Vonoprazan Explained

Tradename:Voquezna, Takecab, Vocinti
Dailymedid:Vonoprazan
Routes Of Administration:By mouth
Class:Potassium-competitive acid blocker
Atc Prefix:A02
Atc Suffix:BC08
Legal Us:Rx-only
Legal Us Comment:[1]
Legal Status:Rx-only
Bioavailability:Unknown
Protein Bound:80%
Metabolism:Liver, by cytochrome P450 (3A4, 2B6, 2C19, 2D6)
Elimination Half-Life:7.7 h
Duration Of Action:> 24 h
Excretion:Kidney
Index2 Label:as fumarate
Cas Number:881681-00-1
Cas Number2:1260141-27-2
Pubchem:15981397
Pubchem2:45375887
Drugbank:DB11739
Chemspiderid:13112797
Unii:1R5L3J156G
Unii2:4QW3X4AMLB
Kegg:D11784
Kegg2:D10466
Chebi:136048
Chembl:2079130
Chembl2:2064032
Pdb Ligand:HKT
C:17
H:16
F:1
N:3
O:2
S:1
Smiles:Fc1ccccc1-c2cc(CNC)cn2S(=O)(=O)c3cccnc3
Stdinchi:InChI=1S/C17H16FN3O2S/c1-19-10-13-9-17(15-6-2-3-7-16(15)18)21(12-13)24(22,23)14-5-4-8-20-11-14/h2-9,11-12,19H,10H2,1H3
Stdinchikey:BFDBKMOZYNOTPK-UHFFFAOYSA-N

Vonoprazan, sold under the brand name Voquezna among others, is a first-in-class potassium-competitive acid blocker medication. Vonoprazan is used in form of the fumarate for the treatment of gastroduodenal ulcer (including some drug-induced peptic ulcers) and reflux esophagitis, and can be combined with antibiotics for the eradication of Helicobacter pylori.[2] It is a potassium-competitive acid blocker.

It was approved in Japan in February 2015,[3] [4] and in Russia in April 2021.[5] Vonoprazan was approved for medical use in the United States in November 2023.[6] Co-packaged combinations of vonoprazan with amoxicillin and vonoprazan with amoxicillin and clarithromycin are available.[7] [8]

Medical uses

Vonoprazan is indicated for healing of all grades of erosive esophagitis and relief of heartburn associated with erosive esophagitis in adults; to maintain healing of all grades of erosive esophagitis and relief of heartburn associated with erosive esophagitis in adults; in combination with amoxicillin and clarithromycin for the treatment of Helicobacter pylori (H. pylori) infection in adults; in combination with amoxicillin for the treatment of H. pylori infection in adults.[9]

In July 2024, the indication was expanded in the US to include non-erosive gastroesophageal reflux disease.[10]

Society and culture

Names

Vonoprazan is the international nonproprietary name (INN).[11]

Adverse effects

The most common side effects constipation, diarrhea, enlarged feeling of abdomen, nausea, rash, and edema.

Notes and References

  1. Web site: Voquezna- vonoprazan fumarate tablet . DailyMed . 8 November 2023 . 20 November 2023.
  2. Echizen H . The First-in-Class Potassium-Competitive Acid Blocker, Vonoprazan Fumarate: Pharmacokinetic and Pharmacodynamic Considerations . Clinical Pharmacokinetics . 55 . 4 . 409–418 . April 2016 . 26369775 . 10.1007/s40262-015-0326-7. 5984975 . free .
  3. Garnock-Jones KP . Vonoprazan: first global approval . Drugs . 75 . 4 . 439–43 . 2015 . 25744862 . 10.1007/s40265-015-0368-z. 43293048 .
  4. Takecab Now Available for the Treatment of Acid-related Diseases in Japan . Takeda Pharmaceuticals . 26 February 2015 . 20 November 2023 . 26 October 2023 . https://web.archive.org/web/20231026071338/https://www.takeda.com/newsroom/newsreleases/2015/takecab-now-available-for-the-treatment-of-acid-related-diseases-in-japan/ . live .
  5. Web site: Russian State Register of Medicines. Vocinti (vonoprazan) Film-Coated Tablets. Full Prescribing Information . grls.rosminzdrav.ru . Takeda Pharmaceutical Company Limited . 18 February 2023 . Russian . 18 February 2023 . https://web.archive.org/web/20230218091924/https://grls.rosminzdrav.ru/Grls_View_v2.aspx?routingGuid=17b9e1e6-c001-4811-b9e6-9252c4dcb861 . live .
  6. 28 November 2023 . Phathom Pharmaceuticals Announces Commercial Availability of Voquezna (vonoprazan) Tablets, a Powerful First-In-Class PCAB for the Treatment of Erosive GERD and Relief of Associated Heartburn . 26 January 2024 . Phathom Pharmaceuticals . GlobeNewswire .
  7. Web site: Voquezna Dual Pak- vonoprazan fumarate and amoxicillin kit; Voquezna Triple Pak- vonoprazan fumarate, amoxicillin and clarithromycin kit . DailyMed . 21 June 2022 . 3 July 2022 . 3 July 2022 . https://web.archive.org/web/20220703054730/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=0cb2ee04-8581-46c8-a781-7be170ab5c86 . live .
  8. Phathom Pharmaceuticals Announces FDA Approval of Voquezna Triple Pak (vonoprazan, amoxicillin, clarithromycin) and Voquezna Dual Pak (vonoprazan, amoxicillin) for the Treatment of H. pylori Infection in Adults . Phathom Pharmaceuticals . GlobeNewswire . 3 May 2022 . 9 May 2022 . 10 May 2022 . https://web.archive.org/web/20220510034341/https://www.globenewswire.com/en/news-release/2022/05/03/2435147/0/en/Phathom-Pharmaceuticals-Announces-FDA-Approval-of-VOQUEZNA-TRIPLE-PAK-vonoprazan-amoxicillin-clarithromycin-and-VOQUEZNA-DUAL-PAK-vonoprazan-amoxicillin-for-the-Treatment-of-H-pylo.html . live .
  9. Web site: Drug Approval Package: Voquezna . U.S. Food and Drug Administration (FDA) . 8 June 2022 . 3 February 2024.
  10. Phathom Pharmaceuticals Announces FDA Approval of Voquezna (vonoprazan) Tablets for the Relief of Heartburn Associated with Non-Erosive GERD in Adults . Phathom Pharmaceuticals . GlobeNewswire . 18 July 2024 . 19 July 2024.
  11. ((World Health Organization)) . 2012 . International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 68 . WHO Drug Information . 26 . 3 . 10665/109813 . free . World Health Organization .