Novel approaches to the pharmacological blockade of gastric acid secretion

Expert Opin Investig Drugs. 2005 Apr;14(4):411-21. doi: 10.1517/13543784.14.4.411.

Abstract

Research into new methods of controlling acid secretion is driven by existing medical needs in gastro-oesophageal reflux disease treatment. Histamine receptor subtype 3 agonists offer one approach for acid inhibition but no agent is yet undergoing clinical testing. Other, as yet unrealized strategies include preventing the fusion of the tubulovesicular elements that contain H+/K+-ATPase with the parietal cell membrane, or blocking channels that recycle K+ in the parietal cell. Of more promise are gastrin (cholecystokinin) receptor antagonists and potassium-competitive acid blockers; examples of both are in clinical development. It is probable that gastrin receptor antagonists would be used adjunctively with proton pump inhibitors, possibly for meal-induced reflux. The potassium-competitive acid blockers have attributes that may facilitate use as monotherapy for the treatment of gastro-oesophageal reflux disease. The early promise of gastrin receptor antagonists and potassium-competitive acid blockers remains to be defined in large-scale trials.

Publication types

  • Review

MeSH terms

  • Animals
  • Clinical Trials as Topic
  • Gastric Acid / metabolism*
  • Gastric Mucosa / drug effects*
  • Gastric Mucosa / metabolism
  • Gastroesophageal Reflux / drug therapy*
  • Gastroesophageal Reflux / metabolism
  • Gastrointestinal Agents / pharmacology*
  • Gastrointestinal Agents / therapeutic use
  • H(+)-K(+)-Exchanging ATPase / metabolism
  • Histamine Agonists / pharmacology
  • Histamine Agonists / therapeutic use
  • Humans
  • Parietal Cells, Gastric / drug effects
  • Parietal Cells, Gastric / metabolism
  • Potassium Channel Blockers / pharmacology
  • Potassium Channel Blockers / therapeutic use
  • Proton Pump Inhibitors
  • Proton Pumps / metabolism
  • Receptor, Cholecystokinin B / antagonists & inhibitors
  • Receptor, Cholecystokinin B / metabolism
  • Receptors, Histamine H3 / drug effects
  • Receptors, Histamine H3 / metabolism

Substances

  • Gastrointestinal Agents
  • Histamine Agonists
  • Potassium Channel Blockers
  • Proton Pump Inhibitors
  • Proton Pumps
  • Receptor, Cholecystokinin B
  • Receptors, Histamine H3
  • H(+)-K(+)-Exchanging ATPase