The incidence of type 2 diabetes mellitus (T2DM) has been on the increase in recent times. Although several oral treatments for T2DM are available, some of them have been found to elicit undesirable side effects. This therefore underscores the need for new treatment options with lesser side effects than the existing ones for people with T2DM. Free fatty acid receptor 1 (FFAR1), also known as GPR40, belongs to a class of G-protein coupled receptors that are encoded by FFAR1 genes in humans. It is expressed in the pancreatic β-cells and it is activated by medium- and long-chain saturated and unsaturated fatty acids. Thus it responds to endogenous medium and long chain unsaturated fatty acids, resulting in enhancement of insulin secretion during increased glucose levels. The glucose dependency of insulin secretion has made this receptor a very good target for developing therapies that could be efficacious with fewer side effects than the existing therapies for the treatment of T2DM. Given that tremendous efforts have been made in recent times in developing novel FFAR1 agonists with antidiabetic potentials, this article provides a current status of knowledge on the efforts made so far in developing novel FFAR1 agonists that would be of relevance in the management of T2DM.

近年来，2型糖尿病（T2DM）的发病率一直在上升。尽管有几种针对T2DM的口服治疗方法，但已经发现其中一些会引起不良的副作用。因此，这突显了对于T2DM患者而言，需要新的治疗方法，且副作用要比现有方法少。游离脂肪酸受体1（FFAR1）也称为GPR40，属于一类由FFAR1基因编码的G蛋白偶联受体。它在胰腺β细胞中表达，并被中链和长链饱和和不饱和脂肪酸激活。因此，它对内源性中链和长链不饱和脂肪酸有反应，导致葡萄糖水平升高时胰岛素分泌增加。胰岛素分泌的葡萄糖依赖性使该受体成为开发有效的方法的靶标，与现有的治疗T2DM的方法相比，该方法可能有效且副作用更少。鉴于最近在开发具有抗糖尿病潜力的新型FFAR1激动剂方面已付出了巨大的努力，本文提供了有关到目前为止开发新型FFAR1激动剂与T2DM管理相关的努力的最新知识。