Van Bambeke Françoise
Université catholique de Louvain, Unité de Pharmacologie cellulaire et moléculaire, UCL 7370, Avenue Mounier 73, 1200 Brussels, Belgium.
Curr Opin Investig Drugs. 2006 Aug;7(8):740-9.
Hemi-synthetic derivatives of glycopeptides have demonstrated bactericidal activity towards Gram-positive bacteria, including vancomycin-resistant strains (oritavancin and telavancin), and a prolonged half-life, allowing for once-daily (oritavancin and telavancin) or once-weekly (dalbavancin) administration. These compounds have proved effective for the treatment of infections caused by multidrug-resistant Gram-positive bacteria, including complicated skin and skin structure infections (oritavancin, telavancin and dalbavancin), bacteremia (oritavancin and dalbavancin) and nosocomial pneumonia. This review compares the antibacterial activity and clinical activity of three glycopeptides, oritavancin, telavancin and dalbavancin, and the natural lipoglycopeptide, ramoplanin, which, being unstable in the bloodstream, is administered orally to treat Clostridium difficile colitis and for digestive tract decontamination. All of these compounds, with the exception of oritavancin, have received Fast Track designation from the FDA because of their clinical efficacy.
糖肽类半合成衍生物已显示出对革兰氏阳性菌具有杀菌活性，包括耐万古霉素菌株（奥利万星和替考拉宁），且半衰期延长，可每日一次（奥利万星和替考拉宁）或每周一次（达巴万星）给药。这些化合物已被证明对治疗由多重耐药革兰氏阳性菌引起的感染有效，包括复杂性皮肤及皮肤结构感染（奥利万星、替考拉宁和达巴万星）、菌血症（奥利万星和达巴万星）及医院获得性肺炎。本综述比较了三种糖肽类药物奥利万星、替考拉宁和达巴万星以及天然脂糖肽类药物雷莫拉宁的抗菌活性和临床活性，雷莫拉宁在血液中不稳定，口服用于治疗艰难梭菌性结肠炎和进行消化道去污。除奥利万星外，所有这些化合物因其临床疗效均已获得美国食品药品监督管理局的快速通道指定。
