Pharmacokinetics and pharmacodynamic effects of an oral ghrelin agonist in healthy subjects.

Academic Article


  • CONTEXT: An oral formulation of EP01572, a peptidomimetic growth hormone secretagogue, was studied. An oral delivery system would be preferable in many of the possible therapeutic indications of ghrelin agonists such as EP01572. OBJECTIVES: Our objective was to establish the pharmacological profile and the GH-releasing activity of increasing oral doses of EP01572 in healthy volunteers. In addition, the pharmacokinetics and pharmacological effects of EP01572 were investigated after intraduodenal (ID) administration. SETTING: This study was a single-center escalating dose study with oral and ID applications. SUBJECTS AND METHODS: In the first part, EP01572 was given orally to 36 male subjects; the treatment consisted of one oral dose of either EP01572 or placebo (0.005, 0.05, and 0.5 mg/kg body weight). Six subjects received two additional oral doses of EP01572: 0.125 and 0.25 mg/kg body weight. In the second part, the following treatments were performed in a randomized order: 1) administration of a bolus of saline (placebo) to the small intestine; 2) ID administration of a bolus of EP01572 at 0.2 mg/kg body weight; 3) ID perfusion of a bolus of EP01572 at 0.35 mg/kg body weight; and 4) ID perfusion of a bolus of EP01572 at 0.5 mg/kg body weight. RESULTS: The oral and ID administration of EP01572 induced a rapid and dose-dependent increase in plasma drug concentrations and a potent GH release in healthy male volunteers. CONCLUSIONS: This study showed that EP01572 was active with regard to stimulation of GH release in humans after oral and ID administration.
  • Authors


  • Administration, Oral, Adult, Area Under Curve, Dose-Response Relationship, Drug, Duodenum, Ghrelin, Growth Hormone-Releasing Hormone, Half-Life, Hormones, Human Growth Hormone, Humans, Indoles, Intubation, Gastrointestinal, Male, Oligopeptides, Peptide Hormones, Tryptophan
  • Digital Object Identifier (doi)

    Author List

  • Piccoli F; Degen L; MacLean C; Peter S; Baselgia L; Larsen F; Beglinger C; Drewe J
  • Start Page

  • 1814
  • End Page

  • 1820
  • Volume

  • 92
  • Issue

  • 5