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达托霉素是微生物产生的环状脂肽抗生素,20世纪80年代末由美国礼来公司发现。1997年Cubist制药公司从礼来公司获得了达托霉素的全球独家开发、生产及销售权。经过6年的研发,2003年美国FDA相继批准了Cubicin(达托霉素注射剂)用于治疗成年人由革兰阳性菌(包括耐甲氧西林金黄葡萄球菌与耐万古霉素肠球菌等)所致的复杂性皮肤和软组织感染(cSSSI),以及金葡菌引起的菌血症和右侧心内膜炎,目前尚未批准系统用药。本文总结了达托霉素的研发历程,包括其发现、抗菌活性、临床试验、结构修饰及合成方法等。
Daptomycin is a cyclic lipopeptide antibiotic produced by microorganisms and was discovered by Eli Lilly and Company in the late 1980s. In 1997 Cubist Pharmaceuticals acquired the exclusive worldwide right to develop, manufacture and distribute daptomycin from Eli Lilly and Company. After six years of research and development, in 2003, the U.S. FDA approved Cubicin (daptomycin injections) for the treatment of Gram-positive bacteria (including methicillin-resistant Staphylococcus aureus and vancomycin-resistant enterococci) The resulting complex skin and soft tissue infections (cSSSI), as well as bacteremia and right endocarditis caused by S. aureus, have not been approved for systemic administration. This article summarizes the history of daptomycin research, including its discovery, antibacterial activity, clinical trials, structural modification and synthesis methods.