GLP-1 Receptor Agonist

A GLP-1 Receptor Agonist is a receptor agonist that binds to and activates GLP-1 receptors on target cells (primarily in pancreatic tissue and brain tissue).

• AKA: Incretin Mimetic, GLP-1 Analog, GLP-1RA.
• Context:
  • It can typically activate GLP-1 Receptors on pancreatic beta cells to stimulate glucose-dependent insulin secretion.
  • It can typically lower Blood Glucose Levels through incretin-like mechanisms.
  • It can typically resist Enzymatic Degradation by dipeptidyl peptidase-4 (DPP-4).
  • It can typically promote Weight Loss through appetite suppression and gastric emptying delay.
  • It can typically reduce Cardiovascular Risk in type 2 diabetes patients.
  • ...
  • It can often be administered through Subcutaneous Injection or oral formulation.
  • It can often have Extended Half-Lifes compared to native GLP-1 hormone.
  • It can often cause Gastrointestinal Side Effects including nausea and vomiting.
  • It can often be used in combination with metformin or other antidiabetic medications.
  • ...
  • It can range from being a Short-Acting GLP-1 Receptor Agonist to being a Long-Acting GLP-1 Receptor Agonist, depending on its pharmacokinetic profile.
  • It can range from being a Pure GLP-1 Receptor Agonist to being a Dual Incretin Receptor Agonist, depending on its receptor selectivity.
  • ...
  • It can achieve Glycemic Control without significant hypoglycemia risk.
  • It can preserve Pancreatic Beta Cell Function through protective mechanisms.
  • It can slow Atherosclerosis Progression through anti-inflammatory effects.
  • It can be contraindicated in medullary thyroid carcinoma and multiple endocrine neoplasia syndrome type 2.
  • ...
• Examples:
  • First-Generation GLP-1 Receptor Agonists, such as:
    • Exenatide, requiring twice-daily administration.
    • Liraglutide, with once-daily administration.
  • Second-Generation GLP-1 Receptor Agonists, such as:
    • Semaglutide, with once-weekly administration and oral formulation option.
    • Dulaglutide, with once-weekly administration and ready-to-use pen.
  • Dual Incretin Receptor Agonists, such as:
    • Tirzepatide, targeting both GLP-1 receptors and GIP receptors.
  • Extended-Release GLP-1 Receptor Agonists, such as:
    • Exenatide Extended-Release, with once-weekly administration.
    • Albiglutide, with once-weekly administration (discontinued).
  • ...
• Counter-Example(s):
  • DPP-4 Inhibitors, which increase endogenous GLP-1 levels rather than directly activating GLP-1 receptors.
  • Insulin, which directly replaces hormone deficiency rather than enhancing incretin pathways.
  • Sulfonylureas, which stimulate insulin secretion through glucose-independent mechanisms.
  • SGLT2 Inhibitors, which lower blood glucose through renal glucose excretion rather than incretin effects.
• See: Glucagon-Like Peptide-1 (GLP-1) Hormone, GLP-1 Receptor, Type 2 Diabetes Mellitus, Incretin, Dipeptidyl Peptidase-4, Glucose-Dependent Insulinotropic Peptide, Antidiabetic Drug, Peptide Therapeutic, Subcutaneous Injection.

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