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**HMS1005** is a second-generation glucokinase activator (GKA) developed by Hua Medicine as a new molecular entity with optimized physicochemical properties. It functions as a prodrug of dorzagliatin (HMS5552), rapidly converting to the active form in the body, and is formulated as an extended-release tablet for once-daily oral administration. This design prolongs the drug's action time, enhances patient adherence, increases intestinal exposure to stimulate GLP-1 secretion, and supports stable 24-hour blood glucose control in type 2 diabetes (T2D) patients, including those with obesity. Following positive Phase Ia single-ascending dose results in the US, it has advanced to Phase Ib multiple-ascending dose trials evaluating safety, tolerability, pharmacokinetics, pharmacodynamics, and biomarkers like glucose, insulin, C-peptide, GLP-1, and glucagon.[1][2][5]
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