Potassium-competitive acid blockers - are they the next generation of proton pump inhibitors?

Rawla, Prashanth; Sunkara, Tagore; Ofosu, Andrew; Gaduputi, Vinaya

doi:10.4292/wjgpt.v9.i7.63

Cited by 40 publications

(46 citation statements)

References 26 publications

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“…Increasing PPI dosage does not increase the eradication rate of PPI-based regimens [ 15 , 16 , 17 ]. Vonoprazan and tegoprazan are new potential gastric acid suppression agents, classified as potassium-competitive acid blockers (P-CAB), that function by H + /K + -ATPase inhibition [ 18 , 19 ] ( Figure 1 ). Japanese guidelines on the management of H. pylori infections recommend replacing PPI with vonoprazan in first-line and second-line H. pylori eradication therapies since first introduced in 2015, while tegoprazan has been established as treatment for gastroesophageal reflux disease (GERD) in South Korea since 2018 [ 20 , 21 ].…”

Section: Introductionmentioning

confidence: 99%

The Potential Benefits of Vonoprazan as Helicobacter pylori Infection Therapy

2020

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Helicobacter pylori infection is a severe global health problem that is closely associated with acid-related diseases and gastric malignancies. Eradicating H. pylori is strongly recommended for lowering peptic ulcer recurrence and preventing gastric cancer. The current approved H. pylori eradication regimen combines a proton pump inhibitor (PPI) with two antibiotics. Unfortunately, this regimen failed to meet expectations mostly due to antibiotic resistance and insufficient gastric acid suppression. Vonoprazan, a novel potassium-competitive acid blocker, showed promising results as a PPI replacement. Vonoprazan inhibits gastric acid secretion by acting as a reversible competitive inhibitor against potassium ions and forming disulfide bonds with the cysteine molecule of H+/K+-ATPase. Vonoprazan has superior pharmacological characteristics over PPI, such as no requirement for acid activation, stability in acidic conditions, shorter optimum acid suppression period, and resistance to cytochrome P (CYP)2C19 polymorphism. Several comparative randomized controlled trials and meta-analyses revealed the superiority of vonoprazan in eradicating H. pylori, notably the resistant strains. The adverse effect caused by vonoprazan is long-term acid suppression that may induce elevated gastrin serum, hypochlorhydria, and malabsorption. All vonoprazan studies have only been conducted in Japan. Further studies outside Japan are necessary for universally conclusive results.

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Section: Introductionmentioning

confidence: 99%

The Potential Benefits of Vonoprazan as Helicobacter pylori Infection Therapy

2020

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“…11,12 Despite these advantages, it is also true that there are some concerns for hepatotoxicity from P-CABs. 13,14 Now, revaprazan (Yuhan Corp.), vonoprazan (Takeda Pharmaceutical Co., Ltd.) and tegoprazan (HK inno.N Corp.) are the commercially available P-CABs.…”

Section: Introductionmentioning

confidence: 99%

Pharmacodynamics of tegoprazan and revaprazan after single and multiple oral doses in healthy subjects

Sunwoo

et al. 2020

Aliment Pharmacol Ther

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SummaryBackgroundPotassium‐competitive acid blockers (P‐CABs) are emerging as novel treatments for acid‐related disorders including gastroesophageal reflux disease. Tegoprazan and revaprazan are approved P‐CABs in South Korea, but the pharmacodynamics and safety/tolerability of the two drugs have never been compared.AimsTo evaluate the pharmacodynamics and safety/tolerability of tegoprazan and revaprazan after single and multiple oral dosesMethodsA randomised, open‐label, active‐controlled study was conducted in Helicobacter pylori‐negative healthy Korean male subjects. Tegoprazan 50 mg or revaprazan 200 mg was administered orally, once daily for 7 days; 24‐h intragastric pH monitoring and serum gastrin were measured for pharmacodynamic evaluation. Safety parameters including serum microRNA‐122 (miR‐122) level were also collected.ResultsAfter a single dose, the %Time pH ≥4 for tegoprazan was greater than that for revaprazan (54.5% vs 25.1%). After multiple doses, the %Time pH ≥4 for tegoprazan was also greater than that for revaprazan (68.2% vs 25.3%). %Time pH ≥4 during 12 hours at nighttime for tegoprazan was greater than that for revaprazan (71.8% vs 31.9%). The changes in the serum gastrin were not clinically significant for either drug. Despite the slight increases of serum miR‐122 for each drug, tegoprazan and revaprazan were well tolerated considering other safety parameters including AST and ALT levels.ConclusionTegoprazan 50 mg showed stronger gastric acid suppression than revaorazan 200 mg. Both drugs were well tolerated.

