GLP-1 and metabolic receptor agonists

Incretin and glucagon-family peptides characterised against the GLP-1, GIP, glucagon and amylin receptors.

This category groups compounds by receptor rather than by research area. The receptors are four: GLP-1, GIP, glucagon and amylin. That rule is why an amylin analogue sits beside the incretin agonists — the grouping follows the receptor families the entries describe, not the subject areas they appear under.

Three distinctions organise what is here. The first is how many receptors a single molecule engages: semaglutide engages one, tirzepatide two, retatrutide three. The second is which receptors those are, since the glucagon arm and the two incretin arms are described differently in the literature. The third is regulatory position, which varies sharply across the group and does not follow from pharmacology.

Four background articles cover the receptors one at a time: the GLP-1 receptor, the GIP receptor, the glucagon receptor and the amylin receptor. Triple receptor agonists explained covers multi-agonist design. Side-by-side pages set out retatrutide against tirzepatide, tirzepatide against semaglutide and cagrilintide against semaglutide.

Compounds listed below without a link do not yet have a published entry.

Compounds in this category

13 of 13 entries are published. Compounds without a published entry are listed without a link.

  • SemaglutideSemaglutide is a synthetic, acylated analogue of human glucagon-like peptide-1 that acts as an agonist at a single receptor, GLP-1R. It is the active ingredient of approved pharmaceutical products, and that approval belongs to those finished products rather than to the chemical.
  • TirzepatideTirzepatide (development code LY3298176) is a synthetic, fatty-acid-modified peptide that acts as an agonist at two receptors at once — the GIP receptor and the GLP-1 receptor. It is the active ingredient of approved pharmaceutical products, and that approval belongs to those finished products rather than to the chemical.
  • RetatrutideRetatrutide (development code LY3437943) is an investigational synthetic peptide that acts as an agonist at three receptors at once — the GIP, GLP-1 and glucagon receptors. It is not approved by the FDA for any use.
  • CagrilintideCagrilintide (development code NNC0174-0833) is an investigational lipidated analogue of the pancreatic hormone amylin, designed for a weekly interval. It acts at amylin receptors rather than at incretin receptors, and it is not approved by the FDA for any use.
  • CagriSemaCagriSema is an investigational fixed-ratio combination of two separate peptides — the amylin analogue cagrilintide and the GLP-1 receptor agonist semaglutide — administered together once weekly. It is not a single molecule and has no identifiers of its own, and it is not approved by the FDA.
  • SurvodutideSurvodutide (development code BI 456906) is an investigational synthetic acylated peptide that acts as an agonist at two receptors at once — the glucagon receptor and the GLP-1 receptor. It is not approved by the FDA for any use.
  • MazdutideMazdutide is a synthetic acylated analogue of oxyntomodulin that acts as an agonist at two receptors — the GLP-1 receptor and the glucagon receptor. It is approved in China and has not been approved by the FDA for any use.
  • PemvidutidePemvidutide (development code ALT-801) is an investigational synthetic peptide that acts as an agonist at two receptors — the GLP-1 receptor and the glucagon receptor — and has been studied principally in liver disease. It is not approved by the FDA for any use.
  • EloralintideEloralintide (development code LY3841136) is an investigational synthetic analogue of amylin reported to act selectively at the amylin 1 receptor rather than across the calcitonin receptor family. It is not approved by the FDA for any use.
  • LiraglutideLiraglutide is a synthetic, acylated analogue of human glucagon-like peptide-1 that acts as an agonist at a single receptor, GLP-1R. It is the active ingredient of approved pharmaceutical products, and that approval belongs to those finished products rather than to the chemical.
  • DulaglutideDulaglutide is a recombinant fusion protein in which a modified GLP-1 analogue is joined to an immunoglobulin G4 Fc fragment, acting as an agonist at a single receptor, GLP-1R. It is the active ingredient of an approved pharmaceutical product, and that approval belongs to that finished product rather than to the substance.
  • ExenatideExenatide is the synthetic form of exendin-4, a 39-residue peptide isolated from Gila monster venom that acts as an agonist at a single receptor, GLP-1R. It is the active ingredient of approved pharmaceutical products, and that approval belongs to those finished products rather than to the chemical.
  • LixisenatideLixisenatide is a synthetic 44-residue peptide derived from exendin-4 by deleting one proline and appending six lysine residues, acting as an agonist at a single receptor, GLP-1R. It is the active ingredient of approved pharmaceutical products, and that approval belongs to those finished products rather than to the chemical.