新型头孢菌素类抗生素ceftobiprole

A first-in-class anti-MRSA broad-spectrum cephalosporin: Ceftobiprole

抗生素滥用导致的多重耐药菌株的出现,限制了临床常规抗生素的使用范围,使严重的院内感染难以得到控制。Ceftobiprole是最新研制出的惟一对耐甲氧西林金葡菌有效的头孢菌素类抗生素。现对其研发现况、作用机制、体内外抗菌活性以及临床应用等方面做一综述。

The occurrence of multidrug resistant strains closely associated with abuse of antibiotics narrows the clinical option of common antibiotics, and makes the hospital-acquired infections refractory. Ceftobiprole is the first of a new class of broad-spectrum anti-MSRA cephalosporin antibiotics that was specially designed to bind to the penicillin-resistant targets in Gram-positive cocci, resulting in potent bactericidal activity towards methicillin-resistant Staphylococcus aureus （MRSA） and penicillin-resistant Streptococcus pneumoniae （PRSP）. Ceftobiprole not only has a broad-spectrum profile targeting other Gram-positive as well as Gram-negative pathogens, but has also shown a low potential to induce resistance in vitro. This review detailed its newest research status, mechanism of action, antibacterial activities in vitro and in vivo and ongoing clinical trials.