Zastaprazan

Last updated

Zastaprazan
Zastaprazan.svg
Clinical data
Trade names Jaqbo
Other namesJP-1366
Legal status
Legal status
  • Rx in South Korea
Identifiers
  • azetidin-1-yl-[8-[(2,6-dimethylphenyl)methylamino]-2,3-dimethylimidazo[1,2-a]pyridin-6-yl]methanone
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
Formula C22H26N4O
Molar mass 362.477 g·mol−1
3D model (JSmol)
  • CC1=C(C(=CC=C1)C)CNC2=CC(=CN3C2=NC(=C3C)C)C(=O)N4CCC4
  • InChI=1S/C22H26N4O/c1-14-7-5-8-15(2)19(14)12-23-20-11-18(22(27)25-9-6-10-25)13-26-17(4)16(3)24-21(20)26/h5,7-8,11,13,23H,6,9-10,12H2,1-4H3
  • Key:FEQFUBYYZYQTOJ-UHFFFAOYSA-N

Zastaprazan (trade name Jaqbo) is a pharmaceutical drug for gastrointestinal disorders. It is classified as a potassium-competitive acid blocker. [1] [2] In April 2024, it was approved for use in South Korea for the treatment of erosive gastroesophageal reflux disease (GERD). [3] In addition, it is in Phase III clinical trials for gastric ulcer and peptic ulcer. [4]

Related Research Articles

<span class="mw-page-title-main">Proton-pump inhibitor</span> Class of drugs for reducing stomach acid

Proton-pump inhibitors (PPIs) are a class of medications that cause a profound and prolonged reduction of stomach acid production. They do so by irreversibly inhibiting the stomach's H+/K+ ATPase proton pump. The body eventually synthesizes new proton pumps to replace the irreversibly inhibited ones, a process driven by normal cellular turnover, which gradually restores acid production.

<span class="mw-page-title-main">Peptic ulcer disease</span> Ulcer of an area of the gastrointestinal tract

Peptic ulcer disease is a break in the inner lining of the stomach, the first part of the small intestine, or sometimes the lower esophagus. An ulcer in the stomach is called a gastric ulcer, while one in the first part of the intestines is a duodenal ulcer. The most common symptoms of a duodenal ulcer are waking at night with upper abdominal pain, and upper abdominal pain that improves with eating. With a gastric ulcer, the pain may worsen with eating. The pain is often described as a burning or dull ache. Other symptoms include belching, vomiting, weight loss, or poor appetite. About a third of older people with peptic ulcers have no symptoms. Complications may include bleeding, perforation, and blockage of the stomach. Bleeding occurs in as many as 15% of cases.

<span class="mw-page-title-main">Gastroesophageal reflux disease</span> Flow of stomach contents into the esophagus

Gastroesophageal reflux disease (GERD) or gastro-oesophageal reflux disease (GORD) is a chronic upper gastrointestinal disease in which stomach content persistently and regularly flows up into the esophagus, resulting in symptoms and/or complications. Symptoms include dental corrosion, dysphagia, heartburn, odynophagia, regurgitation, non-cardiac chest pain, extraesophageal symptoms such as chronic cough, hoarseness, reflux-induced laryngitis, or asthma. In the long term, and when not treated, complications such as esophagitis, esophageal stricture, and Barrett's esophagus may arise.

<span class="mw-page-title-main">Esophagitis</span> Inflammation of the esophagus

Esophagitis, also spelled oesophagitis, is a disease characterized by inflammation of the esophagus. The esophagus is a tube composed of a mucosal lining, and longitudinal and circular smooth muscle fibers. It connects the pharynx to the stomach; swallowed food and liquids normally pass through it.

H<sub>2</sub> receptor antagonist Class of medications

H2 antagonists, sometimes referred to as H2RAs and also called H2 blockers, are a class of medications that block the action of histamine at the histamine H2 receptors of the parietal cells in the stomach. This decreases the production of stomach acid. H2 antagonists can be used in the treatment of dyspepsia, peptic ulcers and gastroesophageal reflux disease. They have been surpassed by proton pump inhibitors (PPIs). The PPI omeprazole was found to be more effective at both healing and alleviating symptoms of ulcers and reflux oesophagitis than the H2 blockers ranitidine and cimetidine.

<span class="mw-page-title-main">Pantoprazole</span> Stomach acid suppressing medication

Pantoprazole, sold under the brand name Protonix, among others, is a medication used for the treatment of stomach ulcers, short-term treatment of erosive esophagitis due to gastroesophageal reflux disease (GERD), maintenance of healing of erosive esophagitis, and pathological hypersecretory conditions including Zollinger–Ellison syndrome. It may also be used along with other medications to eliminate Helicobacter pylori. Pantoprazole is a proton-pump inhibitor (PPI) and its effectiveness is similar to that of other PPIs. It is available by mouth and by injection into a vein.

