Pharmacology of exenatide (synthetic exendin-4) for the treatment of type 2 diabetes

Curr Opin Investig Drugs. 2003 Apr;4(4):401-5.


New therapies for the long-term treatment of type 2 diabetes are needed to ameliorate declining pancreatic beta-cell function. Ideally, these therapies should lower fasting and post-prandial blood glucose, produce no hypoglycemia or weight gain, cause no other limiting side effects, and reduce cardiovascular complications. Exenatide (synthetic exendin-4) is a potential therapeutic which may fulfill these criteria. Dose-ranging studies have identified an optimal dose of 0.05 to 0.2 microgram/kg administered subcutaneously twice daily. Pharmacokinetic data support a pivotal study design which mitigates the transient nausea observed in early studies by including a dose initiation period of 1 month at 5 micrograms twice daily, followed by maintenance therapy at 10 micrograms twice daily. Ongoing studies suggest exenatide improves glycemic control through a combination of mechanisms discussed in this review.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blood Glucose / metabolism
  • Clinical Trials, Phase I as Topic
  • Clinical Trials, Phase II as Topic
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Exenatide
  • Glycated Hemoglobin A / metabolism
  • Homeostasis / drug effects
  • Humans
  • Hypoglycemic Agents / adverse effects
  • Hypoglycemic Agents / pharmacology*
  • Hypoglycemic Agents / therapeutic use*
  • Peptides / adverse effects
  • Peptides / pharmacology
  • Peptides / therapeutic use
  • Recombinant Proteins / pharmacology
  • Recombinant Proteins / therapeutic use
  • Venoms*


  • Blood Glucose
  • Glycated Hemoglobin A
  • Hypoglycemic Agents
  • Peptides
  • Recombinant Proteins
  • Venoms
  • Exenatide