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[市场上及研发中的新型抗菌药物]

[New antibacterial agents on the market and in the pipeline].

作者信息

Kern W V

出版信息

Internist (Berl). 2015 Nov;56(11):1255-63. doi: 10.1007/s00108-015-3705-0.

Abstract

After some years of stagnation there have been several new successful developments in the field of antibacterial agents. Most of these new developments have been in conventional antibacterial classes. New drugs among the beta-lactam agents are methicillin-resistant Staphylococcus aureus (MRSA) active cephalosporins (ceftaroline and ceftobiprole) and new combinations of beta-lactam with beta-lactamase inhibitors (ceftolozane/tazobactam, ceftazidime/avibactam, imipenem/relebactam and meropenem/RPX7009). New developments can also be observed among oxazolidinones (tedizolid, radezolid, cadazolid and MRX-I), macrolides/ketolides (modithromycin and solithromycin), aminoglycosides (plazomicin), quinolones (nemonoxacin, delafloxacin and avarofloxacin), tetracyclines (omadacycline and eravacycline) as well as among glycopeptides and lipopeptides (oritavancin, telavancin, dalbavancin and surotomycin). New agents in a very early developmental phase are FabI inhibitors, endolysines, peptidomimetics, lipid A inhibitors, methionyl-tRNA synthetase inhibitors and teixobactin.

摘要

在经历了数年的停滞之后,抗菌药物领域出现了几项新的成功进展。这些新进展大多属于传统抗菌类别。β-内酰胺类药物中的新药有对耐甲氧西林金黄色葡萄球菌(MRSA)有效的头孢菌素(头孢洛林和头孢比普)以及β-内酰胺与β-内酰胺酶抑制剂的新组合(头孢托罗/他唑巴坦、头孢他啶/阿维巴坦、亚胺培南/瑞来巴坦和美罗培南/RPX7009)。恶唑烷酮类(特地唑胺、瑞地唑胺、卡地唑胺和MRX-I)、大环内酯类/酮内酯类(莫地霉素和索利霉素)、氨基糖苷类(普拉佐米星)、喹诺酮类(奈诺沙星、德拉沙星和阿伐沙星)、四环素类(奥玛环素和依拉环素)以及糖肽类和脂肽类(奥利万星、替考拉宁、达巴万星和舒罗霉素)中也有新进展。处于非常早期研发阶段的新药物有FabI抑制剂、内溶素、肽模拟物、脂质A抑制剂、甲硫氨酰-tRNA合成酶抑制剂和替加环素。

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