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Insulin tregopil is an ultra-fast onset, short-acting oral prandial insulin analog developed for the treatment of type 1 and type 2 diabetes mellitus. It is a recombinant human insulin modified by covalent attachment of a methoxy-triethylene-glycol-propionyl moiety at the B29-Lys-amino group via an amide linkage, resulting in a molecule with 100% identical polypeptide sequence to human insulin except for this modification[4][5]. The drug is designed to be administered orally and demonstrates rapid absorption from the gastrointestinal tract, reaching peak plasma concentrations within approximately 30 minutes and exerting its maximal glucose-lowering effect around 30–40 minutes post-dose[2][4][5]. Insulin tregopil acts as an agonist at the insulin receptor, facilitating cellular uptake of glucose in muscle and fat tissue while inhibiting hepatic glucose output[3][7]. Its hepato-preferential action may better mimic physiological first-phase insulin release after meals compared to subcutaneous insulins, potentially reducing early postprandial hyperglycemia without depleting endogenous pancreatic reserves[5][7]. Clinical studies have shown significant reductions in postprandial blood glucose levels when administered before meals in patients with diabetes[1][4].
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