Potent Potassium-competitive Acid Blockers: A New Era for the Treatment of Acid-related Diseases
Tadayuki Oshima,Hiroto Miwa +1 more
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TL;DR: Vonoprazan was recently innovated as a novel, orally active P-CAB, which does not require an acidic environment for activation, has long-term stability at the site of action, and has satisfactory safety and tolerability and may address the unmet medical need for the treatment of acid-related diseases.
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Abstract: Conventional proton pump inhibitors (PPIs) are used as a first-line therapy to treat acid-related diseases worldwide. However, they have a number of limitations including slow onset of action, influence by cytochrome P450 polymorphisms, unsatisfactory effects at night, and instability in acidic conditions. Alternative formulations of conventional PPIs have been developed to overcome these problems; however, these drugs have only introduced small advantages for controlling acid secretion compared to conventional PPIs. Potassium-competitive acid blockers (P-CABs) were developed and have beneficial effects including rapid, long-lasting, and reversible inhibition of the gastric hydrogen potassium ATPase, the proton pump of the stomach. Vonoprazan was recently innovated as a novel, orally active P-CAB. It is currently indicated for the treatment of gastric and duodenal ulcers, reflux esophagitis, and prevention of low-dose aspirin- or nonsteroidal anti-inflammatory drug-related gastric and duodenal ulcer recurrence in Japan. Vonoprazan does not require enteric coating as it is acid-stable, and it can be taken without food because it is quickly absorbed. Vonoprazan accumulates in parietal cells under both acidic and neutral conditions. It does not require an acidic environment for activation, has long-term stability at the site of action, and has satisfactory safety and tolerability. Thus, vonoprazan may address the unmet medical need for the treatment of acid-related diseases.
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Citations
Phase III, randomised, double-blind, multicentre study to evaluate the efficacy and safety of vonoprazan compared with lansoprazole in Asian patients with erosive oesophagitis
Yinglian Xiao,Shutian Zhang,Ning Dai,Guijun Fei,Khean-Lee Goh,Hoon Jai Chun,Bor Shyang Sheu,Chui Fung Chong,Nobuo Funao,Wen Zhou,Minhu Chen +10 more
TL;DR: The findings demonstrate the non-inferior efficacy of vonoprazan versus lansoprazole in terms of EO healing rate at 8 weeks in this population of Asian patients with erosive oesophagitis.
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Systematic review with meta-analysis: Vonoprazan, a potent acid blocker, is superior to proton-pump inhibitors for eradication of clarithromycin-resistant strains of Helicobacter pylori.
Min Li,Tadayuki Oshima,Tomoki Horikawa,Katsuyuki Tozawa,Toshihiko Tomita,Hirokazu Fukui,Jiro Watari,Hiroto Miwa +7 more
TL;DR: The ability of vonoprazan to eradicate clarithromycin‐susceptible and clarithroitcin‐resistant H. pylori strains is summarized in this meta‐analysis.
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2020 Seoul Consensus on the Diagnosis and Management of Gastroesophageal Reflux Disease.
Hye Kyung Jung,Chung Hyun Tae,Kyung Ho Song,Seung Joo Kang,Jong Kyu Park,Eun Jeong Gong,Jeong Eun Shin,Hyun Chul Lim,Sang Kil Lee,Da Hyun Jung,Yoon Jin Choi,Seung In Seo,Joon Sung Kim,Jung Min Lee,Beom Jin Kim,Sun Hyung Kang,Chan Hyuk Park,Suck Chei Choi,Joong Goo Kwon,Kyung Sik Park,Moo In Park,Tae Hee Lee,Seung Young Kim,Young Sin Cho,Han Hong Lee,Kee Wook Jung,Do Hoon Kim,Hee Seok Moon,Hirota Miwa,Chien-Lin Chen,Sutep Gonlachanvit,Uday C Ghoshal,Justin C.Y. Wu,Kewin Tien Ho Siah,Xiaohua Hou,Tadayuki Oshima,Miyoung Choi,Kwang Jae Lee +37 more
TL;DR: Based on a meta-analysis of 19 estimated acid-exposure time values in Asians, the reference range upper limit for esophageal acid exposure time was 3.2% (95% confidence interval, 2.7-3.9%) in the Asian countries.
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Randomised clinical trial: vonoprazan versus lansoprazole for the initial relief of heartburn in patients with erosive oesophagitis.
Tadayuki Oshima,Eitatsu Arai,Masato Taki,Takashi Kondo,Toshihiko Tomita,Hirokazu Fukui,Jiro Watari,Hiroto Miwa +7 more
TL;DR: A new potassium‐competitive acid blocker (P‐CAB) can rapidly block acid secretion and whether this P-CAB can relieve GORD symptoms quickly and adequately soon after starting treatment is unknown.
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Night‐time gastric acid suppression by tegoprazan compared to vonoprazan or esomeprazole
Eunsol Yang,Seokuee Kim,Bongtae Kim,Boram Kim,Yechan Kim,Sung Sup Park,Geun Seog Song,Kyung Sang Yu,In-Jin Jang,Seung Hwan Lee +9 more
TL;DR: This study aimed to compare night‐time acid suppression by tegoprazan with that by vonopazan or esomeprazole, and to explore the effect of CYP2C19 phenotypes on acid‐suppressive effects.
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