Glucagon-like peptide-1 receptor agonist
Glucagon-like peptide-1 receptor agonists also known as GLP-1 receptor agonists or incretin mimetics are agonists of the GLP-1 receptor. This class of drugs is used for the treatment of type 2 diabetes.[1] [2] One of their advantages over older insulin secretagogues, such as sulfonylureas or meglitinides, is that they have a lower risk of causing hypoglycemia.[3]
There is some concern over the safety profile of these drugs due to proliferative effects in the pancreas. At the same time, diabetes is associated with both acute pancreatitis and pancreatic cancer, and the most recent studies have not found that these drugs can cause either pancreatitis or cancer.[4]
Approved GLP-1 agonists:
- exenatide (Byetta/Bydureon), approved in 2005/2012
- liraglutide (Victoza, Saxenda), approved 2010[5]
- lixisenatide (Lyxumia), approved in EU 2013[6]
- albiglutide (Tanzeum), approved in 2014 by GSK[7]
- dulaglutide (Trulicity), approved in 2014—manufactured by Eli Lilly[8]
Under investigation: [1]
- taspoglutide, phase III halted Sept 2010,
- semaglutide, oral, 160 hr half-life.[9]
These agents work in the same pathway as DPP-4 inhibitors but are generally considered more potent.[10]
References
- 1 2 Baggio LL (2008). "Glucagon-like Peptide-1 Analogs Other Than Exenatide". Medscape Diabetes & Endocrinology.
- ↑ Ali ES, Hua J, Wilson CH, Tallis GA, Zhou FH, Rychkov GY, Barritt GJ (2016). "The glucagon-like peptide-1 analogue exendin-4 reverses impaired intracellular Ca2+ signalling in steatotic hepatocytes". BBA-Molecular Cell Research. 1863 (9): 2135–46. doi:10.1016/j.bbamcr.2016.05.006. PMID 27178543.
- ↑ "Standards of medical care in diabetes—2012". Diabetes Care. 35 Suppl 1: S11–63. 2012. doi:10.2337/dc12-s011. PMC 3632172
. PMID 22187469. - ↑ Forsmark, CE (2016). "Incretins, Diabetes, Pancreatitis and Pancreatic Cancer: What the GI specialist needs to know.". Pancreatology. 16 (1): 10–3. doi:10.1016/j.pan.2015.11.009. PMID 26795258.
- ↑ "FDA Approves New Treatment for Type 2 Diabetes".
- ↑ "Sanofi New Drug Application for Lixisenatide Accepted for Review by FDA".
- ↑ "FDA Approves Weekly Injectable Diabetes Drug: Albiglutide".
- ↑ "FDA Approves Weekly Injectable Diabetes Drug: Dulaglutide".
- ↑ Longer Acting GLP-1 Receptor Agonists and the Potential for Improved Cardiovascular Outcomes. 2013
- ↑ "GLP-1 Receptor Agonists vs. DPP-4 Inhibitors for Type 2 Diabetes".