Contribution of protein binding to the pharmacokinetics of the ghrelin receptor agonist TZP-101 in healthy volunteers and adults with symptomatic gastroparesis: two randomized, double-blind studies and a binding profile study.

Background And Objective: TZP-101 is a selective, small molecule ghrelin receptor agonist in clinical development for the treatment of gastric motility disorders. The objectives of this study was to assess pharmacokinetic parameters of TZP-101 after multiple- and single-dose administration to healthy subjects and patients with gastroparesis, respectively, and to determine the contribution of protein binding to its pharmacokinetic behaviour.

Methods: Pharmacokinetics following 30-minute intravenous infusions of single (160-600 microg/kg) doses of TZP-101 in patients with gastroparesis and multiple (80-600 mug/kg/day) doses of TZP-101 in healthy subjects were characterized.