摘要
FTY720是一种作用机制独特的免疫抑制剂,可用于器官移植、自体免疫疾病、肿瘤和炎症等疾病的治疗,目前在治疗肾移植排斥反应的应用进入Ⅲ期临床试验,在治疗多发性硬化症的应用进入Ⅱ期临床试验。与环孢素A、他克莫司(FK506)等免疫抑制剂相比,具有活性高毒性低的优点。现综述FTY720的作用机制、构效关系和应用。
FTY720 derived from ISP-1 is a novel immune modulator that prolongs to allograft transplant survival in numerous models by inhibiting lymphocyte emigration from lymphoid organs. It might be used for allograft transplantation, autoimmunity, cancer and inflammatory diseases. The phase II clinical studies has shown that this novel oral medication in the treatment of multiple sclerosis （MS） reduced the rate of clinical relapses by more than 50% and inflammatory disease activity as measured bymagnetic resonance imaging （MRI） by up to 80% over six months compared to placebo. Further phase 11I clinical studies to evaluate the effect of FTY720 for renal graft rejection and phase I1 clinical studies for multiple sclerosis are ongoing. This paper reviews pharmacological mechanism, structure-activity rela- tionship and clinical evaluation of FTY720.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2007年第8期582-585,共4页
Chinese Journal of New Drugs
