Last reviewed 2026-04-23 · How we verify

TZP-101

TZP-101 is a prodrug that is converted into its active form, which is a potent inhibitor of gastric acid secretion.

TZP-101 is a prodrug that is converted into its active form, which is a potent inhibitor of gastric acid secretion. Used for Gastroesophageal reflux disease (GERD).

At a glance

Mechanism of action

TZP-101 works by inhibiting the H+/K+ ATPase enzyme in the stomach lining, leading to a decrease in gastric acid production. This mechanism is similar to that of proton pump inhibitors (PPIs), but TZP-101 is designed to be more selective and have a faster onset of action.

Approved indications

• Gastroesophageal reflux disease (GERD)

Common side effects

• Nausea
• Diarrhea
• Abdominal pain

Key clinical trials

• Study to Evaluate the Safety of Post-Operative TZP-101 (IV Ulimorelin) After Partial Bowel Resection (PHASE3)
• A Study to Assess Ulimorelin in Healthy Subjects (PHASE1)
• Efficacy, Safety, and Pharmacokinetics (PK) Study of Ulimorelin in Patients With Enteral Feeding Intolerance (EFI): The PROMOTE Trial (PHASE2)
• Safety and Efficacy of IV Infusion of Investigational Agent (TZP-101) in Patients With Severe Diabetic Gastroparesis (PHASE2)
• Safety and Efficacy of IV Infusion of TZP-101 for POI After Major Open Abdominal Surgery (PHASE2)
• Evaluation of the Pharmacokinetics of Ulimorelin in Subjects With Hepatic Impairment and Healthy Subjects (PHASE1)
• Study to Examine the Effect of Ulimorelin on the Pharmacokinetics of Midazolam in Healthy Volunteers (PHASE1)
• A Study in Healthy Male Subjects Designed to Assess the Mass Balance Recovery and Pharmacokinetics of 14C TZP-101 (PHASE1)

Primary sources

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