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Showing 1 - 10 of 38 results

Vonoprazan (Vonoprazan fumarate or TAK-438) under brand name Takecab, discovered by Takeda, is a new medicine for treating acid-related diseases with a novel mechanism of action called potassium-competitive acid blockers (P-CABs) which competitively inhibits the binding of potassium ions to H+,K+-ATPase (also known as the proton pump) in the final step of gastric acid secretion in gastric parietal cells. The drug is approved in Japan for the treatment of acid-related diseases, including gastric ulcer, duodenal ulcer, reflux esophagitis and Adjunct to Helicobacter pylori eradication in the case of Helicobacter pylori gastritis.
Pantoprazole is a proton pump inhibitor that inhibits gastric acid secretion and used for short-term treatment of erosive esophagitis associated with gastroesophageal reflux disease. Pantoprazole suppresses the final step in gastric acid production by covalently binding to the (H+, K+)-ATPase enzyme system at the secretory surface of the gastric parietal cell. This effect leads to inhibition of both basal and stimulated gastric acid secretion, irrespective of the stimulus. The binding to the (H+, K+)-ATPase results in a duration of antisecretory effect that persists longer than 24 hours. Pantoprazole is used for short-term treatment of erosion and ulceration of the esophagus for adults and pediatric patients 5 years of age and older caused by gastroesophageal reflux disease. It can be used as a maintenance therapy for long-term use after initial response is obtained, but there have not been any controlled studies about the use of pantoprazole past a duration of 12 months. Pantoprazole may also be used in combination with antibiotics to treat ulcers caused by Helicobacter pylori. Use of pantoprazole may increase the chance of developing infections such as pneumonia, particularly in hospitalized patients.
Rabeprazole was discovered by Eisai Co., Ltd. Janssen Pharmaceutica N.V. and Eisai Co., Ltd. have a strategic alliance in which Eisai and Janssen-Cilag co-promote the drug in Germany and the U.K. In the US rabeprazole sodium is co-promoted under the brand name AcipHex by Eisai Inc. and Janssen Pharmaceutica Inc. Pariet is available through Janssen-Cilag in most other countries excluding Japan and some Asian countries. Rabeprazole is an antiulcer drug in the class of proton pump inhibitors. Rabeprazole is a prodrug and is converted to the active sulphenamide form in the acid environment of the parietal cells. Rabeprazole is used to heal and maintain the healing of Erosive or Ulcerative Gastroesophageal Reflux Disease (GERD), for healing Duodenal Ulcers, and for treatment of pathological hypersecretory conditions such as Zollinger-Ellison Syndrome. Rabeprazole suppresses gastric acid secretion by inhibiting the gastric H , K ATPase at the secretory surface of the gastric parietal cell and does not exhibit anticholinergic or histamine H2-receptor antagonist properties. Because this enzyme is regarded as the acid (proton) pump within the parietal cell, rabeprazole has been characterized as a gastric proton-pump inhibitor which blocks the final step of gastric acid secretion. In gastric parietal cells, rabeprazole is protonated, accumulates, and is transformed to an active sulfonamide.
Dexlansoprazole (trade names Kapidex, Dexilant) is a proton pump inhibitor (PPI) that is marketed by Takeda Pharmaceuticals for the treatment of erosive esophagitis and gastro-oesophageal reflux disease. Dexlansoprazole is used to heal and maintain healing of erosive esophagitis and to treat heartburn associated with gastroesophageal reflux disease (GERD). It lasts longer than lansoprazole, to which it is chemically related, and needs to be taken less often. Dexlansoprazole is supplied for oral administration as a dual delayed-release formulation in capsules and orally disintegrating tablets. The capsules and tablets contain dexlansoprazole in a mixture of two types of enteric-coated granules with different pH-dependent dissolution profiles. The most significant adverse reactions (≥2%) reported in clinical trials were diarrhea, abdominal pain, nausea, upper respiratory tract infection, vomiting, and flatulence.
Esomeprazole strontium is a proton pump inhibitor. It suppresses gastric acid secretion by specific inhibition H+/K+ ATPase in the gastric parietal cell. The S- and R-isomers of omeprazole are protonated and converted in the acidic compartment of the parietal cell forming the active inhibitor, the achiral sulphenamide. By acting specifically on the proton pump, esomeprazole blocks the final step in acid production, thus reducing gastric acidity. The drug is indicated for the treatment of gastroesophageal reflux disease, reduction the risk of NSAID-associated gastric ulcer, eradication of H.pylori, and pathological hypersecretory conditions.
Status:
Investigational
Source:
NCT00206284: Phase 2 Interventional Completed GERD Without Erosive Esophagitis
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Linaprazan is a member of a new group of acid-suppressing agents, which unlike proton pump inhibitors, act through potassium-competitive inhibition of the H+,K+-ATPase located in the apical membrane of parietal cells. It displayed rapid inhibition of acid production and had a prolonged, dose-dependent duration of effect. Linaprazan reduced porcine renal Na(+),K(+)-ATPase activity by 9+/-2%, demonstrating a high selectivity for H(+),K(+)-ATPase. It provided similar efficacy to esomeprazole in terms of esophagitis healing and heartburn control.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



PF-03716556 is a novel, potent, and selective acid pump antagonist for the treatment of gastroesophageal reflux disease. PF-03716556 inhibits the porcine, canine, and human recombinant gastric H+,K+-ATPase in a competitive manner without any biologically relevant activity against other tested receptors, ion channels, and enzymes, including the Na+,K+-ATPase. PF-03716556 inhibits gastric acid secretion in a dose-dependent manner in Ghosh-Schild rats and Heidenhain pouch dogs, producing full efficacy on treatment day 1. PF-03716556 is used for the treatment of gastroesophageal reflux disease.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

SCH-28080 is an inhibitor of H+, K+-ATPase. Administration of SCH-28080 led to significant reduction in the volume, acid output and peptic activity of gastric secretions in a clinical trial.
Status:
Possibly Marketed Outside US
Source:
SENNA
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Sennoside B is a member of the class of sennosides that used as the laxative. Sennosides are used all over the world as a treatment for constipation. Sennosides are hydroxyanthracene glycosides derived from Senna leaves. The phytoconstituents principally responsible for its characteristic action are two anthraquinone glycosides namely; Sennoside A and Sennoside B. Sennoside A and B together are responsible for up to 40 – 60% activity of crude senna. They have identical molecular weights and formulae and are in fact diastereomers with the same substituent (H) located in opposite directions. Sennoside B has reported that it has inhibitory effects on PDGF receptor signaling and cell proliferation induced by PDGF-BB in human osteosarcoma cells.