exenatide (Byetta, AC2993, extendin-4, Gilly, Lizzie, Bydureon)
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Introduction
Originally isolated from the saliva of Gila monsters*
Patients may call it 'Gilly' or 'Lizzie'
Indications
- diabetes mellitus type 2
- for use in conjunction with
- somewhat improves glycemic control in an inpatient setting[22]
- may have symptomatic benefit in Parkinson's disease[20]
Contraindications
- once weekly SQ exenatide does not diminish risk of cardiovascular events[21]
- gastroparesis[23]
Dosage
- 2.5-10 ug injection SC BID
- Bydureon, once weekly long-acting form[8][15][19]
- FDA-approved Jan 2012
- once weekly Bydureon as effective as metformin in decreasing hemoglobin A1c & in weight reduction[16]
- promotes weight reduction in patients with or without diabetes mellitus[17]
Byetta pens can be kept at room temperature for 30 days
Adverse effects
- nausea/vomiting (frequent, but tends to lessen with time)[3]
- acute pancreatitis (hemorrhagic, necrotizing)[6][7]
- does not increase risk of acute pancreatis[11]
- acute renal failure (risk 1 in 13,000)[9]
Mechanism of action
- incretin mimetic
- stimulation of the glucagon-like peptide-1 receptor
- stimulation of insulin production in response to high blood glucose levels
- inhibition of the release of glucagon
- slowing the rate of gastric emptying
- appetite suppression
- preservation & formation of pancreatic beta cells
- weight loss[14]
* The Gila monster eats four times a year, & at these times, exendin-4 is released to turn the pancreas on.
Notes
- exenatide is associated with less hypoglycemia lower body weight (4.5-kg difference) than insulin glargine
- HbA1c effects are similar to insulin glargine
Estimated cost (2005) = $200/month; $323.month (2011)
More general terms
References
- ↑ Prescriber's Letter 11(7):41 2004 Exenatide (Synthetic Exendin-4) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=200705&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Journal Watch 25(12):100, 2005 DeFronzo RA, Ratner RE, Han J, Kim DD, Fineman MS, Baron AD. Effects of exenatide (exendin-4) on glycemic control and weight over 30 weeks in metformin-treated patients with type 2 diabetes. Diabetes Care. 2005 May;28(5):1092-100. PMID: https://www.ncbi.nlm.nih.gov/pubmed/15855572
Kendall DM, Riddle MC, Rosenstock J, Zhuang D, Kim DD, Fineman MS, Baron AD. Effects of exenatide (exendin-4) on glycemic control over 30 weeks in patients with type 2 diabetes treated with metformin and a sulfonylurea. Diabetes Care. 2005 May;28(5):1083-91. PMID: https://www.ncbi.nlm.nih.gov/pubmed/15855571
Buse JB, Henry RR, Han J, Kim DD, Fineman MS, Baron AD; Exenatide-113 Clinical Study Group. Effects of exenatide (exendin-4) on glycemic control over 30 weeks in sulfonylurea-treated patients with type 2 diabetes. Diabetes Care. 2004 Nov;27(11):2628-35. <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/15504997 <Internet> http://care.diabetesjournals.org/cgi/content/full/27/11/2628 - ↑ 3.0 3.1 Heine RJ, Van Gaal LF, Johns D, Mihm MJ, Widel MH, Brodows RG; GWAA Study Group. Exenatide versus insulin glargine in patients with suboptimally controlled type 2 diabetes: a randomized trial. Ann Intern Med. 2005 Oct 18;143(8):559-69. Summary for patients in: Ann Intern Med. 2005 Oct 18;143(8):I30. PMID: https://www.ncbi.nlm.nih.gov/pubmed/16230722
- ↑ Prescriber's Letter 13(5): 2006 Byetta (Exenatide) for Weight Loss Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220506&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Prescriber's Letter 14(4): 2007 Change in storage for Byetta and new insulin pens: HumaPen Memoir and HumaPen Luxura HD Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=230408&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 6.0 6.1 FDA Medwatch http://www.fda.gov/medwatch/safety/2007/safety07.htm#Byetta http://www.fda.gov/CDER/Drug/InfoSheets/HCP/exenatide2008HCP.htm
Prescriber's Letter 14(11): 2007 Pancreatitis and Byetta (Exenatide) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=231104&pb=PRL (subscription needed) http://www.prescribersletter.com - ↑ 7.0 7.1 FDA MedWatch http://www.fda.gov/medwatch/safety/2007/safety07.htm#Byetta
- ↑ 8.0 8.1 Drucker DJ et al. Exenatide once weekly versus twice daily for the treatment of type 2 diabetes: A randomised, open-label, non-inferiority study. Lancet 2008 Oct 4; 372:1240 PMID: https://www.ncbi.nlm.nih.gov/pubmed/18782641
