Cubist Pharmaceuticals, Inc. 65 Hayden Avenue, Lexington, MA 02421, USA +1 781 860 8310 ; +1 781 860 1110 ;
Expert Opin Drug Discov. 2007 Nov;2(11):1523-36. doi: 10.1517/17460441.2.11.1523.
Gram-positive bacteria such as Staphylococcus aureus are important human pathogens. An increasing proportion of S. aureus are methicillin resistant. For decades, methicillin-resistant S. aureus infections have been treated with vancomycin, but susceptibility is decreasing, and tissue penetration and safety profile (especially nephrotoxicity) is not ideal. Consequently, there is a great need for the development of antibiotics with demonstrated efficacy and safety for infections caused by S. aureus and other Gram-positive pathogens. One such antibiotic is daptomycin, which has a unique mechanism of action and potent, rapid bactericidal activity, without causing cell lysis. Daptomycin has demonstrated significant efficacy in the treatment of complicated skin and skin structure infections, as well as methicillin-susceptible and methicillin-resistant S. aureus bacteremia, including right-sided endocarditis. Other attributes include an excellent safety profile, low potential for resistance, and once-daily dosing.
革兰氏阳性菌，如金黄色葡萄球菌，是重要的人类病原体。耐甲氧西林金黄色葡萄球菌的比例在不断增加。几十年来，耐甲氧西林金黄色葡萄球菌感染一直用万古霉素治疗，但敏感性正在下降，组织穿透性和安全性（特别是肾毒性）并不理想。因此，迫切需要开发具有良好疗效和安全性的抗生素，用于治疗金黄色葡萄球菌和其他革兰氏阳性病原体引起的感染。达托霉素就是这样一种抗生素，它具有独特的作用机制和强大、快速的杀菌活性，而不会导致细胞裂解。达托霉素在治疗复杂性皮肤和皮肤结构感染以及耐甲氧西林敏感和耐甲氧西林金黄色葡萄球菌菌血症方面具有显著疗效，包括右侧心内膜炎。其他特点包括安全性良好、耐药潜力低以及每日一次给药。
