在研广谱头孢菌素类抗生素的新进展在研广谱头孢菌素类抗生素的新进展.pdf

中国抗生素杂志2010年12月第35卷第12期 . 881 . 文章编号：1001-8689(2010) 12-0881-11 综 述 在研广谱头孢菌素类抗生素的新进展 * 崔玉彬 蒋晓磊 曹胜华 (中国医药集团总公司四川抗菌素工业研究所，成都 610052) 摘要： 目前头孢菌素类药物的研究热点在于寻找对耐药革兰阳性致病菌敏感，尤其是对耐甲氧西林金黄色葡萄球菌 (MRSA)敏感的头孢菌素类化合物及对高活性化合物进行结构修饰，改善其药学性质。本文先就2008 年上市的抗MRSA 广谱新药ceftobiprole进行介绍，再将近十余年研发中的广谱头孢菌素类抗生素的新进展做一简要综述，其中ceftaroline和 FR264205(CXA-101)是较有前景的候选药物，ceftaroline新药上市申请(NDA)有望于2010年获准。 关键词：头孢菌素；MRSA ；Ceftobiprole ；Ceftaroline ；FR264205(CXA-101) ；RWJ-54428 ；BMS-247243 中图分类号：R978.1 文献标识码：A An update on progress in investigational broad-spectrum cephalosporins Cui Yu-bin, Jiang Xiao-lei and Cao Sheng-hua (Sichuan Industrial Institute of Antibiotics, China National Pharmaceutical Group Corporation, Chengdu 610052) Abstract The objects of active research on cephalosporin drugs were new cephalosporins with high antibacterial activities against gram-positive pathgens, especially against methicillin-resistant Staphylococcus aureus (MRSA), and prodrugs with improved pharmaceutical properties which were derived from high active compounds. This article fi rst introduced ceftobiprole approved in 2008, a new broad-spectrum antibiotic effective against MRSA, and then gave an investigational review of broad-spectrum cephalosporins of this decade, among which ceftaroline and FR264205(CXA-101) were more promising drug candidates. And it was expected that new drug application (NDA) of ceftaroline would be approved in 2010. Key words Cephalosporins; MRSA; Ceftobiprole; Ceftaroline; FR264205(CXA-101); RWJ-54428; BMS- 247243 头孢菌素类抗生素是临床上用于治疗细菌感染 球菌(MRSA)等革兰