exenatide

• Brand name in US: Byetta
• Class: incretin mimetic.
• For: type 2 diabetes
• Route of Administration: Fixed dose, subcutaneous injection given prior to the morning and evening meals.
• Available as: 5-microgram per dose and 10-microgram per dose prefilled pen-injector devices
• Action: lowers blood sugar
• Side effects: nausea, hypoglycemia when used with sulfonylureas.
• manufacturer: Amylin Pharmaceuticals, Inc.
• Status: Approved by FDA, April 2005; to be available to pharmacies by June 1, 2005.
• Source of Information: press release from Amylin (reproduced below).
• Additional information: Exenatide is a synthetic version of a natural compound found in the saliva of the Gila monster lizard.

SAN DIEGO, Calif. and INDIANAPOLIS, Ind., April 29 /PRNewswire-FirstCall/ -- Amylin Pharmaceuticals, Inc. (Nasdaq: AMLN), and Eli Lilly and Company (NYSE: LLY) announce that the U.S. Food and Drug Administration (FDA) has approved BYETTA(TM) (exenatide) injection as adjunctive therapy to improve blood sugar control in patients with type 2 diabetes who have not achieved adequate control on metformin and/or a sulfonylurea, two common oral diabetes medications. BYETTA (pronounced bye-A-tuh), the trade name for exenatide, is the first in a new class of medicines known as incretin mimetics. BYETTA will be available to pharmacies by June 1, 2005.

BYETTA improves blood sugar control by lowering both postmeal and fasting glucose levels leading to better long-term control as measured by hemoglobin A1C. BYETTA does this through several actions, including the stimulation of insulin secretion only when blood sugar is high and by restoring the first- phase insulin response, an activity of the insulin-producing cells in the pancreas that is lost in patients who have type 2 diabetes. Most patients in the long-term BYETTA clinical studies also experienced reductions in weight.

"The availability of a treatment that lowers blood sugar and has the potential to help restore the response of the body's insulin-producing cells is an exciting advance for patients with type 2 diabetes," said Dr. David Kendall, Medical Director at International Diabetes Center in Minneapolis, Minnesota, and an investigator for the BYETTA clinical studies. "BYETTA is a truly unique tool for the management of type 2 diabetes and is an appropriate option to consider when patients cannot control their blood sugar using one or more oral medications."

"Successfully managing diabetes is a daily struggle for millions of Americans," said Ginger L. Graham, President and Chief Executive Officer, Amylin Pharmaceuticals, Inc. "Often, current treatments do not provide adequate blood sugar control leaving patients and caregivers frustrated. BYETTA, a first-in-class medicine, is a new therapy for those who are not able to effectively control their blood sugar with their current oral medications."

"BYETTA offers an exciting new option for people with type 2 diabetes and marks an important milestone for Amylin and Lilly's successful collaboration," said Sidney Taurel, Chairman and Chief Executive Officer, Eli Lilly and Company. "With BYETTA's demonstrated effects on blood sugar and its safety profile, physicians and patients now have a new approach to fight the growing diabetes epidemic."

In addition to approving BYETTA for use as an adjunct to existing oral medicines, the FDA also stated that BYETTA is approvable as a stand-alone therapy (monotherapy) for patients with type 2 diabetes. Any additional data submitted to support a monotherapy indication is expected to receive a six- month review.

BYETTA is formulated for self-administration as a fixed dose, subcutaneous injection given prior to the morning and evening meals. BYETTA will be made available in both a 5-microgram per dose and a 10-microgram per dose prefilled pen-injector device.

Safety and Tolerability Information

In the three 30-week controlled trials, adverse events associated with BYETTA were generally mild to moderate in intensity. The most frequently reported adverse event was mild-to-moderate, dose-dependent nausea. With continued therapy in most patients who initially experienced nausea, the frequency and severity decreased over time.

Patients receiving BYETTA in combination with a sulfonylurea have an increased risk of hypoglycemia; to reduce this risk, reduction in the dose of the sulfonylurea should be considered. In the 30-week controlled clinical trials, hypoglycemia appeared to be dependent on the doses of both BYETTA and a sulfonylurea. Most episodes of hypoglycemia were mild to moderate in intensity and all were resolved with oral administration of carbohydrate. No increased risk of hypoglycemia was observed in the 30-week controlled studies with BYETTA when used in combination with metformin compared to placebo.

Patients should also be advised that treatment with BYETTA may result in a reduction in appetite, food intake, and/or body weight and that there is no need to modify the dosing regimen due to such effects.

BYETTA should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis, nor is BYETTA a substitute for insulin in insulin-requiring patients. Use of BYETTA is not recommended in patients with end-stage renal disease or severe renal impairment, or in patients with severe gastrointestinal disease. BYETTA should be used with caution in patients receiving oral medications that require rapid gastrointestinal absorption.

For full Prescribing Information, visit www.BYETTA.com.

About BYETTA

BYETTA is the first in a new class of drugs for the treatment of type 2 diabetes called incretin mimetics and exhibits many of the same effects as the human incretin hormone glucagon-like peptide-1 (GLP-1). GLP-1, secreted in response to food intake, has multiple effects on the stomach, liver, pancreas and brain that work in concert to regulate blood sugar.(1) BYETTA was approved by the FDA for use by people with type 2 diabetes who are unsuccessful at controlling their blood sugar levels despite using the commonly prescribed oral medications metformin, a sulfonylurea or both. For full Prescribing Information, visit www.BYETTA.com .

About Incretin Mimetics

Incretin mimetics is a new class of therapeutics for use in the fight against type 2 diabetes. An incretin mimetic works to mimic the antidiabetic or glucose-lowering actions of naturally occurring human hormones called incretins. These actions include stimulating the body's ability to produce insulin in response to elevated levels of blood sugar, inhibiting the release of a hormone called glucagon following meals, slowing the rate at which nutrients are absorbed into the bloodstream and reducing food intake. BYETTA is the first FDA-approved agent of this new class of medications.

SOURCE Amylin Pharmaceuticals, Inc.; Eli Lilly and Company

Jamaison Schuler of Lilly, +1-317-655-2111; or Eric Shearin of Amylin,
+1-858-552-2200, ext. 7177