GLP-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 medications 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 dispute over the safety profile of these drugs due to proliferative effects in the pancreas.[citation needed] Diabetes is associated with both acute pancreatitis and pancreatic cancer. While some recent studies have not found that these drugs can cause either pancreatitis or cancer,[4] a 2017 study found that recent prescription of incretins was associated with an increased risk of pancreatic cancer over non-insulin anti diabetic drugs (NIADs).[5]
Approved GLP-1 agonists:
- exenatide (Byetta/Bydureon), approved in 2005/2012
- liraglutide (Victoza, Saxenda), approved 2010[6]
- lixisenatide (Lyxumia), approved in 2016[7]
- albiglutide (Tanzeum), approved in 2014 by GSK[8]
- dulaglutide (Trulicity), approved in 2014—manufactured by Eli Lilly[9]
- semaglutide (Ozempic), approved in 2017.[10]
Under investigation:[1]
- taspoglutide, phase III halted Sept 2010
These agents work by activating the GLP-1R, rather than inhibiting the breakdown of GLP-1 as do DPP-4 inhibitors, and are generally considered more potent.[11]
As of 2017 it was unclear if they affect a person's risk of death.[12]
A JAMA article meta-analysis in 2018 (covering studies concerning GLP-1 agonists, DPP-4 inhibitors, and SGLT2 inhibitors) showed GLP-1 agonists were associated with lower stroke risk than controls.[13]
References
- ^ a b 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.
- ^ Schroeder, C. "Incretin Meds Like Januvia and Victoza Again Linked to Pancreatic Cancer". DrugNews. Retrieved 24 February 2018.
- ^ "FDA Approves New Treatment for Type 2 Diabetes".
- ^ "FDA approves Adlyxin to treat type 2 diabetes".
- ^ "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".
- ^ Liu, J; Li, L; Deng, K; Xu, C; Busse, JW; Vandvik, PO; Li, S; Guyatt, GH; Sun, X (8 June 2017). "Incretin based treatments and mortality in patients with type 2 diabetes: systematic review and meta-analysis". BMJ (Clinical research ed.). 357: j2499. doi:10.1136/bmj.j2499. PMC 5463186. PMID 28596247.
- ^ Zheng, Sean L.; Roddick, Alistair J.; Aghar-Jaffar, Rochan; Shun-Shin, Matthew J.; Francis, Darrel; Oliver, Nick; Meeran, Karim (2018-04-17). "Association Between Use of Sodium-Glucose Cotransporter 2 Inhibitors, Glucagon-like Peptide 1 Agonists, and Dipeptidyl Peptidase 4 Inhibitors With All-Cause Mortality in Patients With Type 2 Diabetes". JAMA. 319 (15). doi:10.1001/jama.2018.3024. ISSN 0098-7484.
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