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“…However, postoperative bleeding remains one of the most common adverse events that can cause severe consequences . Recently, a newly developed acid‐suppressing drug, vonoprazan, has shown potential efficacy for the treatment of acid‐related diseases . As a member of novel potassium‐competitive acid blockers, vonoprazan inhibits gastric acid secretion reversibly by hindering K + from binding to gastric H + /K + ‐ATPase .…”

Section: Introductionmentioning

confidence: 99%

“…6 Recently, a newly developed acid-suppressing drug, vonoprazan, has shown potential efficacy for the treatment of acid-related diseases. 7,8 As a member of novel potassium-competitive acid blockers, vonoprazan inhibits gastric acid secretion reversibly by hindering K + from binding to gastric H + /K + -ATPase. 9 Compared with PPIs, vonoprazan provides a more rapid acid-inhibitory effect that sustains for a longer time duration 10 together with a mean elimination half-life of up to 9 h, which is much longer than that of a typical 1 to 2 hours of PPIs.…”

mentioning

confidence: 99%

The efficacy of vonoprazan for management of post‐endoscopic submucosal dissection ulcers compared with proton pump inhibitors: A meta‐analysis

Liu

Feng

Zhang

et al. 2019

J of Digest Diseases

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Objective Artificial ulcers after endoscopic submucosal dissection (ESD) are usually treated by proton pump inhibitors (PPIs) in clinical setting. Vonoprazan, a newly developed potassium‐competitive acid blocker, has recently been used to treat post‐ESD ulcers. We aimed to evaluate the efficacy and safety of vonoprazan on the healing of post‐ESD artificial ulcers compared with those of proton pump inhibitors (PPIs) using a meta‐analysis. Methods EMBASE, MEDLINE, Scopus and Cochrane Library databases were searched for all studies comparing the efficacy and safety of vonoprazan with those of PPIs in the treatment of post‐ESD ulcers. Results Fourteen articles with 1328 patients were included in this meta‐analysis. When comparing ulcer shrinkage rate, vonoprazan showed a better efficacy than PPIs (mean difference 0.56, 95% confidence interval [CI] 0.18‐0.93). Vonoprazan also led to a higher scar formation rate (odds ratio [OR] 1.58, 95% CI 1.00‐2.47) and showed a potential superiority on reducing the risk of post‐ESD bleeding compared with PPIs, with a pooled OR of 0.69, although there was no statistically significant difference. Conclusions Compared with PPIs, vonoprazan showed a better efficacy in ulcer shrinkage rate and achieved more complete healing in the treatment of post‐ESD ulcers. Vonoprazan did not induce any incremental risk of post‐ESD bleeding as well. It may be an appropriate choice in the management of artificial ulcers after ESD.

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Potassium-competitive acid blockers - are they the next generation of proton pump inhibitors?

Cited by 40 publications

References 26 publications

The Potential Benefits of Vonoprazan as Helicobacter pylori Infection Therapy

The Potential Benefits of Vonoprazan as Helicobacter pylori Infection Therapy

Pharmacodynamics of tegoprazan and revaprazan after single and multiple oral doses in healthy subjects

The efficacy of vonoprazan for management of post‐endoscopic submucosal dissection ulcers compared with proton pump inhibitors: A meta‐analysis

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