Pharmacokinetics and Pharmacodynamic Effects of Oral GLP-1 and PYY3-36: A Proof-of-concept Study in Healthy Subjects

This proof‐of‐concept study was performed in order to establish the pharmacokinetics and pharmacodynamics of increasing oral doses of the satiety peptides glucagon‐like peptide‐1 (GLP‐1) and peptide YY3‐36 (PYY3‐36). Six healthy male subjects were given oral doses of either a placebo or GLP‐1 in a d...

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Bibliographic Details
Published in:Clinical pharmacology and therapeutics 2008-10, Vol.84 (4), p.468-474
Main Authors: Beglinger, C, Poller, B, Arbit, E, Ganzoni, C, Gass, S, Gomez‐Orellana, I, Drewe, J
Format: Article
Language:English
Subjects:
Administration, Oral
Adult
Area Under Curve
Biological and medical sciences
Dose-Response Relationship, Drug
Feasibility Studies
Ghrelin - blood
Ghrelin - metabolism
Glucagon-Like Peptide 1 - administration & dosage
Glucagon-Like Peptide 1 - adverse effects
Glucagon-Like Peptide 1 - pharmacokinetics
Humans
Insulin - blood
Insulin - metabolism
Insulin Secretion
Male
Medical sciences
Peptide Fragments
Peptide YY - administration & dosage
Peptide YY - adverse effects
Peptide YY - pharmacokinetics
Pharmacology. Drug treatments
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Summary:This proof‐of‐concept study was performed in order to establish the pharmacokinetics and pharmacodynamics of increasing oral doses of the satiety peptides glucagon‐like peptide‐1 (GLP‐1) and peptide YY3‐36 (PYY3‐36). Six healthy male subjects were given oral doses of either a placebo or GLP‐1 in a dose‐escalating schedule (doses of 0.5, 1.0, 2.0, and 4.0 mg). Next, another group of six healthy male subjects were given oral doses of either a placebo or PYY3‐36 in the same pattern of escalating doses (doses of 0.25, 0.5, 1.0, 2.0, and 4.0 mg). In healthy male volunteers, (i) oral administration of either of the peptides induced a rapid and dose‐dependent increase in plasma drug concentrations; (ii) oral administration of GLP‐1 induced a potent effect on insulin release; and (iii) both peptides suppressed ghrelin secretion. In conclusion, this study showed, for the first time, that satiety peptides such as GLP‐1 and PYY3‐36 can be orally delivered safely and effectively in humans. Clinical Pharmacology & Therapeutics (2008); 84, 4, 468–474 doi:10.1038/clpt.2008.35
ISSN:0009-9236
1532-6535
DOI:10.1038/clpt.2008.35