Drug intelligence / Profile preview

dextofisopam

Development stage
Phase 2
Lead developer
Pharmos
Modality
Small Molecules
Administration
Oral
01

Overview

Dextofisopam is the R-enantiomer of racemic tofisopam and is a small molecule drug investigated primarily for the treatment of irritable bowel syndrome (IBS), particularly diarrhea-predominant and alternating types. It represents a novel, first-in-class non-serotonergic agent that binds to specific receptors in the brain affecting autonomic and gastrointestinal function. Unlike existing IBS therapies targeting 5-HT3 or 5-HT4 receptors, dextofisopam acts at a distinct site known as the 2,3-benzodiazepine receptor—different from classical benzodiazepine sites—and does not significantly bind other receptors or ion channels. Its mechanism may involve modulation of central nervous system activity related to stress and visceral sensitivity. Dextofisopam has shown positive proof-of-concept results in clinical trials for IBS with an improved safety profile compared to serotonergic agents[1][2][4].

Other names
dextofisopam (USAN/INN)
02

Targets

GABRR (GABA-A receptor subunit rho)PDE10A (Phosphodiesterase 10A)PDE3PDE2 (Phosphodiesterase 2)PDE4A

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