Origin, structure, and activity in vitro and in vivo of dalbavancin
Origin, structure, and activity in vitro and in vivo of dalbavancin
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DOI：
10.1093/jac/dki005
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发表时间：
2005-03-01
影响因子：
5.2
通讯作者：
Goldstein, BP
中科院分区：
文献类型：
--
作者：
Malabarba, A;Goldstein, BP
达巴万星是一种新型半合成脂糖肽，旨在改善目前可用的天然糖肽万古霉素和替考拉宁。天然糖肽的化学修饰产生了具有更强抗菌活性和更长t（1/2）的化合物，同时保持了优异的安全性。从替考拉宁样糖肽制备的达巴万星在体外和动物感染模型中的活性优于万古霉素和替考拉宁。特别地，达巴霉素对葡萄球菌（包括凝固酶阴性的葡萄球菌）具有优异的活性。达巴霉素的独特特征是其药代动力学，其特征在于在人体中的长消除t（1/2），这使得每周一次给药方案可行。达巴万星最近完成了皮肤和皮肤结构感染的3期临床试验。
Dalbavancin is a novel semi-synthetic lipoglycopeptide that was designed to improve upon the natural glycopeptides currently available, vancomycin and teicoplanin. Chemical modification of natural glycopeptides has produced compounds with more potent antimicrobial activity and longer t(1/2), while maintaining an excellent safety profile. Dalbavancin, prepared from a teicoplanin-like glycopeptide, has better activity, in vitro and in animal infection models, than vancomycin and teicoplanin. In particular, dalbavancin has excellent activity against staphylococci, including coagulase-negatives. A unique feature of dalbavancin is its pharmacokinetics, characterized by a long elimination t(1/2) in humans which makes a once-weekly dosing regimen feasible. Dalbavancin recently completed Phase 3 clinical trials in skin and skin structure infection.