GLP-1 receptor
Incretin receptor with G-protein-coupled signalling cascade. Activation glucose-dependently stimulates insulin secretion, inhibits glucagon, delays gastric emptying and modulates central satiety signalling. Pharmacological target of multiple approved obesity and diabetes therapies.
Peptides on this topic
7 peptides researched for this topicGLP-1 receptor agonist designed as a fusion protein of two modified GLP-1(7-37) sequences covalently linked to a human IgG4-Fc fragment. FDA-approved 2014 (Trulicity) for type 2 diabetes; EMA approval 2014.
- Human RCTHbA1c reduction versus placebo, sitagliptin, exenatide and insulin glargine documented in the AWARD trial series
Synthetic version of exendin-4, originally isolated from the saliva of the Gila monster (Heloderma suspectum). First GLP-1 receptor agonist, FDA-approved 2005 as Byetta. Weekly depot form Bydureon approved 2012.
- Human RCTHbA1c reduction versus placebo in type 2 diabetes over 30 weeks documented in the AMIGO trials
GLP-1 receptor agonist with a half-life of about 13 hours. The first daily (not weekly) modern GLP-1 RA — approved as Victoza for type 2 diabetes (2010) and Saxenda for obesity (2014).
- Human RCTReduction in cardiovascular events (MACE) in type-2-diabetes patients at high CV risk over 3.8 years
Synthetic exendin-4 analog with a C-terminal lysine extension. Prandial GLP-1 RA focused on postprandial glucose. FDA-approved 2016 as Adlyxin; EMA-approved 2013 as Lyxumia. Sanofi discontinued US distribution in 2023.
- Human RCTReduction of postprandial glucose stronger than with weekly GLP-1 RAs documented across several GetGoal trials
- Human RCTWeight loss as a secondary endpoint reported in the GetGoal trials — smaller than with weekly GLP-1 RAs
Synthetic triagonist peptide that simultaneously activates the GLP-1, GIP and glucagon receptors. Developed by Eli Lilly; in phase-3 trials for obesity (TRIUMPH programme) and type 2 diabetes. No marketing approval yet.
- Human RCTWeight reduction over 48 weeks observed in the phase-2 obesity trial — at the highest dose greater than documented for other incretin-based therapies
Synthetic peptide that simultaneously activates the GLP-1 and glucagon receptors. Developed by Boehringer Ingelheim and Zealand Pharma; in phase-3 trials for obesity (SYNCHRONIZE) and MASH. No marketing approval yet.
- Human RCTWeight reduction over 46 weeks documented in a phase-2 obesity trial
Synthetic peptide that simultaneously activates the GLP-1 and GIP receptor (dual agonist). Approved in the US and EU for type 2 diabetes (Mounjaro) and obesity (Zepbound).
- Human RCTReduction in HbA1c versus placebo and versus semaglutide observed in randomised trials