The present invention provides uses of a glucokinase activator in combination with metformin. Uses include treating type 2 diabetes, lowering blood glucose, improving insulin sensitivity, enhancing phosphorylation of glucose, and improving the therapeutic effectiveness of metformin. The invention also provides pharmaceutical compositions that comprise a GK activator and metformin. The invention also provides a salt formed between metformin and a GK activator.本發明提供葡萄糖激酶活化劑併以二甲雙胍之用途。該用途包括治療2型糖尿病、降低血糖、改良胰島素敏感性、增強葡萄糖之磷酸化及改良二甲雙胍之治療有效性。本發明亦提供一種包含GK活化劑及二甲雙胍之醫藥組合物。本發明亦提供一種由二甲雙胍與GK活化劑之間形成之鹽。
