Visceral Antinociceptive Effects of RDX5791, a First-in-Class Minimally Systemic NHE3 Inhibitor on Stress-Induced Colorectal Hypersensitivity to Distension in Rats

@article{Eutamene2011VisceralAE,
  title={Visceral Antinociceptive Effects of RDX5791, a First-in-Class Minimally Systemic NHE3 Inhibitor on Stress-Induced Colorectal Hypersensitivity to Distension in Rats},
  author={Helene Eutamene and Dominique Campbell Charmot and Marc Navre and Lionel Bu{\'e}no},
  journal={Gastroenterology},
  year={2011},
  volume={140}
}
Tenapanor: new approach to counter irritable bowel syndrome with constipation
TLDR
Tenanapor a novel molecule acts locally on gastrointestinal sodium/hydrogen exchanger isoform 3 (NHE3), an antiporter a counter transporter and exert antinociceptive effects on visceral sensation thereby decreases the frequency of abdominal pain.
Plecanatide for the treatment of constipation-predominant irritable bowel syndrome
  • P. Miner
  • Medicine
    Expert review of gastroenterology & hepatology
  • 2020
TLDR
All clinical trial results supporting approval of plecanatide in IBS-C are reported, evaluated and interpreted in the context of the complex pathophysiology of functional diseases and the barriers that must be overcome for appropriate protocol design and conduct.
Tenapanor for the treatment of irritable bowel syndrome with constipation
TLDR
Aim of this article is to sum up the evidences about pharmacodynamics and pharmacokinetics of tenapanor, focusing on animal models and in vitro studies, but also discuss clinical trials onTenapanor’s safety and efficacy in view of its important potential role in IBS-C treatment.
Effect of Food Intake on the Pharmacodynamics of Tenapanor: A Phase 1 Study
TLDR
The data suggest the effect of tenapanor on sodium absorption is most pronounced when administered before meals, whereas the effect on phosphate is similar whether administered before or after meals, which may support different timings ofTenapanor administration with respect to food for sodium‐ and phosphate‐related indications.
New therapeutic perspectives in irritable bowel syndrome: Targeting low-grade inflammation, immuno-neuroendocrine axis, motility, secretion and beyond
TLDR
This literature review aims to summarize the findings related to new and investigational therapeutic agents for IBS, most recently developed in preclinical as well as Phase 1 and Phase 2 clinical studies.
Tenapanor Treatment of Patients With Constipation-Predominant Irritable Bowel Syndrome: A Phase 2, Randomized, Placebo-Controlled Efficacy and Safety Trial
TLDR
Tenapanor 50 mg b.i.d. significantly increased stool frequency and reduced abdominal symptoms in patients with IBS-C, and further research into tenapanor as a potential treatment for these patients is justified.
A phase 1 study of the safety, tolerability, pharmacodynamics, and pharmacokinetics of tenapanor in healthy Japanese volunteers
TLDR
Tenapanor treatment reduced absorption of intestinal sodium and phosphate from the gut in Japanese adults and had minimal systemic exposure and was well tolerated.
Early investigational therapeutics for gastrointestinal motility disorders: from animal studies to Phase II trials
TLDR
Treatment of gastrointestinal motility disorders requires the understanding of the pathophysiological mechanisms, biomarkers to identify subgroups of these disorders and robust pharmacological studies from animal to Phase II studies, which are prerequisites for the development of efficacious medications and individualizing therapy.
Tenapanor hydrochloride for the treatment of constipation-predominant irritable bowel syndrome
TLDR
The non-systemic action of tenapanor constitutes a significant advantage, as it minimizes possible adverse effects or drug–drug interactions, whereas limiting diarrhea, its major adverse effect.
...
1
2
...