molecules of the month


oral allosteric glucokinase activator

Ph. III candidate in T2DM

HbA1c reduction vs placebo

Nat. Med.

Hua Medicine, Shanghai, CN

Dorzagliatin Chemical Structure, oral allosteric glucokinase activator - Hua Medicine, Shanghai, CN
5 mins read

Context. Dorzagliatin (Hua Medicine) is an oral dual-acting full glucokinase (GK) activator being developed for type 2 diabetes. More than 50 years since the first report of the role of GK in glucose metabolism, no agents targeting this enzyme have been approved, although not for lack of trying. We recently covered a partial GK activator, BMS-820132 (BMS), with more context. Roche’s piragliatin was the first GK activator to be studied in patients with type 2 diabetes, but the compound, like many to succeed it, disappointed in the clinic due to increased risk of hypoglycemia and gradual loss of efficacy. Alternative strategies such as the development of hepatoselective molecules and partial activation of the enzyme have been tried and some of…

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