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[摘要]：TAK-875 is a free fatty acid receptor 1 (FEA1R/GPR40) agonist, the first in this novel class of antidiabetic agents to enter clinical development. It is a glucose-dependent insulinotropic agent, with a mechanism of action that is novel among insulinotropic drugs, including sulfonylureas, incretins and meglitinides. Single oral doses of TAK-875 stimulate enhanced glucose-dependent insulin secretion and improve postprandial and fasting hyperglycemia, with a low risk of hypoglycemia and no evidence of beta cell toxicity, in preclinical testing. It is well tolerated and has demonstrated efficacy in phase I and II clinical trials, with rapid and effective improvements in postprandial and fasting hyperglycemia, glycosylated hemoglobin-lowering activity, and a low risk of hypoglycemia in patients with type 2 diabetes. TAK-875 is currently undergoing phase 111 testing in Japan and phase 11 testing in the U.S. and Europe. |
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