Incretin receptor agonists

Incretin receptor agonists groups 12 indexed compounds. Also written as GLP-1 receptor agonists, incretin mimetics, GLP-1 analogues.

Definition

Incretin receptor agonists are synthetic peptides that bind one or more of the incretin and glucagon family receptors, principally the glucagon-like peptide-1 receptor. A 2024 review in Signal Transduction and Targeted Therapy surveys the signalling mechanisms of the GLP-1 receptor and the agents developed against it, and a 2024 BMJ systematic review and network meta-analysis compares agents in this class on glycaemic control, body weight and lipid profile in type 2 diabetes.

[1, 2]

Class-level mechanism as reported

Members of this class act as agonists at incretin family receptors. The retrieved literature distinguishes single-receptor agonists from dual and triple agonists: tirzepatide is described in its 2021 Lancet trial report as a dual GIP and GLP-1 receptor agonist, and retatrutide in its 2023 Lancet trial report as a GIP, GLP-1 and glucagon receptor agonist. The 2024 GLP-1 receptor review covers the receptor-level mechanisms common to the class.

[3, 4, 1]

Members

Compounds indexed under Incretin receptor agonists
CompoundOther namesPeptideReported half-life
SemaglutideNN9535, NNC 0113-0217YesWithheld pending qualified review
TirzepatideLY3298176, GIP/GLP-1 dual agonistYesWithheld pending qualified review
RetatrutideLY3437943YesWithheld pending qualified review
LiraglutideNN2211, NNC 90-1170YesWithheld pending qualified review
SurvodutideBI 456906YesWithheld pending qualified review
MazdutideIBI362, LY3305677YesWithheld pending qualified review
Maridebart cafraglutideMariTide, AMG 133, AMG133NoWithheld pending qualified review
Exenatideexendin-4, synthetic exendin-4, ByettaYesWithheld pending qualified review
DulaglutideLY2189265, TrulicityNoWithheld pending qualified review
LixisenatideAVE0010, Adlyxin, LyxumiaYesWithheld pending qualified review
OrforglipronLY3502970, FoundayoNoWithheld pending qualified review
GLP-1glucagon-like peptide-1, GLP-1 (7-36) amide, GLP1YesWithheld pending qualified review

12 of 12 compounds in this class are withheld pending qualified review, so their reported values are not shown here and their pages are not published. They are listed because the class is incomplete without them.

Where this page sits

Research records for compounds in this class

Side-by-side pages within this class

All classes: class index. All compounds: compound index.

Sources

  1. Glucagon-like peptide-1 receptor: mechanisms and advances in therapy. Signal Transduct Target Ther (2024). pmid:39289339
  2. Comparative effectiveness of GLP-1 receptor agonists on glycaemic control, body weight, and lipid profile for type 2 diabetes: systematic review and network meta-analysis. BMJ (2024). pmid:38286487
  3. Efficacy and safety of a novel dual GIP and GLP-1 receptor agonist tirzepatide in patients with type 2 diabetes (SURPASS-1): a double-blind, randomised, phase 3 trial. Lancet (2021). pmid:34186022
  4. Retatrutide, a GIP, GLP-1 and glucagon receptor agonist, for people with type 2 diabetes: a randomised, double-blind, placebo and active-controlled, parallel-group, phase 2 trial conducted in the USA. Lancet (2023). pmid:37385280

On each stated value was matched to the record cited for it. That is record matching, not an appraisal of the research. Compiled and checked by: Peptide Monographs editorial desk. No qualified clinical reviewer.

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