Unimolecular dual incretins maximize metabolic benefits in rodents, monkeys, and humans

Sci Transl Med. 2013 Oct 30;5(209):209ra151. doi: 10.1126/scitranslmed.3007218.

Abstract

We report the discovery and translational therapeutic efficacy of a peptide with potent, balanced co-agonism at both of the receptors for the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). This unimolecular dual incretin is derived from an intermixed sequence of GLP-1 and GIP, and demonstrated enhanced antihyperglycemic and insulinotropic efficacy relative to selective GLP-1 agonists. Notably, this superior efficacy translated across rodent models of obesity and diabetes, including db/db mice and ZDF rats, to primates (cynomolgus monkeys and humans). Furthermore, this co-agonist exhibited synergism in reducing fat mass in obese rodents, whereas a selective GIP agonist demonstrated negligible weight-lowering efficacy. The unimolecular dual incretins corrected two causal mechanisms of diabesity, adiposity-induced insulin resistance and pancreatic insulin deficiency, more effectively than did selective mono-agonists. The duration of action of the unimolecular dual incretins was refined through site-specific lipidation or PEGylation to support less frequent administration. These peptides provide comparable pharmacology to the native peptides and enhanced efficacy relative to similarly modified selective GLP-1 agonists. The pharmacokinetic enhancement lessened peak drug exposure and, in combination with less dependence on GLP-1-mediated pharmacology, avoided the adverse gastrointestinal effects that typify selective GLP-1-based agonists. This discovery and validation of a balanced and high-potency dual incretin agonist enables a more physiological approach to management of diseases associated with impaired glucose tolerance.

Publication types

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

MeSH terms

  • Acylation / drug effects
  • Adolescent
  • Adult
  • Aged
  • Animals
  • Diabetes Mellitus, Type 2 / drug therapy
  • Exenatide
  • Female
  • Gastric Inhibitory Polypeptide / administration & dosage
  • Gastric Inhibitory Polypeptide / pharmacology
  • Glucagon-Like Peptide 1 / administration & dosage
  • Glucagon-Like Peptide 1 / analogs & derivatives
  • Glucagon-Like Peptide 1 / pharmacology
  • Glucagon-Like Peptide-1 Receptor
  • Glucose Tolerance Test
  • Haplorhini / metabolism*
  • Humans
  • Hyperglycemia / drug therapy
  • Incretins / administration & dosage
  • Incretins / pharmacology*
  • Incretins / therapeutic use
  • Insulin / metabolism
  • Liraglutide
  • Male
  • Mice
  • Middle Aged
  • Peptides / pharmacology
  • Rats
  • Receptors, Gastrointestinal Hormone
  • Receptors, Glucagon / agonists
  • Receptors, Glucagon / metabolism
  • Rodentia / metabolism*
  • Treatment Outcome
  • Venoms / pharmacology
  • Weight Loss / drug effects
  • Young Adult

Substances

  • GLP1R protein, human
  • Glp1r protein, mouse
  • Glp1r protein, rat
  • Glucagon-Like Peptide-1 Receptor
  • Incretins
  • Insulin
  • Peptides
  • Receptors, Gastrointestinal Hormone
  • Receptors, Glucagon
  • Venoms
  • Gastric Inhibitory Polypeptide
  • Liraglutide
  • Glucagon-Like Peptide 1
  • Exenatide
  • gastric inhibitory polypeptide receptor