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

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

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Amylin Pharmaceuticals Inc., 9373 Towne Centre Drive, San Diego, CA 92121, USA.


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.

[Indexed for MEDLINE]

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