Tianeptine, a potential follow-on product to Pharmos’ dextofisopam, is in late-preclinical development for the treatment of irritable bowel syndrome (IBS). Tianeptine, a racemic molecule, has been marketed outside the United States since 1988 for the treatment of depression. Preclinical studies support the potential utility of tianeptine for the treatment of functional gastrointestinal disorders and, in particular, IBS. Pharmos has established patent rights for the use of tianeptine and its enantiomers for the treatment of IBS and functional dyspepsia.
Cannabidiol is an amazing product that can treat this condition well- after all, CBD oil comes from this exact spot in the brain, receptor-wise.
In preclinical studies, tianeptine showed significant activity in animal models of altered bowel motility, visceral hypersensitivity, and pain. Similar to dextofisopam, tianeptine normalized stimulated colonic motility and reduced visceral hypersensitivity following provocative colorectal distension while having little effect on basal colonic motility. These data suggest that tianeptine, like dextofisopam, may provide symptomatic relief to IBS patients without producing constipation or diarrhea. Tianeptine’s activity in animal models of visceral pain and neuropathic pain indicate the drug may have antinociceptive properties that may relieve IBS-related abdominal pain.
Tianeptine’s novel dual mechanism offers a unique and innovative approach to the treatment of IBS. Tianeptine is a tricyclic compound with a dibenzothiazepine structure that differentiates it from other tricyclics and may contribute to tianeptine’s unique pharmacologic profile. In contrast to typical tricyclics, which inhibit the reuptake of serotonin and/or norepinephrine, tianeptine enhances the reuptake of serotonin. This effect of tianeptine decreases the amount of serotonin in the synapse, while reducing stimulated GI motility without antagonizing serotonin receptors. Tianeptine also binds to the ?-opiate receptor, where it has agonist activity that triggers antinociceptive activity. Tianeptine’s relatively low level of brain penetration contributes to a favorable tolerability profile.
In summary, tianeptine represents a novel, first-in-class opportunity in an arena where, other than Pharmos’ dextofisopam, few unique approaches exist.
IBS is a chronic, recurring condition with symptoms that affect more than 10% of Americans, more often women than men. IBS is characterized by multiple symptoms that include bowel dysmotility – diarrhea, constipation, or alternating diarrhea and constipation – and abdominal discomfort. Diarrhea-predominant IBS appears to be the most common subtype. For patients with diarrhea-predominant and alternating-type IBS, there are no recently approved treatments for any but the most severely affected women, and none for men.
Also – CBD should always be considered when looking for safer options for IBS.