Glucagon
The endogenous counter-regulatory hormone to insulin — FDA-approved for severe hypoglycemia (injectable GlucaGen, nasal Baqsimi, autoinjector Gvoke). Also the pharmacological template for GLP-1/glucagon dual agonists like Pemvidutide and Retatrutide.
A 29-amino-acid pancreatic α-cell peptide hormone that opposes insulin by stimulating hepatic glycogenolysis and gluconeogenesis; FDA-approved for the rescue treatment of severe hypoglycemia and as a diagnostic aid in endocrine imaging, and the structural and pharmacological template for the glucagon-receptor agonist arm of GLP-1/glucagon dual and triple agonists currently in late-stage development.
Mechanism of action
Binds the glucagon receptor (a class B GPCR) on hepatocytes, activating adenylyl cyclase, raising cAMP, and driving phosphorylase-mediated glycogenolysis and the gluconeogenic program. The acute rise in blood glucose reverses severe hypoglycemia. Chronic partial glucagon-receptor agonism is the basis for the "energy-expenditure arm" of GLP-1/glucagon dual agonists such as pemvidutide, cotadutide, and the glucagon component of retatrutide.
Primary uses
- Severe hypoglycemia (rescue)
- Diagnostic adjunct in gastrointestinal and endocrine imaging
- Research template for glucagon-receptor agonism in dual/triple agonist development
Typical dosing
Rescue dosing only; not a maintenance medication.
Regulatory status
FDA-approved in multiple formulations: GlucaGen (injectable, Novo Nordisk), Baqsimi (nasal powder, Amphastar/Lilly, 2019), Gvoke (subcutaneous autoinjector, Xeris, 2019). Indicated for severe hypoglycemia and as a diagnostic aid.
References
- [fda-pi] GlucaGen (glucagon) Prescribing Information. Novo Nordisk.
- [fda-pi] Baqsimi (glucagon) Prescribing Information. Amphastar Pharmaceuticals.
- [fda-pi] Gvoke (glucagon) Prescribing Information. Xeris Biopharma.
Related peptides
This entry is for educational purposes only and does not constitute medical advice. Dosing information reflects published regulatory or research data and is not a recommendation. Many compounds described here are not approved for human use in the United States. Consult a licensed medical professional before considering any peptide therapy.