Once-weekly dulaglutide 1.5 mg restores insulin secretion in response to intravenous glucose infusion

Diabetes Obes Metab. 2017 Apr;19(4):517-523. doi: 10.1111/dom.12847. Epub 2017 Feb 17.

Abstract

Aims: To evaluate the effects of dulaglutide 1.5 mg on first- and second-phase insulin secretion in response to an intravenous (i.v.) glucose bolus challenge, in subjects with type 2 diabetes mellitus (T2DM; primary objective) and in healthy subjects.

Materials and methods: In this randomized, double-blind, placebo-controlled, 2-period crossover study, subjects received a single subcutaneous injection of dulaglutide 1.5 mg or placebo on day 1 of each period. On day 3, subjects underwent a 6-hour insulin infusion, followed by an i.v. glucose bolus and a glucagon challenge during hyperglycaemia. Areas under the concentration-time curve and maximum concentrations for first- (AUC0-10 and Cmax0-10 ) and second-phase secretion (AUC10-180 and Cmax10-180 ) were calculated for insulin and C-peptide. The glucose disappearance constant (Kg ) and homeostasis model assessment of β-cell function (HOMA-β) were assessed.

Results: In 20 subjects with T2DM, dulaglutide increased mean insulin AUC0-10 by 7.92-fold and Cmax0-10 by 5.40-fold vs placebo, and mean AUC10-180 and Cmax10-180 by 2.44- and 3.78- fold, respectively. In 10 healthy subjects, dulaglutide increased the mean insulin AUC0-10 by 3.09-fold and Cmax0-10 by 2.96-fold vs placebo, and mean AUC10-180 and Cmax10-180 by 2.04- and 4.15-fold, respectively. The corresponding C-peptide values also increased. Mean Kg and HOMA-β were higher after dulaglutide compared with placebo.

Conclusions: In subjects with T2DM, a single dulaglutide 1.5-mg dose restored the first-phase insulin secretion in response to an i.v. glucose bolus, increased the second-phase insulin response and enhanced β-cell function.

Keywords: dulaglutide; insulin secretion; type 2 diabetes; β-cells.

Publication types

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

MeSH terms

  • Adult
  • Area Under Curve
  • Blood Glucose / drug effects
  • C-Peptide / blood
  • Cross-Over Studies
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Diabetes Mellitus, Type 2 / physiopathology
  • Double-Blind Method
  • Drug Administration Schedule
  • Female
  • Glucagon
  • Glucagon-Like Peptides / administration & dosage
  • Glucagon-Like Peptides / analogs & derivatives*
  • Glucose / administration & dosage*
  • Humans
  • Hyperglycemia / drug therapy
  • Hypoglycemic Agents / administration & dosage*
  • Immunoglobulin Fc Fragments / administration & dosage*
  • Infusions, Intravenous
  • Injections, Subcutaneous
  • Insulin / blood*
  • Insulin-Secreting Cells / drug effects
  • Male
  • Middle Aged
  • Recombinant Fusion Proteins / administration & dosage*
  • Treatment Outcome

Substances

  • Blood Glucose
  • C-Peptide
  • Hypoglycemic Agents
  • Immunoglobulin Fc Fragments
  • Insulin
  • Recombinant Fusion Proteins
  • Glucagon-Like Peptides
  • Glucagon
  • Glucose
  • dulaglutide