Tenapanor for the treatment of irritable bowel syndrome with constipation

ABSTRACT

Introduction

Irritable bowel syndrome with constipation is associated with higher rates of functional impairment, as compared to other subtypes of the syndrome. Conventional laxative-based pharmacologic therapy of IBS-C, which is mostly symptom-based, is often unsatisfactory.

Tenapanor represents a first-in-class orally available inhibitor of NHE3, which is minimally absorbed in the GI tract, what constitutes a significant therapeutic benefit, as it may act on the drug target.

Areas covered

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 on tenapanor’s safety and efficacy in view of its important potential role in IBS-C treatment.

Expert opinion

In the challenging setting of irritable bowel syndrome with constipation, tenapanor represents a novel strategy in the pipeline of the therapies of IBS-C. Its pharmacokinetic and pharmacodynamic profile provides that it is minimally absorbed from the intestinal lumen and that its action is local, but not systemic action, therefore guaranteeing the reduction of drug–drug interactions, toxicity and severe adverse effects. Phase 2b and 3 trials showed an optimal satisfaction of primary and secondary endpoints.

KEYWORDS:

• Irritable bowel syndrome
• constipation
• tenapanor
• efficacy
• safety

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership, or options, expert testimony, grants, or patents received or pending, or royalties.

Reviewer declarations

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This paper was not funded.