抗整合素药物risuteganib治疗眼底疾病的研究现状与进展  

Progress of anti-integrin drug risuteganib in the treatment of ocular fundus diseases

作　　者：胡亚男 郑志[1] Hu Yanan;Zheng Zhi(Department of Ophthalmology,Shanghai General Hospital,Shanghai Jiao Tong University,Shanghai Key Laboratory of Ocular Fundus Diseases,Shanghai 200080,China)

机构地区：[1]上海交通大学附属第一人民医院眼科,上海市眼底病重点实验室,200080

出　　处：《中华眼底病杂志》2020年第10期813-816,共4页Chinese Journal of Ocular Fundus Diseases

基　　金：国家自然科学基金(81770947);国家科技重大专项(2017ZX09304010)。

摘　　要：整合素是介导细胞-细胞和细胞-细胞外基质相互作用的一类黏附分子,它将胞外配体与胞内骨架、信号转导通路相联系,参与多种生理病理过程。Risuteganib(商品名:Luminate®)是一种广谱整合素抑制剂,具有抗新生血管、诱导玻璃体后脱离、神经保护等作用,可用于治疗糖尿病黄斑水肿、玻璃体黄斑牵引、萎缩型老年性黄斑变性等多种眼底疾病。Risuteganib已成功达到三项2期临床试验终点,并即将开展治疗糖尿病黄斑水肿的3期临床试验。目前的临床试验结果显示,risuteganib的耐受性良好,没有出现药物相关的毒性反应或反复眼内注射引起的炎症。基于其独特的作用机制和较长的药效持续时间,眼内注射抗整合素药物risuteganib既可能成为一种有效的独立疗法,也可作为现有抗VEGF药物治疗的补充疗法。Integrins is a family of multi-functional cell-adhesion molecules,heterodimeric receptors that connect extracellular matrix to actin cytoskeleton in the cell cortex,thus regulating various physiological and pathological processes.Risuteganib(Luminate®)is a novel broad-spectrum integrin inhibitor.Based on multiple biological functions of anti-angiogenesis,vitreolysis,and neuroprotection,risuteganib is hopeful in treating several fundus diseases such as diabetic macular edema,vitreomacular traction,and non-exudative age-related macular degeneration.By far,risuteganib has successfully met the endpoints for three phase 2 studies and is preparing to enter the phase 3 of diabetic macular edema clinical trials.Overall the risuteganib is safe with no serious ocular or systemic adverse events.Given the unique mechanism of action and longer duration of efficacy,intravitreal injection of risuteganib has the potential to serve as a primary therapy,or adjunctive therapy to anti-VEGF agents.

关 键 词：整合素类 玻璃体脱离 黄斑变性/药物疗法 黄斑水肿/药物疗法 综述 

分 类 号：R774.5[医药卫生—眼科]