Authors : T. Rama Rao; D. Akshaya; G. Sravya; T. Kaushik

Volume/Issue : Volume 10 - 2025, Issue 2 - February

Google Scholar : https://tinyurl.com/5dajtfh4

Scribd : https://tinyurl.com/47ffxf7b

DOI : https://doi.org/10.5281/zenodo.14937088

Abstract : A frequent condition of the upper gastrointestinal system, gastro-esophageal reflux extermination causes the contents of the stomach to reflux into the esophagus. Less frequent reflux symptoms include heartburn, dysphagia, belching, hiccups, nausea, and vomiting. In order to treat and prevent acid-related conditions such as erosive esophagitis, gastric ulcer, duodenal ulcer, peptic ulcer, gastro-esophageal reflux, reflux esophagitis, and Helicobacter pylori eradication, vonoprazan, an oral bioavailable P-CAB, is being developed. 10 mg and 20 mg are among the dosages. Women who are or may become pregnant should not use vanoprazon unless the anticipated therapeutic benefit is deemed to outweigh any potential risks. Patients who as mild, moderate, or severe hepatic abnormalities as well as participants with normal hepatic function were used to assess the impact of hepatic disorders on the pharmacokinetics of vonoprazan. The new potassium-competitive acid blocker (P-CAB) vonoprazan (TAK-438) was first approved worldwide in 2014 and became available for use as an acid suppressant in 2015. Recently, there have been reports of possible drug related(PK) interactions with vonoprazan. According to reports, CYP3A primarily drives the hepatic metabolism of vonoprazan through the cytochrome P450 pathway30.

Keywords : Vanoprazan, Potassium-Competitive Acid Blocker (P-CAB), Proton Pump Inhibitors, Lasnoprazon, Pharmacokinectics (Pk), Pharmacodynamics.

References :

1. Sadafi, S., Azizi, A., Pasdar, Y. et al. Risk factors for gastroesophageal reflux disease: a population-based study. BMC Gastroenterol 24, 64 (2024). https://doi.org/10.1186/s12876-024-03143-9).
2. Garnock-Jones KP. Vonoprazan: first global approval. Drugs. 2015 Mar;75(4):439-43. doi: 10.1007/s40265-015-0368-z. PMID: 25744862. 
3. Eusebi LH, Ratnakumaran R, Yuan Y, Solaymani-Dodaran M, Bazzoli F, Ford AC. Global prevalence of, and risk factors for, gastro-oesophageal reflux symptoms: a meta-analysis. Gut. 2018 Mar;67(3):430-440. doi: 10.1136/gutjnl-2016-313589. Epub 2017 Feb 23. PMID: 28232473.
4. Tytgat GN. Shortcomings of the first-generation proton pump inhibitors. Eur J Gastroenterol Hepatol. 2001 May;13 Suppl 1:S29-33. PMID: 11430506.
5. Shin JM, Munson K, Vagin O, Sachs G. The gastric HK-ATPase: structure, function, and inhibition. Pflugers Arch. 2009 Jan;457(3):609-22. doi: 10.1007/s00424-008-0495-4. Epub 2008 Jun 6. Erratum in: Pflugers Arch. 2011 Mar;461(3):399. PMID: 18536934; PMCID: PMC3079481.
6. Shin JM, Sachs G. Long lasting inhibitors of the gastric H,K-ATPase. Expert Rev Clin Pharmacol. 2009 Sep;2(5):461-468. doi: 10.1586/ecp.09.33. PMID: 21132072; PMCID: PMC2995460.
7. Shin JM, Inatomi N, Munson K, Strugatsky D, Tokhtaeva E, Vagin O, Sachs G. Characterization of a novel potassium-competitive acid blocker of the gastric H,K-ATPase, 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine monofumarate (TAK-438). J Pharmacol Exp Ther. 2011 Nov;339(2):412-20. doi: 10.1124/jpet.111.185314. Epub 2011 Aug 9. PMID: 21828261; PMCID: PMC3199995.
8. Munson K, Law RJ, Sachs G. Analysis of the gastric H,K ATPase for ion pathways and inhibitor binding sites. Biochemistry. 2007 May 8;46(18):5398-417. doi: 10.1021/bi062305h. Epub 2007 Apr 11. PMID: 17425287; PMCID: PMC2837483.
9. Wang Y, Wang C, Wang S, Zhou Q, Dai D, Shi J, Xu X, Luo Q. Cytochrome P450-Based Drug-Drug Interactions of Vonoprazan In Vitro and In Vivo. Front Pharmacol. 2020 Feb 14;11:53. doi: 10.3389/fphar.2020.00053. PMID: 32116727; PMCID: PMC7033572.
10. Murakami K, Sakurai Y, Shiino M, Funao N, Nishimura A, Asaka M. Vonoprazan, a novel potassium-competitive acid blocker, as a component of first-line and second-line triple therapy for Helicobacter pylori eradication: a phase III, randomised, double-blind study. Gut. 2016 Sep;65(9):1439-46. Doi: 10.1136/gutjnl-2015-311304. Epub 2016 Mar 2. PMID: 26935876; PMCID: PMC5036253.
11. Miyazaki H, Igarashi A, Takeuchi T, Teng L, Uda A, Deguchi H, Higuchi K, Tango T. Vonoprazan versus proton-pump inhibitors for healing gastroesophageal reflux disease: A systematic review. J Gastroenterol Hepatol. 2019 Aug;34(8):1316-1328. Doi: 10.1111/jgh.14664.
12. Cheng, Y., Liu, J., Tan, X. et al. Direct Comparison of the Efficacy and Safety of Vonoprazan Versus Proton-Pump Inhibitors for Gastroesophageal Reflux Disease: A Systematic Review and Meta-Analysis. Dig Dis Sci 66, 19–28 (2021). https://doi.org/10.1007/s10620-020-06141-5)