<span class="mw-page-title-main">Imidazopyridine</span> Class of compounds

An imidazopyridine is a nitrogen containing heterocycle that is also a class of drugs that contain this same chemical substructure. In general, they are GABAA receptor agonists, however recently proton pump inhibitors, aromatase inhibitors, NSAIDs and other classes of drugs in this class have been developed as well. Despite usually being similar to them in effect, they are not chemically related to benzodiazepines. As such, GABAA-agonizing imidazopyridines, pyrazolopyrimidines, and cyclopyrrones are sometimes grouped together and referred to as "nonbenzodiazepines." Imidazopyridines include:

<span class="mw-page-title-main">Nissen fundoplication</span> Surgical procedure to treat gastric reflux and hiatal hernia

A Nissen fundoplication, or laparoscopic Nissen fundoplication when performed via laparoscopic surgery, is a surgical procedure to treat gastroesophageal reflux disease (GERD) and hiatal hernia. In GERD, it is usually performed when medical therapy has failed; but, with a Type II (paraesophageal) hiatus hernia, it is the first-line procedure. The Nissen fundoplication is total (360°), but partial fundoplications known as Thal, Belsey, Dor, Lind, and Toupet fundoplications are alternative procedures with somewhat different indications and outcomes.

<span class="mw-page-title-main">Famotidine</span> Medication that reduces stomach acid

Famotidine, sold under the brand name Pepcid among others, is a histamine H2 receptor antagonist medication that decreases stomach acid production. It is used to treat peptic ulcer disease, gastroesophageal reflux disease, and Zollinger-Ellison syndrome. It is taken by mouth or by injection into a vein. It begins working within an hour.

<span class="mw-page-title-main">Esomeprazole</span> Medication which reduces stomach acid

Esomeprazole, sold under the brand name Nexium [or Neksium] among others, is a medication which reduces stomach acid. It is used to treat gastroesophageal reflux disease, peptic ulcer disease, and Zollinger–Ellison syndrome. Its effectiveness is similar to that of other proton pump inhibitors (PPIs). It is taken by mouth or injection into a vein.

<span class="mw-page-title-main">Achlorhydria</span> Lack of hydrochloric acid production in the digestive organs

Achlorhydria and hypochlorhydria refer to states where the production of hydrochloric acid in gastric secretions of the stomach and other digestive organs is absent or low, respectively. It is associated with various other medical problems.

<span class="mw-page-title-main">Nizatidine</span> Chemical compound

Nizatidine is a histamine H2 receptor antagonist that inhibits stomach acid production, and is commonly used in the treatment of peptic ulcer disease and gastroesophageal reflux disease.

<span class="mw-page-title-main">Sucralfate</span> Chemical compound and gastrointestinal medication

Sucralfate, sold under various brand names, is a medication used to treat stomach ulcers, gastroesophageal reflux disease (GERD), radiation proctitis, and stomach inflammation and to prevent stress ulcers. Its usefulness in people infected by H. pylori is limited. It is used by mouth and rectally.

<span class="mw-page-title-main">Lesogaberan</span> Chemical compound

Lesogaberan (AZD-3355) was an experimental drug candidate developed by AstraZeneca for the treatment of gastroesophageal reflux disease (GERD). As a GABAB receptor agonist, it has the same mechanism of action as baclofen, but is anticipated to have fewer of the central nervous system side effects that limit the clinical use of baclofen for the treatment of GERD.

There are several classes of drugs for acid-related disorders, such as dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD), or laryngopharyngeal reflux.

<span class="mw-page-title-main">Vonoprazan</span> Pharmaceutical compound

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 and reflux esophagitis, and can be combined with antibiotics for the eradication of Helicobacter pylori.

<span class="mw-page-title-main">Azeloprazole</span> Chemical compound

Azeloprazole is a drug under investigation for acid-related medical conditions responsive to suppressing the production of stomach acid. It is considered a member of the proton pump inhibitor class of medications.

<span class="mw-page-title-main">Acid peptic diseases</span> Overview of the acid peptic diseases of the stomach and gastrointestinal tract

Acid peptic diseases, such as peptic ulcers, Zollinger-Ellison syndrome, and gastroesophageal reflux disease, are caused by distinct but overlapping pathogenic mechanisms involving acid effects on mucosal defense. Acid reflux damages the esophageal mucosa and may also cause laryngeal tissue injury, leading to the development of pulmonary symptoms.

<span class="mw-page-title-main">Linaprazan</span> Pharmaceutical molecule

Linaprazan is an experimental drug for the treatment of gastroesophageal reflux disease (GERD). Unlike the proton-pump inhibitors (PPIs) which are typically used to treat GERD, linaprazan is a potassium-competitive acid blocker (P-CAB). Linaprazan was developed by AstraZeneca, but it was not successful in clinical trials.

<span class="mw-page-title-main">Fexuprazan</span> Chemical compound

Fexuprazan is a drug for the treatment of gastroesophageal reflux disease (GERD). It is a potassium-competitive acid blocker.

References

  1. Yang E, Hwang I, Ji SC, Kim J, Lee S (December 2024). "Population pharmacokinetic analysis of zastaprazan (JP-1366), a novel potassium-competitive acid blocker, in patients and healthy volunteers". CPT. 13 (12): 2150–2158. doi:10.1002/psp4.13228. PMC   11646930 . PMID   39268835.
  2. Tietto A, Faggin S, Scarpignato C, Savarino EV, Giron MC (September 2024). "Safety of potassium-competitive acid blockers in the treatment of gastroesophageal reflux disease". Expert Opinion on Drug Metabolism & Toxicology: 1–16. doi:10.1080/17425255.2024.2397433. PMID   39189409.
  3. Blair HA (July 2024). "Zastaprazan: First Approval". Drugs. 84 (7): 863–866. doi:10.1007/s40265-024-02057-w. PMID   38916840.
  4. "Zastaprazan". AdisInsight. Springer Nature Switzerland AG.