Eisenstein Barry I
Cubist Pharmaceuticals, Lexington, MA, USA.
Expert Opin Investig Drugs. 2004 Sep;13(9):1159-69. doi: 10.1517/13543784.13.9.1159.
The increasing incidence of serious infections caused by antibiotic-resistant Gram-positive bacteria has led to the development of new spectrum-specific agents. One such agent is Cubicin (daptomycin for injection), the first member of a new class of antibacterials called cyclic lipopeptides. Daptomycin has rapid, concentration-dependent bactericidal activity against most clinically significant Gram-positive pathogens, including vancomycin-resistant enterococci, methicillin-resistant Staphylococcus aureus, and vancomycin-intermediate and -resistant S. aureus. This cyclic lipopeptide has a unique mechanism of action and exhibits a relatively prolonged concentration-dependent postantibiotic effect in vitro. In September 2003 the US FDA approved daptomycin for the treatment of complicated skin and skin-structure infections. With its once-daily dosing, excellent safety profile and low potential for resistance, daptomycin is a welcome new addition to the armamentarium against Gram-positive infections.
由耐抗生素革兰氏阳性菌引起的严重感染发病率不断上升，促使新型谱特异性药物得以研发。其中一种药物是 Cubicin（注射用达托霉素），它是一类名为环脂肽的新型抗菌药物中的首个成员。达托霉素对大多数具有临床意义的革兰氏阳性病原体具有快速、浓度依赖性杀菌活性，包括耐万古霉素肠球菌、耐甲氧西林金黄色葡萄球菌以及万古霉素中介和耐药金黄色葡萄球菌。这种环脂肽具有独特的作用机制，且在体外表现出相对较长的浓度依赖性抗生素后效应。2003 年 9 月，美国食品药品监督管理局批准达托霉素用于治疗复杂性皮肤及皮肤结构感染。达托霉素每日给药一次，安全性良好，耐药可能性低，是抗革兰氏阳性感染药物库中一个受欢迎的新成员。
