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TD-2749 is a selective serotonin 4 (5-HT4) receptor agonist developed by Theravance (now Innoviva) as an oral, small molecule prokinetic agent for the treatment of gastrointestinal motility disorders. It was designed using multivalent drug design to improve selectivity and efficacy for GI conditions such as chronic constipation, constipation-predominant irritable bowel syndrome (C-IBS), opioid-induced constipation, functional dyspepsia, and diabetic gastroparesis. The compound demonstrated high affinity and functional potency at the 5-HT4 receptor with selectivity over the 5-HT3 receptor in preclinical studies. Despite entering Phase 1 clinical trials for GI disorders, development was discontinued before reaching later stages[1][2][3][7][9].
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