在研广谱头孢菌素类抗生素的新进展

An update on progress in investigational broad-spectrum cephalosporins

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。

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 first 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.