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apraglutide

A synthetic, long-acting glucagon-like peptide-2 (GLP-2) agonist, with intestinotrophic activity. Apraglutide is a synthetic 33 amino acid peptide with four amino acid substitutions as compared to the native protein: alanine (Ala) to glycine (Gly) at position 2 (A2G), methionine (Met) to the synthetic lysine analog, aminocaproic acid (Ahx) at position 10 (M10Ahx), asparagine (Asn) to D-phenylalanine (D-Phe) at position 11 (N11F), and asparagine (Asn) to leucine (Leu) at position 16 (N16L). Following subcutaneous administration, apraglutide, as an analog of natural GLP-2, selectively activates GLP-2 receptors in the gastrointestinal (GI) tract, which stimulates intestinal growth, increases intestinal fluid and nutrient absorption, promotes healing, and improves intestinal epithelial integrity and function. As apraglutide becomes highly bound to plasma protein and resistant to degradation by dipeptidyl peptidase-4 (DPP-4), this agent has a longer half-life as compared to other GLP-2 agonists, which allows for less frequent dosing.
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