Biology Department, Indiana University, Bloomington, IN 47405, USA.
Curr Opin Pharmacol. 2012 Oct;12(5):527-34. doi: 10.1016/j.coph.2012.06.003. Epub 2012 Jun 28.
New antibiotic agents are desperately needed to treat the multidrug-resistant pathogens that continue to emerge at alarming rates. Many of the agents that have entered full clinical development since 1995 have been members of previously accepted classes of antibiotics. Among these are a new aminoglycoside (plazomicin), anti-MRSA cephalosporins (ceftobiprole and ceftaroline), a monocyclic β-lactam (BAL30072), the β-lactamase inhibitor combination of tazobactam with the anti-pseudomonal cephalosporin ceftolozane, β-lactam combinations with new non-β-lactam inhibitors (MK-7655 with imipenem, and avibactam with ceftazidime and ceftaroline), new macrolides (cethromycin and solithromycin), oxazolidinones (tedizolid phosphate and radezolid), and quinolones (delafloxacin, nemonoxacin and JNJ-Q2). Resistance and safety issues have been circumvented by some of these new agents that have well-established mechanisms of action and defined pathways leading toward regulatory approval.
急需新型抗生素来治疗那些以惊人速度不断出现的耐药病原体。自 1995 年以来，许多已进入全面临床开发阶段的药物都属于先前被认可的抗生素类别。其中包括一种新型氨基糖苷类药物（plazomicin）、抗耐甲氧西林金黄色葡萄球菌（MRSA）头孢菌素（ceftobiprole 和 ceftaroline）、单环β-内酰胺类药物（BAL30072）、β-内酰胺酶抑制剂组合他唑巴坦与抗假单胞菌头孢菌素头孢洛扎烷、具有新型非β-内酰胺抑制剂的β-内酰胺类药物组合（MK-7655 与亚胺培南，以及 avibactam 与头孢他啶和 ceftaroline）、新型大环内酯类药物（cethromycin 和 solithromycin）、恶唑烷酮类（tedizolid 磷酸盐和 radezolid）和喹诺酮类（delafloxacin、nemonoxacin 和 JNJ-Q2）。其中一些新型药物具有明确的作用机制和明确的监管审批途径，从而规避了耐药性和安全性问题。
