"目录号: HY-15295
Membrane Transporter/Ion Channel-
TAK-438是钾竞争性的酸阻滞剂，能可逆的抑制H_addition_/K_addition_-ATPase，IC50为19 nM(pH 6.5)。
相关产品
Omeprazole-Pantoprazole sodium-(R)-Lansoprazole-Zinc Pyrithione-AZD0865-Ilaprazole-Esomeprazole Magnesium trihydrate-TAK-438 free base-Bamaquimast-Rabeprazole sodium-Soraprazan-Chebulinic acid-Picoprazole-SKF96067-Tenatoprazole sodium-
生物活性
Description
TAK-438 is a novel P-CAB (potassium-competitive acid blocker) that reversibly inhibits H+/K+, ATPase with IC50 of 19 nM (pH 6.5), controls gastric acid secretion.IC50 value: 19 nM [1]Target: H+/K+ATPasein vitro: TAK-438 is a pyrrole derivative with a chemical structure that is completely different from the P-CABs developed to date. TAK-438 inhibits gastric H+, K+-ATPase activity in a concentration-dependent manner. Under neutral conditions (pH 7.5), the inhibitory activity of TAK-438 is almost the same as that under weakly acidic conditions (pH 6.5). TAK-438 does not inhibit Na+, K+-ATPase activity even at concentration 500 times higher than their IC50 values against gastric H+,K+-ATPase activity. TAK-438 inhibits gastric H+, K+-ATPase in a K+-competitive manner with Ki of 3 nM [2]. in vivo: TAK-438 inhibits basal gastric acid secretion in a dose-dependent manner, and the ID50 value is 1.26 mg/kg . Intravenous administration of TAK-438 dose-dependently increases the pH of the gastric perfusate, and the increase in pH is sustained for 5 h after administration. At the 1 mg/kg dose, the pH plateaues 90 min after administration, and the highest pH value reached is 5.9 [2]. In addition, TAK-438 shows a potent and longer-lasting inhibitory effect on the histamine-stimulated gastric acid secretion in rats and dogs. TAK-438 shows significant antisecretory activity through high accumulation and slow clearance from the gastric tissue. TAK-438 is unaffected by the gastric secretory state, unlike PPIs [3].
Clinical Trial
Takeda
Erosive Esophagitis(EE)-Gastroesophageal Reflux Disease (GERD)
October 2008
Phase 1
Takeda
Healthy Volunteers
August 2010
Phase 1
Takeda
Healthy Participants
April 25, 2017
Phase 1
Takeda
Erosive Esophagitis
September 2011
Phase 3
Takeda
Dose Finding Study
October 2008
Phase 1
Takeda
Ascending Single Dose Study
September 2007
Phase 1
Takeda
Non-erosive Gastroesophageal Reflux Disease
December 1, 2016
Phase 3
Takeda
Erosive Esophagitis
October 2011
Phase 3
Takeda-Richmond Pharmacology Limited
Dose Finding Study
October 2007
Phase 1
Takeda
Helicobacter Pylori
September 21, 2016
Phase 1
Takeda
Non-erosive Gastroesophageal Reflux Disease
December 2011
Phase 3
Takeda
H. Pylori Infection
January 2012
Phase 3
Takeda
Erosive Esophagitis
Phase 3
Takeda
Gastric Ulcer
November 2011
Phase 3
Takeda
Gastric Ulcer-Peptic Ulcer-Gastrointestinal Diseases-Digestive System Diseases-Lansoprazole-Anti-Ulcer Agents-Gastrointestinal Agents-Proton Pump Inhibitors-Enzyme Inhibitors-Molecular Mechanisms of Pharmacological Action
April 17, 2017
Phase 3
Takeda
Duodenal Ulcer
April 4, 2017
Phase 3
Takeda
Duodenal Ulcer
October 2011
Phase 3
Takeda
Gastric Ulcer-Duodenal Ulcer
May 2012
Phase 3
Takeda
Gastric Ulcer-Duodenal Ulcer
April 2012
Phase 3
Takeda
Gastric Ulcers-Duodenal Ulcers
October 2011
Phase 3
Takeda
Gastric Ulcers-Duodenal Ulcers
March 2012
Phase 3
Takeda
Gastric Ulcers-Duodenal Ulcers
October 2011
Phase 3
Takeda
Gastric Ulcers-Duodenal Ulcers
September 2011
Phase 3
Takeda
Erosive Esophagitis
July 2012
Phase 3
Takeda
Reflux Esophagitis
April 21, 2017
Phase 4
Takeda
Erosive Esophagitis
March 29, 2016
Phase 4
Takeda
Gastroesophageal Reflux
July 14, 2016
Phase 2
Takeda
A History of Gastric or Duodenal Ulcers
September 1, 2016
Takeda
Gastric or Duodenal Ulcers
September 1, 2016
Takeda
Gastric Ulcer, Duodenal Ulcer, and Reflux Esophagitis
March 1, 2016
Takeda
Reflux Esophagitis
March 1, 2016
Hamamatsu University
Gastritis Associated With Helicobacter Pylori
July 2016
Phase 3
Takeda
Erosive Esophagitis
March 16, 2015
Phase 3
Takeda
Erosive Esophagitis
April 2015
Phase 3
Takeda
Healthy Volunteers
January 2014
Phase 3
Takeda
Gastric/Duodenal Ulcer, Gastric MALT Lymphoma, Idiopathic Thrombocytopenic Purpura, or H. Pylori Gastritis, and Other
September 1, 2015
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References
