FK506(FK)是1984年日本从链霉菌属中分离出来的一种新的大环内酯类免疫抑制剂。1986年Ochiai等首次报告了其对大鼠心脏移植模型有免疫抑制作用。其后,英国、日本、美国相继开展了有关FK的基础研究。1989年2月匹兹堡大学开始将其应用于临床,至1990年6月止的15个月中,应用例数达700例以上。其适应证主要为需进行免疫抑制治疗的脏器移植,其中包括肝、肾、心、肺、胰、胰岛以及小肠等所有脏器的移植,效果极佳。此外,对少数皮肤和肾脏的自身免疫性疾患也应用了FK506。根据上述结果,本文概述FK的有效性和存在的问题,以及与以往的免疫抑制剂环孢菌素A(CSA)的异同。免疫抑制作用FK与CSA的化学结构不同,但作用机制基本相同,都是以IL-2的产生为中心,特异性地抑制T细胞活性。其抑制作用均系与其他的细 FK506 (FK) is a new macrolide immunosuppressive agent isolated from Streptomyces in Japan in 1984. In 1986, Ochiai et al. first reported its immunosuppressive effects on rat heart transplantation models. Since then, Britain, Japan, and the United States have carried out basic research on FK. In February 1989, the University of Pittsburgh began to apply it in clinical practice. By the end of June of 1990, the number of cases had reached more than 700. The indications are mainly for organ transplantation requiring immunosuppressive therapy, including liver, kidney, heart, lung, pancreas, islets, and small intestine, with excellent results. In addition, FK506 has also been applied to a small number of skin and kidney autoimmune disorders. Based on the above results, this article outlines the effectiveness and existing problems of FK, as well as the similarities and differences between conventional immunosuppressant cyclosporin A (CSA). The immunosuppressive effects of FK and CSA are different in chemical structure, but the mechanism of action is basically the same. All of them focus on the production of IL-2 and specifically inhibit the activity of T cells. Its inhibitory effect is similar to other fine