Introduction of Vonoprazan FuMarate

Vonoprazan fumarate, a potassium-competitive acid blocker(P-CAB), produces a stronger acid-inhibitory effect than proton pump inhibitors (PPIs). Vonoprazan fumarate are agents that inhibit H+, K+ -adenosine triphosphatase (ATPase) through reversible K+competitive ionic binding that results in the inhibition of gastric acid secretion. Because vonoprazan has a relatively high pKa value and is stable in an acidic environment, it can accumulate in the acidic compartment of gastric parietal cells, unlike PPIs. In addition, vonoprazan does not require acid activation, in contrast to PPIs. Thus, vonoprazan can achieve stronger, longer-lasting suppression of gastric acid secretion than PPIs can.

Vonoprazan FuMarate for the treatment of Peptic Ulcer Disease(PUD)

Proton-Pump Inhibitors (PPIs) represented the mainstay for the treatment of gastroesophageal reflux disease (GERD), peptic ulcer disease (PUD), low-dose aspirin or non-steroidal anti-inflammatory drug-induced peptic ulcer and Helicobacter pylori (H. pylori) infection.

A randomized trial confirmed the non-inferiority of vonoprazan compared to lansoprazole in the treatment of gastric ulcer (93.5% and 93.8%, respectively), even if there was a possible bias due to the fact that drop-out subjects were put in the non-healed group. Other studies with vonoprazan (at the dose of both 10 and 20mg) showed similar results to PPIs in patients taking long-term NSAIDs, in the absence of severe adverse effects. Therefore, vonoprazan at the dose of 10mg has been approved for this indication^[1].

Vonoprazan FuMarate for the treatment of Helicobacter pylori Infection

H. pylori can infect the gastric mucosa and cause gastritis. Chronic inflammation caused by H. pylori can lead to a variety of diseases such as atrophic gastritis, gastroduodenal ulcer, mucosa-associated lymphoid tissue (MALT) lymphoma, gastric adenocarcinoma, and even idiopathic thrombocytopenic purpura. Therefore, these diseases can be prevented or treated by eradicating H. pylori.

The H. pylori eradication rate with vonoprazan was found to be higher than that with PPIs. The H. pylori eradication rate with vonoprazan-based triple therapy (vonoprazan, amoxicillin, and clarithromycin) was approximately 90% and had an incidence of adverse events similar to that of PPIs^[2-3].

References:

[1] MARABOTTOELISA. Vonoprazan Fumarate for the Treatment of Gastric Ulcers: A Short Review on Emerging Data.[J]. Clinical and Experimental Gastroenterology, 2020, 13: 99-104. DOI:10.2147/CEG.S228352.

[2] MIFTAHUSSURURMUHAMMAD; YamaokaYoshio; Pratama PutraBoby. The Potential Benefits of Vonoprazan as Helicobacter pylori Infection Therapy.[J]. Pharmaceuticals, 2020. DOI:10.3390/ph13100276.

[3] KIYOTOKISHU SakaidaIsao NishikawaJun. Efficacy of Vonoprazan for Helicobacter pylori Eradication.[J]. Internal Medicine, 2020, 59 2: 153-161. DOI:10.2169/internalmedicine.2521-18.