GLP-1 (7-36) amide

Summary

GLP-1 (7-36) amide is the primary biologically active, C-terminally amidated form of glucagon-like peptide-1 secreted by intestinal L-cells in response to nutrient ingestion. It is the endogenous ligand for the GLP-1 receptor and the molecular template upon which all GLP-1 receptor agonist drugs (e.g., semaglutide, liraglutide) are based. Its extreme short half-life in vivo limits therapeutic use of the native peptide itself, but it is widely used in research and has been administered intravenously in clinical studies to characterize its pharmacodynamics.

Mechanism of Action

Binds and activates the GLP-1 receptor (GLP1R), a class B GPCR, stimulating glucose-dependent insulin secretion, suppressing glucagon release, slowing gastric emptying, and promoting satiety via central and peripheral pathways. Rapidly degraded by DPP-4 (half-life ~1–2 minutes in vivo).

Routes of Administration

Goals & Uses

• NeuroprotectionNeurologyLow
• Glycemic control (type 2 diabetes)Metabolic / EndocrineHigh
• CardioprotectionCardiovascularModerate
• Body weight reduction / appetite suppressionMetabolic / ObesityModerate
• Beta-cell preservationMetabolicModerate

Contraindications

• Personal or family history of medullary thyroid carcinomaOncologicHigh
• Severe hypersensitivity to GLP-1 peptidesImmunologicalHigh
• Multiple endocrine neoplasia syndrome type 2 (MEN2)OncologicHigh

Adverse Effects

• HypoglycemiaMetabolicUncommonAbnormally low blood glucose
• Injection site reactionsLocalUncommon
• TachycardiaCardiovascularUncommonAbnormally fast heart rate
• NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
• VomitingGastrointestinalUncommonForceful expulsion of stomach contents

Drug Interactions

• Insulin and insulin secretagoguesModerate
• Oral medications with narrow therapeutic indexLow
• DPP-4 inhibitors (e.g., sitagliptin)Moderate

Population Constraints

• PregnancyReproductive SafetyRelative
• Personal or family history of pancreatitisGastrointestinalRelative
• Severe renal impairmentOrgan ImpairmentRelative
• Pediatric populationAgeRelative

Regulatory Status

• European UnionUnapprovedNot approved by EMA as a medicinal product. Serves as research reference compound.
• United StatesUnapprovedNative GLP-1 (7-36) amide is not approved by the FDA as a drug product. Used in research settings. Multiple GLP-1 receptor agonist analogs are FDA-approved (e.g., semaglutide, liraglutide, exenatide).
• United KingdomUnapprovedNot approved by MHRA. Research use only; GLP-1 analogs are approved through EMA/MHRA pathways.

The native peptide is not approved as a drug product in any major jurisdiction. It serves as the pharmacological reference compound and is used in academic and clinical research settings. Approved GLP-1 receptor agonist drugs are structurally modified analogs designed to resist DPP-4 degradation.

Evidence & Sources

No sources recorded yet.