RDX5791, a First-in-Class Minimally Systemic NHE3 Inhibitor in Clinical Development for CIC and IBS-C, Increases Intestinal Sodium Leading to Enhanced Intestinal Fluid Volume and Transit

Spencer, Andrew; Jacobs, J. W.; Leadbetter, Michael R.; Carreras, Christopher W.; Du, Xunxiang; Bell, Noah; Koo-McCoy, Samantha; Kohler, Jill; Labonté, Eric D.; Rosenbaum, David P.; Navre, Marc; Charmot, Dominique

doi:10.1016/s0016-5085(11)60405-8

Cited by 14 publications

(13 citation statements)

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“…Of note, the compound did not change urinary or fecal potassium content. Finally, the effect of tenapanor was similar in mouse, rabbit, dog and cynomolgus monkey [21].…”

Section: Pharmacodynamicsmentioning

confidence: 75%

“…In the mouse model of morphine-induced constipation, tenapanor (10 mg/kg per os) improved average intestinal transit (99.0 ± 0.7 vs 74.0 ± 5.2% for vehicle-treated group) [21].…”

Section: Pharmacodynamicsmentioning

confidence: 92%

“…Lubiprostone is an activator of type-2 chloride channel in the intestine (releasing chloride and water into the intestine). Pivotal trial(s) [21,23,24] M. Zieliń ska et al…”

Section: Overview Of the Marketmentioning

confidence: 99%

“…For example, experiments in rats showed 92.2 ± 1.6% recovery of tenapanor in feces upon oral administration [21]. In humans, the inactive metabolites of tenapanor were found in plasma, but they were only about 9% of the parent compound.…”

Section: Pharmacokinetics and Metabolismmentioning

confidence: 99%

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Tenapanor hydrochloride for the treatment of constipation-predominant irritable bowel syndrome

Zielińska

Wasilewski

Fichna

2015

Expert Opinion on Investigational Drugs

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Tenapanor possesses an excellent preclinical safety profile and, as of now, there are no serious concerns about its side effects. The non-systemic action of tenapanor constitutes a significant advantage, as it minimizes possible adverse effects or drug-drug interactions. However, Phase III clinical trials are still needed to confirm results obtained in earlier phases and optimize the dose-response for tenapanor, whereas limiting diarrhea, its major adverse effect.

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“…Of note, the compound did not change urinary or fecal potassium content. Finally, the effect of tenapanor was similar in mouse, rabbit, dog and cynomolgus monkey [21].…”

Section: Pharmacodynamicsmentioning

confidence: 75%

“…In the mouse model of morphine-induced constipation, tenapanor (10 mg/kg per os) improved average intestinal transit (99.0 ± 0.7 vs 74.0 ± 5.2% for vehicle-treated group) [21].…”

Section: Pharmacodynamicsmentioning

confidence: 92%

“…Lubiprostone is an activator of type-2 chloride channel in the intestine (releasing chloride and water into the intestine). Pivotal trial(s) [21,23,24] M. Zieliń ska et al…”

Section: Overview Of the Marketmentioning

confidence: 99%

Section: Pharmacokinetics and Metabolismmentioning

confidence: 99%

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Tenapanor hydrochloride for the treatment of constipation-predominant irritable bowel syndrome

Zielińska

Wasilewski

Fichna

2015

Expert Opinion on Investigational Drugs

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“…This would theoretically allow for more gradual hydration of stool, and less of a tendency for diarrhea as the dose is increased. The effects of RDX5791 on stool consistency and transit time have been demonstrated in animal models (Spencer et al, 2011). RDX5791 has been demonstrated to be anti-nocioceptive in an animal model of visceral hypersensitivity (Eutamene et al, 2011).…”

Section: Rdx-5791mentioning

confidence: 99%

Core Aspects of Clinical Development and Trials in Chronic Idiopathic Constipation

Harris¹,

Daniëls²

2012

Constipation - Causes, Diagnosis and Treatment

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Trastornos funcionales y motores digestivos

Mearin

Rey

Balboa

2011

Gastroenterología y Hepatología

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As in previous years, a huge number of studies were presented at the Congress of the American Gastroenterology Association (Digestive Diseases Week [DDW]), some of which were better than others. The present article attempts to extract and summarize the most interesting findings reported. In general terms, certain technological advances have been consolidated, with full incorporation into clinical practice, such as impedancemetry and high-resolution manometry. New physiopathological data are coming to light that increasingly indicate the inextricable link between organic and psychological factors (the biopsychosocial model) in functional gastrointestinal disorders (FGID). Despite the high hopes that the Rome III criteria would improve the diagnosis of FGID and especially that of functional dyspepsia, their practical application has been fairly discouraging. Moreover, at least two studies have demonstrated that these criteria cannot be used to differentiate subtypes of functional dyspepsia and that there is wide overlap with gastroesophageal reflux disease. New data were presented on the role of genetic, microinflammatory and psychological factors in the etiopathogenesis of the two main FGID: functional dyspepsia and irritable bowel syndrome (IBS). The results on the safety and efficacy of acotiamide in functional dyspepsia and of linaclotide and prucalopride in idiopathic and IBS-associated constipation were also presented. Several studies, and even meta-analyses, have demonstrated the utility of biofeedback in the treatment of constipation. Even so, the efficacy of this therapy has been questioned due to certain methodological deficiencies in some studies. In DDW 2011, studies confirming the utility of biofeedback, whether hospital- or home-based were presented, in dyssynergy constipation. The present article also mentions certain features of special interest in the diagnosis and treatment of rumination syndrome, thoracic pain of possible esophageal origin and cannabinoid-induced hyperemesis syndrome.

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RDX5791, a First-in-Class Minimally Systemic NHE3 Inhibitor in Clinical Development for CIC and IBS-C, Increases Intestinal Sodium Leading to Enhanced Intestinal Fluid Volume and Transit

Cited by 14 publications

References 0 publications

Tenapanor hydrochloride for the treatment of constipation-predominant irritable bowel syndrome

Tenapanor hydrochloride for the treatment of constipation-predominant irritable bowel syndrome

Core Aspects of Clinical Development and Trials in Chronic Idiopathic Constipation

Trastornos funcionales y motores digestivos

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