Dapiglutide
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Product Description
Dapiglutide is a novel synthetic peptide drug candidate currently under investigation in clinical trials, such as NCT05788601, for the treatment of obesity. It is a 34-amino acid dual agonist peptide designed to simultaneously activate the glucagon-like peptide-1 receptor (GLP-1R) and the glucagon-like peptide-2 receptor (GLP-2R), which may improve conditions like short bowel syndrome and combat obesity. Additionally, Dapiglutide acts as a dual agonist of the GLP-1 and GIP (glucose-dependent insulinotropic polypeptide) receptors, positioning it as part of the new generation of incretin mimetics for the treatment of type 2 diabetes and obesity. Structurally, Dapiglutide is a peptide analogue with modifications such as fatty acid side chains for albumin binding and substitutions that enhance its stability against DPP-4 degradation, similar to tirzepatide, another dual GLP-1/GIP agonist.
Synthesis Methods
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Synthetic Peptide Design
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Peptide Backbone: A long chain of amino acids linked by peptide bonds.
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Acylation: Incorporation of a fatty acid side chain (e.g., a C18 di-acid) to enhance binding to albumin and extend half-life.
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Enzymatic Stability: Engineered to be resistant to degradation by DPP-4, extending its duration of action in the body.
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Additional Information
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Comparative Analysis
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Liraglutide: Single GLP-1 agonist with fatty acid chain; Molecular Weight ≈ 3751.2 g/mol.
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Semaglutide: Single GLP-1 agonist, more potent than Liraglutide; Molecular Weight ≈ 4113.6 g/mol.
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Dapiglutide: Dual GLP-1/GIP agonist, designed for superior efficacy; Molecular Weight ≈ 4166.8 g/mol.
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Uses and Applications
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Therapeutic Uses
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Type 2 Diabetes Mellitus: Dapiglutide is being investigated for its potential to improve glucose control by enhancing insulin secretion and reducing glucagon levels.
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Obesity: It is being studied for its ability to reduce appetite and promote weight loss, as demonstrated in clinical trials.
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Short Bowel Syndrome: Dapiglutide has shown promise in improving intestinal function and reducing the need for parenteral nutrition in murine models of short bowel syndrome.
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Research Applications
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Research Use: Currently for research use only. Not approved for clinical use.
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Custom Packaging: Available in quantities ranging from 1 mg to 1000 mg.
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Properties and Characteristics
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Chemical Information
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IUPAC Name: (complex peptide sequence — varies by source; not fully standardized due to its peptide nature)
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Molecular Formula: C₁₉₂H₃₀₂N₄₆O₅₇
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Molecular Weight: ≈ 4166.8 g/mol
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Chemical Class: Synthetic peptide; GLP-1/GIP receptor dual agonist
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Structure Type: Linear peptide with multiple amide linkages, side-chain modifications, and fatty acid acylation to extend half-life.
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Chemical Properties
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Appearance: White to off-white amorphous solid (typically supplied as lyophilized powder)
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Solubility: Freely soluble in aqueous buffers (pH 7–8); insoluble in most organic solvents
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Stability: Stable under refrigeration (2–8 °C); sensitive to high temperature and light
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pKa: Multiple values due to lysine, aspartate, and terminal residues (typ. 3–10)
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LogP (estimated): Very low (hydrophilic peptide)
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Hydrogen bond donors/acceptors: Numerous (typical for large peptides)
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Pharmacological Overview
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Mechanism of Action: Dual activation of GLP-1 and GIP receptors → enhances glucose-dependent insulin secretion, suppresses glucagon, slows gastric emptying, and reduces appetite.
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Therapeutic Area: Type 2 diabetes mellitus, obesity
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Receptor Targets: GLP-1R and GIPR agonist
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Administration: Subcutaneous injection (investigational)
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Half-life: Extended via lipid conjugation and albumin binding (several days in preclinical models)
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Safety and Handling
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Storage Conditions
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Temperature: -20°C, sealed and protected from light.
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Purity: ≥96% (HPLC/MS assay).
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Safety Data
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Hazard Identification: GHS signal word "Warning"; GHS hazard statements include H302 (Harmful if swallowed), H315 (Causes skin irritation), H319 (Causes serious eye irritation), and H335 (May cause respiratory irritation).
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Precautionary Statements: P261 (Avoid breathing dust/fume/gas/mist/vapours/spray), P280 (Wear protective gloves/protective clothing/eye protection/face protection), P301+P312 (IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell), P302+P352 (IF ON SKIN: wash with plenty of soap and water), P305+P351+P338 (IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing).
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Clinical Trials and Safety
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Phase 1b Trial: Dapiglutide appeared safe with no related serious or severe adverse events (AEs). The most frequent AEs reported were gastrointestinal disorders and metabolism and nutrition disorders (mainly decreased appetite). Most AEs were mild. The pharmacokinetics showed dose proportionality and a mean half-life of 112-119 hours across the dose cohorts.
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