GSK2374697, a long duration glucagon-like peptide-1 (GLP-1) receptor agonist, reduces postprandial circulating endogenous total GLP-1 and peptide YY in healthy subjects

Diabetes Obes Metab. 2015 Oct;17(10):1007-10. doi: 10.1111/dom.12533. Epub 2015 Aug 11.

Abstract

We investigated the effects of a long-duration glucagon-like peptide-1 (GLP-1) receptor agonist, GSK2374697, on postprandial endogenous total GLP-1 and peptide YY (PYY). Two cohorts of healthy subjects, one normal/overweight and one obese, were randomized to receive GSK2374697 2 mg (n = 8 each) or placebo (n = 4 and n = 2) subcutaneously on days 1, 4 and 7. Samples for plasma endogenous GLP-1 and PYY were collected after breakfast on days -1 and 12. Weighted mean area under the curve (0-4 h) of total GLP-1 and PYY in treated subjects was reduced compared with placebo. The least squares mean difference for change from baseline was -1.24 pmol/l [95% confidence interval (CI) -2.33, -0.16] and -4.47 pmol/l (95% CI -8.74, -0.20) for total GLP-1 and PYY, respectively, in normal/overweight subjects (p < 0.05 for both), and -1.56 (95% CI -2.95, -0.16) and -3.02 (95% CI -8.58, 2.55), respectively, in obese subjects (p < 0.05 for GLP-1). In healthy subjects, GSK2374697 reduced postprandial total GLP-1 and PYY levels, suggesting feedback suppression of enteroendocrine L-cell secretion of these peptides.

Trial registration: ClinicalTrials.gov NCT01545570.

Keywords: AlbudAb; GLP-1; GSK2374697; PYY; long-duration GLP-1 agonist.

Publication types

  • Letter
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Breakfast
  • Female
  • Glucagon-Like Peptide 1 / blood
  • Glucagon-Like Peptide 1 / drug effects*
  • Healthy Volunteers
  • Humans
  • Male
  • Middle Aged
  • Peptide YY / blood
  • Peptide YY / drug effects*
  • Postprandial Period / drug effects*
  • Recombinant Fusion Proteins / pharmacology*
  • Young Adult

Substances

  • GSK2374697
  • Recombinant Fusion Proteins
  • Peptide YY
  • Glucagon-Like Peptide 1

Associated data

  • ClinicalTrials.gov/NCT01545570