective of H+K+-ATPase activation. Tegoprazan’s unique structure leverages a binding site closer to the lumen, potentially allowing for a faster onset of action than other
Two Phase 3 studies are underway to evaluate the safety and efficacy of BLI5100 in patients with erosive esophagitis (EE) and
Phase 3 EE Study:
Phase 3 NERD Study:
1. Kim DK, Lee KH, Kim SJ, et al. Effects of tegoprazan, a novel potassium-competitive acid blocker, on rat models of gastric acid-related disease. J Pharmacol Exp Ther. 2019;369(3):318-327. doi:10.1124/jpet.118.254904
2. Lee KJ, Son BK, Kim GH, et al. Randomised phase 3 trial: tegoprazan, a novel potassium-competitive acid blocker, vs. esomeprazole in patients with erosive oesophagitis. Aliment Pharmacol Ther. 2019;49(7):864-872. doi:10.1111/apt.15185
3. Oshima T, Miwa H. Potent Potassium-competitive Acid Blockers: A New Era for the Treatment of Acid-related Diseases. J Neurogastroenterol Motil. 2018 Jul 30;24(3):334-344. doi: 10.5056/jnm18029. PMID: 29739175; PMCID: PMC6034668.
4. Takahashi N, Take Y. Tegoprazan, a novel potassium-competitive acid blocker to control gastric acid secretion and motility. J Pharmacol Exp Ther. 2018;364(2):275-286. doi:10.1124/jpet.117.244202
5. Yang E, Kim S, Kim B, Kim B, Kim Y, Park SS, Song GS, Yu KS, Jang IJ, Lee S. 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. Epub 2022 Feb 23. PMID: 35146797; PMCID: PMC9305887.