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List of GLP-1 receptor agonists (revision 10)

Old revision·05:06, 19 Dec 2024·RetatrutideRuben

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List of GLP-1 receptor agonistsReference material
ScopeAgonists at the GLP-1 receptor, alone or with others
ExcludedDPP-4 inhibitors, which raise endogenous hormone
List infobox · conventions

This list enumerates agonists at the GLP-1 receptor, including those that also engage other receptors of the glucagon-secretin family. DPP-4 inhibitors are excluded: they raise endogenous incretin concentrations rather than agonising the receptor directly. See Dipeptidyl peptidase-4.[1]

Status is given as approved or investigational without specifying jurisdiction, since approval differs between countries. See Regulatory status by jurisdiction.[2]

Compounds appearing here are covered by their own articles where one exists. Inclusion is not an endorsement, and several entries are investigational compounds not approved anywhere.[3]

GLP-1 receptor agonists

[edit]
CompoundRouteIntervalStatus
ExenatideSubcutaneousTwice daily or weeklyApproved
LixisenatideSubcutaneousDailyApproved
LiraglutideSubcutaneousDailyApproved
DulaglutideSubcutaneousWeeklyApproved
SemaglutideSubcutaneousWeeklyApproved
Oral semaglutideOralDailyApproved
OrforglipronOralDailyInvestigational

The list spans three architectures: exendin-derived peptides, acylated GLP-1 analogues, an Fc fusion, and a non-peptide small molecule. See GLP-1 receptor agonist for how each solves the half-life problem.[1]

Multi-receptor agonists

[edit]
CompoundReceptorsStatus
TirzepatideGIP, GLP-1Approved
SurvodutideGlucagon, GLP-1Investigational
EfinopegdutideGlucagon, GLP-1Investigational
MazdutideGlucagon, GLP-1Investigational
RetatrutideGIP, GLP-1, glucagonInvestigational

These are treated at Dual incretin agonist and Triple agonist. Their receptor ratios are fixed by chemistry and are not comparable between publications, since reported potencies are assay-dependent.[1]

References

  1. ^ a b c Drucker DJ. "Mechanisms of action and therapeutic application of glucagon-like peptide-1." Cell Metabolism 27(4):740–756 (2018). PMID 29617641.
  2. ^ American Diabetes Association. "Standards of Care in Diabetes." Diabetes Care 47(Suppl 1) (2024).
  3. ^ United States Pharmacopeia, General Chapter <1503>, Quality Attributes of Synthetic Peptide Drug Substances.
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