- ↑ 9.0 9.1 FDA NEWS RELEASE, Nov. 2, 2009 Byetta Label Revised to Include Safety Information on Possible Kidney Problems http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm188708.htm
Prescriber's Letter 16(12): 2009 Byetta (Exenatide) and Altered Kidney Function Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=251203&pb=PRL (subscription needed) http://www.prescribersletter.com - ↑ Diamant M et al Once weekly exenatide compared with insulin glargine titrated to target in patients with type 2 diabetes (DURATION-3): an open-label randomised trial The Lancet 2010, 375(9733):2234-2243 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/20609969 <Internet> http://www.thelancet.com/journals/lancet/article/PIIS0140-6736(10)60406-0/fulltext
- ↑ 11.0 11.1 Garg R et al. Acute pancreatitis in type 2 diabetes treated with exenatide or sitagliptin: A retrospective observational pharmacy claims analysis. Diabetes Care 2010 Nov; 33:2349. PMID: https://www.ncbi.nlm.nih.gov/pubmed/20682680
Gonzalez-Perez A et al. Acute pancreatitis in association with type 2 diabetes and antidiabetic drugs: A population-based cohort study. Diabetes Care 2010 Dec; 33:2580. PMID: https://www.ncbi.nlm.nih.gov/pubmed/20833867 - ↑ 12.0 12.1 Buse JB et al. Use of twice-daily exenatide in basal insulin-treated patients with type 2 diabetes: A randomized, controlled trial. Ann Intern Med 2011 Jan 18; 154:103 PMID: https://www.ncbi.nlm.nih.gov/pubmed/21138825
Nathan DM. Time for clinically relevant comparative effectiveness studies in type 2 diabetes. Ann Intern Med 2011 Jan 18; 154:131 PMID: https://www.ncbi.nlm.nih.gov/pubmed/21135287 - ↑ 13.0 13.1 Prescriber's Letter 18(12): 2011 Using Exenatide (Byetta) with Insulin Glargine (Lantus) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=271204&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 14.0 14.1 Vilsbol T Effects of glucagon-like peptide-1 receptor agonists on weight loss: systematic review and meta-analyses of randomised controlled trials BMJ 2012;344:d7771 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/22236411 <Internet> http://www.bmj.com/node/557082
Padwal R Glucagon-like peptide-1 agonists BMJ 2012;344:d7282 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/22236410 <Internet> http://www.bmj.com//node/557081 - ↑ 15.0 15.1 FDA Approves BYDUREON<TM> - The First and Only Once-Weekly Treatment for Type 2 Diabetes http://phx.corporate-ir.net/phoenix.zhtml?c=101911&p=irol-newsArticle&ID=1653756
- ↑ 16.0 16.1 Russell-Jones D et al. Efficacy and safety of exenatide once weekly versus metformin, pioglitazone, and sitagliptin used as monotherapy in drug- naive patients with type 2 diabetes (DURATION-4): A 26-week double-blind study. Diabetes Care 2012 Feb; 35:252. PMID: https://www.ncbi.nlm.nih.gov/pubmed/22210563
- ↑ 17.0 17.1 Vilsboll T et al. Effects of glucagon-like peptide-1 receptor agonists on weight loss: Systematic review and meta-analyses of randomised controlled trials. BMJ 2012 Jan 11; 344:d7771. PMID: https://www.ncbi.nlm.nih.gov/pubmed/22236411
- ↑ Diamant M et al. Safety and efficacy of once-weekly exenatide compared with insulin glargine titrated to target in patients with type 2 diabetes over 84 weeks. Diabetes Care 2012 Apr; 35:683 PMID: https://www.ncbi.nlm.nih.gov/pubmed/22357185
- ↑ 19.0 19.1 Buse JB et al Exenatide once weekly versus liraglutide once daily in patients with type 2 diabetes (DURATION-6): A randomised, open-label study. Lancet 2012 Nov 7 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/23141817 <Internet> http://www.thelancet.com/journals/lancet/article/PIIS0140-6736(12)61267-7/fulltext
- ↑ 20.0 20.1 Athauda D, Maclagan K, Skene SS et al. Exenatide once weekly versus placebo in Parkinson's disease: A randomised, double-blind, placebo-controlled trial. Lancet 2017 Aug 3 PMID: https://www.ncbi.nlm.nih.gov/pubmed/28781108
- ↑ 21.0 21.1 Holman RR, Bethel MA, Mentz RJ et al Effects of Once-Weekly Exenatide on Cardiovascular Outcomes in Type 2 Diabetes. N Engl J Med. 2017 Sep 28; 377:1228. <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/28910237 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1612917
- ↑ 22.0 22.1 Fayfman M, Galindo RJ, Rubin DJ et al. A randomized controlled trial on the safety and efficacy of exenatide therapy for the inpatient management of general medicine and surgery patients with type 2 diabetes. Diabetes Care 2019 Mar; 42:450-456 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/30679302 <Internet> http://care.diabetesjournals.org/content/42/3/450
- ↑ 23.0 23.1 NEJM Knowledge+ Endocrinology