欧盟正式批准了2mg规格的 Bydureon（exenatide，艾塞那肽缓释注射混悬剂）与一定的口服药物联用于治疗2型糖尿病。该药设计为提高机体胰岛素的产生，Bydureon每周使用一次。
Bydureon的作用包括轻到中度的恶心、呕吐、腹泻、便秘。Bydureon在美国还未获得批准，公司计划将于2011年末向美国FDA递交相关补充资料。Bydureon每周一次分别与二甲双胍、一种磺酰脲类、一种噻唑烷二酮药联用，或是与二甲双胍+一种磺酰脲类或二甲双胍+一种噻唑烷二酮药联用。
BYDUREON
Manufacturer:
Amylin and Alkermes
Pharmacological Class:
Antidiabetic (glucagon-like peptide-1 [GLP-1] receptor agonist).
Active Ingredient(s):
Exenatide extended-release 2mg; pwd for SC inj after reconstitution.
Indication(s):
As adjunct to diet and exercise, to improve glycemic control in adults with type 2 diabetes. Not for first-line therapy in patients inadequately controlled on diet and exercise.
Pharmacology:
Bydureon is an extended-release formulation of exenatide, a GLP-1 receptor agonist. Exenatide has been shown to bind and activate the human GLP-1 receptor in vitro. This leads to an increase in both glucose-dependent synthesis of insulin and in vivo secretion of insulin from pancreatic beta cells, by mechanisms involving cyclic AMP and/or other intracellular signaling pathways. Exenatide also moderates glucagon secretion and lowers glucagon concentrations during periods of hyperglycemia, slows gastric emptying, and decreases food intake.
Clinical Trials:
A 24-week, randomized, open-label trial was conducted to compare the safety and efficacy of Bydureon to Byetta in patients with type 2 diabetes and inadequate glycemic control with diet and exercise alone or with oral antidiabetic therapy, including metformin, a sulfonylurea, a thiazolidinedione, or combination of two of those therapies.
A total of 252 patients were studied. Patients were treated with diet and exercise alone (19%), a single oral antidiabetic agent (47%), or combination therapy of oral antidiabetic agents (35%). The mean baseline HbA1c was 8.4%. Patients were randomly assigned to receive Bydureon 2mg once every seven days (weekly) or Byetta (10mcg twice-daily), in addition to existing oral anti-diabetic agents. Patients assigned to Byetta initiated treatment with 5mcg twice-daily then increased the dose to 10mcg twice-daily after 4 weeks.
The primary endpoint was change in HbA1c from baseline to Week 24 (or the last value at time of early discontinuation). After 24 weeks of treatment, patients taking Bydureon experienced a statistically superior reduction in HbA1c of 1.6 percentage points from baseline, compared to a reduction of 0.9 percentage points for patients taking Byetta. Both treatment groups achieved statistically significant weight loss by the end of the study, with an average loss of 2.3kg for Bydureon patients and 1.4kg for Byetta patients (weight loss was a secondary endpoint).
Legal Classification:
Rx
Adults:
Give by SC inj in abdomen, thigh, or upper arm. Inject immediately after mixing. 2mg once every 7 days (weekly). Changing from Byetta: discontinue, then start Bydureon.
Children:
Not recommended.
Contraindication(s):
History (personal or family) of medullary thyroid carcinoma. Multiple endocrine neoplasia syndrome type 2.
Warnings/Precautions:
Not a substitute for insulin. Not for treating type 1 diabetes or diabetic ketoacidosis. Risk of thyroid C-cell tumors possible. History of pancreatitis; consider other antidiabetics. Monitor for pancreatitis; if suspected, promptly discontinue; if confirmed, do not restart. Severe GI disorders, renal impairment (CrCl <30mL/min), end-stage renal disease: not recommended. Renal transplantation. Pregnancy (Cat.C). Nursing mothers.
Interaction(s):
Concurrent insulin: not recommended. Increased risk of hypoglycemia with concomitant sulfonylurea, insulin, or other insulin secretagogues (eg, meglitinides); consider reducing dose of these. May delay absorption of oral drugs. Monitor warfarin.
Adverse Reaction(s):
GI upset, constipation, headache, inj site reactions; possible antibody formation (glycemic response may be attenuated), pancreatitis (may be fatal), hypersensitivity reactions.
How Supplied:
Single-dose trays—4 (each contains 1 vial, 1 prefilled syringe with diluent, vial connector and needles)
Last Updated:
2/24/2012
