GLP-1 moiety from Dulaglutide
Description
Dulaglutide is a long-acting glucagon-like peptide-1 (GLP-1) receptor agonist (RA) developed for type 2 diabetes mellitus (T2DM) treatment. Its structure comprises a modified GLP-1(7-37) peptide covalently linked to a human immunoglobulin G4 (IgG4) Fc fragment via a small linker. This fusion extends its half-life to ~90 hours by reducing enzymatic degradation by dipeptidyl peptidase-4 (DPP-4) and renal clearance, enabling once-weekly subcutaneous administration . The GLP-1 moiety retains glucose-dependent insulin secretion, suppression of glucagon release, and appetite regulation, while the Fc fragment enhances pharmacokinetic stability .
Comparison with Similar Compounds
Comparison with Similar GLP-1 Receptor Agonists
Dulaglutide is compared below with other GLP-1 RAs, including liraglutide , exenatide extended-release (ER) , and semaglutide , based on efficacy, safety, dosing, and pharmacokinetics.
Efficacy in Glycemic Control and Weight Loss
- Head-to-Head Comparisons: Dulaglutide vs. Liraglutide: In the AWARD-6 trial, dulaglutide demonstrated non-inferiority to liraglutide in HbA1c reduction (-1.42% vs. -1.36%) but showed comparable weight loss (-3.61 kg vs. -3.57 kg) . Dulaglutide vs. Semaglutide: Indirect comparisons from SUSTAIN 7 revealed semaglutide 1.0 mg achieved superior HbA1c reductions (-1.8% vs. -1.4%) and weight loss (-6.5 kg vs. -3.0 kg) compared to dulaglutide 1.5 mg .
Pharmacokinetic and Dosing Advantages
- Key Advantages of Dulaglutide: Simplified dosing regimen due to Fc-mediated stability, improving patient adherence . No requirement for dose titration, unlike liraglutide .
Properties
Molecular Formula |
C₁₄₉H₂₂₁N₃₇O₄₉ |
|---|---|
Molecular Weight |
3314.62 |
sequence |
One Letter Code: HGEGTFTSDVSSYLEEQAAKEFIAWLVKGGG |
Origin of Product |
United States |
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