Department of medicine, St John Hospital and Medical Center, Wayne State University School of Medicine, East Lansing, Michigan, USA.
Clin Infect Dis. 2011 May;52(9):1156-63. doi: 10.1093/cid/cir147.
Ceftaroline (PPI 0903, formerly TAK-599), the active metabolite of a N-phosphono prodrug, ceftaroline fosamil, has been approved by the US Food and Drug Administration for the treatment of acute bacterial skin and skin structure infections and community-acquired bacterial pneumonia. This antimicrobial agent binds to penicillin binding proteins (PBP) inhibiting cell wall synthesis and has a high affinity for PBP2a, which is associated with methicillin resistance. Ceftaroline is consistently active against multidrug-resistant Streptococcus pneumoniae and Staphylococcus aureus, including methicillin-resistant, vancomycin-intermediate, linezolid-resistant, and daptomycin-nonsusceptible strains. It possesses variable activity against Enterobacteriaceae and good activity against oral anaerobes. The drug is usually administrated intravenously at 600 mg every 12 h. Ceftaroline has low protein binding and is excreted by the kidneys and thus requires dose adjustments in individuals with renal failure. Clinical trials have demonstrated noninferiority when compared with vancomycin in the treatment of acute bacterial skin and skin structure infections and noninferiority when compared with ceftriaxone in the treatment of community-acquired bacterial pneumonia. Ceftaroline demonstrated a safety profile similar to that of comparator drugs in clinical trials.
头孢洛林（PPI 0903，前身为 TAK-599）是 N-膦酸酯前药头孢洛林磷酸二酰胺的活性代谢物，已获美国食品和药物管理局批准用于治疗急性细菌性皮肤和皮肤结构感染和社区获得性细菌性肺炎。这种抗菌药物与青霉素结合蛋白（PBP）结合，抑制细胞壁合成，对与耐甲氧西林相关的 PBP2a 具有高亲和力。头孢洛林对多种耐药性肺炎链球菌和金黄色葡萄球菌始终具有活性，包括耐甲氧西林、万古霉素中介、利奈唑胺耐药和达托霉素不敏感株。它对肠杆菌科具有可变的活性，对口腔厌氧菌具有良好的活性。该药通常每 12 小时静脉注射 600mg。头孢洛林的蛋白结合率低，主要经肾脏排泄，因此在肾功能衰竭患者中需要调整剂量。临床试验表明，头孢洛林在治疗急性细菌性皮肤和皮肤结构感染方面与万古霉素相比非劣效，在治疗社区获得性细菌性肺炎方面与头孢曲松相比非劣效。头孢洛林在临床试验中的安全性与对照药物相似。
