GLP-1 receptor
Glucagon-like peptide-1 (GLP-1) is a gut hormone (incretin); its receptor is an 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
16 пептидов с исследованиями по этой темеAmycretin is a unimolecular GLP-1 and amylin receptor agonist from Novo Nordisk — in development both as a once-weekly subcutaneous and a once-daily oral form for obesity and type 2 diabetes.
- РКИ на людяхIn a randomised phase-1b/2a study, subcutaneous amycretin produced a marked, dose-dependent weight loss with no apparent plateau through week 36.
CagriSema is a fixed-dose combination of the amylin analogue cagrilintide and the GLP-1 agonist semaglutide (Novo Nordisk), in late-stage development for obesity and type 2 diabetes.
- Исследование на людяхCombines the amylin and GLP-1 axes in a single weekly product.
GLP-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.
- РКИ на людяхHbA1c reduction versus placebo, sitagliptin, exenatide and insulin glargine documented in the AWARD trial series
Ecnoglutide (XW003) is a long-acting, cAMP-signalling-biased GLP-1 analogue from Sciwind Biosciences. Derived from GLP-1(7-37) with an alanine-to-valine substitution at position 8, it activates the GLP-1 receptor selectively via the cAMP pathway over β-arrestin recruitment. Investigated for weight management and in type 2 diabetes.
- РКИ на людяхStatistically significant HbA1c reduction versus placebo in adults with type 2 diabetes over 20 weeks observed in a phase-2 trial
Efinopegdutide (MK-6024, formerly JNJ-64565111 / HM12525A) is a once-weekly dual agonist at the GLP-1 and glucagon receptors, developed by Hanmi and Merck. It has been studied for obesity and notably for metabolic liver disease (MASH/NAFLD); a phase-2 trial showed greater liver-fat reduction than semaglutide. Investigational, not approved.
- РКИ на людяхGreater relative reduction in liver fat content than semaglutide reported in a 24-week phase-2a trial
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.
- РКИ на людяхHbA1c 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).
- РКИ на людяхReduction 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.
- РКИ на людяхReduction of postprandial glucose stronger than with weekly GLP-1 RAs documented across several GetGoal trials
- РКИ на людяхWeight loss as a secondary endpoint reported in the GetGoal trials — smaller than with weekly GLP-1 RAs
Maridebart cafraglutide (MariTide, Amgen) is a bispecific molecule: a GLP-1 receptor agonist combined with a GIP receptor antagonist, designed for monthly dosing; in phase 3 for obesity.
- РКИ на людяхIn the phase-2 study, participants without diabetes achieved a mean weight loss of up to about 20% at 52 weeks — with no apparent plateau.
Synthetic oxyntomodulin analogue that simultaneously activates the GLP-1 and glucagon receptors (dual agonist). Developed by Innovent Biologics and Eli Lilly. In China the NMPA approved mazdutide on 27 June 2025 for chronic weight management; a further filing for type 2 diabetes is under review in China. Outside China the substance remains in clinical development.
- РКИ на людяхClinically relevant weight reduction in adults with overweight or obesity over 48 weeks documented in a phase-3 trial
Pemvidutide is a 29-amino-acid GLP-1/glucagon dual receptor agonist (Altimmune) under investigation for obesity and the fatty-liver disease MASH.
- Исследование на людяхIn a placebo-controlled 12-week study (MASLD), liver fat content fell by up to 68.5%; 55.6% of those treated reached liver-fat normalisation.
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.
- РКИ на людяхWeight reduction over 48 weeks observed in the phase-2 obesity trial — at the highest dose greater than documented for other incretin-based therapies
Long-acting GLP-1 receptor agonist. Approved as a medicinal product for type-2 diabetes (Ozempic, Rybelsus), chronic weight management (Wegovy) and cardiovascular risk in obesity. One of the best-studied substances on this platform — many large human RCTs.
- РКИ на людяхReduction of HbA1c in type-2 diabetes
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.
- РКИ на людяхWeight 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).
- РКИ на людяхReduction in HbA1c versus placebo and versus semaglutide observed in randomised trials
VK2735 is a dual GLP-1/GIP receptor agonist from Viking Therapeutics, in development in both subcutaneous and oral forms for obesity.
- РКИ на людяхIn the phase-2 VENTURE study (subcutaneous, 13 weeks), VK2735 reached a mean weight loss of up to 14.7% with no apparent plateau.