Ulimorelin

GI Motility / Recovery

Also known as: TZP-101, Tranzyme Ulimorelin

Ghrelin Receptor AgonistsResearch phase: Phase 3 (postoperative ileus, failed primary endpoint)Regulatory: Not approved by any regulatory agency.

Mechanism

Ulimorelin is a ghrelin receptor agonist developed to treat gastroparesis — a condition where the stomach empties too slowly. By activating the same receptor as the hunger hormone ghrelin, it stimulates stomach contractions and accelerates gastric emptying. It reached Phase 3 trials for postoperative ileus but did not gain approval.

Technical detail

Ulimorelin (TZP-101) is a macrocyclic peptidomimetic GHS-R1a agonist with prokinetic activity. Ghrelin receptor activation on gastric smooth muscle and enteric neurons enhances gastric motility via cholinergic pathways and motilin-like contractile patterns. Intravenous formulation showed acceleration of gastric emptying in Phase 2 gastroparesis trials. Phase 3 trials for postoperative ileus did not meet primary endpoints.

Evidence

A multicenter, randomized, double-blind study of ulimorelin and metoclopramide in the treatment of critically ill patients with enteral feeding intolerance: PROMOTE trial
Heyland et al. (2019) — Intensive Care Medicine — PMID: 31062046
In 120 ICU patients with enteral feeding intolerance, ulimorelin and metoclopramide achieved similar feeding success and safety outcomes over 5 days, without a clear efficacy advantage for ulimorelin.
moderate
Safety and efficacy of ulimorelin administered postoperatively to accelerate recovery of gastrointestinal motility following partial bowel resection: results of two randomized, placebo-controlled phase 3 trials
Shaw et al. (2013) — Diseases of the Colon and Rectum — PMID: 23739196
Across two placebo-controlled phase 3 trials in post-colectomy patients, intravenous ulimorelin was generally well tolerated but did not significantly reduce postoperative ileus endpoints versus placebo.
moderate

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