Infectious Disease Center for Excellence in Drug Discovery, GlaxoSmithKline, Collegeville, PA, USA;
Ther Clin Risk Manag. 2009 Feb;5(1):41-9. doi: 10.2147/tcrm.s3459. Epub 2009 Mar 26.
Retapamulin is a novel semisynthetic pleuromutilin antibiotic specifically designed for use as a topical agent. The unique mode of action by which retapamulin selectively inhibits bacterial protein synthesis differentiates it from other nonpleuromutilin antibacterial agents that target the ribosome or ribosomal factors, minimizing the potential for target-specific cross-resistance with other antibacterial classes in current use. In vitro studies show that retapamulin has high potency against the Gram-positive bacteria (Staphylococcus aureus, Streptococcus pyogenes, and coagulase-negative staphylococci) commonly found in skin and skin-structure infections (SSSIs), including S. aureus strains with resistance to agents such as macrolides, fusidic acid, or mupirocin, and other less common organisms associated with SSSIs, anaerobes, and common respiratory tract pathogens. Clinical studies have shown that twice-daily topical retapamulin for 5 days is comparable to 10 days of oral cephalexin in the treatment of secondarily infected traumatic lesions. A 1% concentration of retapamulin ointment has been approved for clinical use as an easily applied treatment with a short, convenient dosing regimen for impetigo. Given the novel mode of action, low potential for cross-resistance with established antibacterial agents, and high in vitro potency against many bacterial pathogens commonly recovered from SSSIs, retapamulin is a valuable enhancement over existing therapeutic options.
瑞他帕林是一种新型半合成截短侧耳素抗生素，专门设计用作局部药物。瑞他帕林通过选择性抑制细菌蛋白质合成的独特作用方式将其与其他非截短侧耳素类抗菌药物区分开来，这些药物的作用靶点是核糖体或核糖体因子，从而最大限度地减少与目前使用的其他抗菌药物类别产生针对特定目标的交叉耐药性的可能性。体外研究表明，瑞他帕林对常见于皮肤和皮肤结构感染（SSSIs）的革兰氏阳性菌（金黄色葡萄球菌、化脓性链球菌和凝固酶阴性葡萄球菌）具有高活性，包括对大环内酯类、夫西地酸或莫匹罗星等药物耐药的金黄色葡萄球菌菌株，以及与 SSSIs 相关的其他不太常见的生物体、厌氧菌和常见的呼吸道病原体。临床研究表明，每日两次局部使用瑞他帕林 5 天与口服头孢氨苄 10 天治疗继发感染的创伤性病变相当。1%浓度的瑞他帕林软膏已被批准用于临床，作为一种易于应用的治疗方法，具有较短、方便的给药方案，适用于脓疱疮。鉴于其新颖的作用方式、与已建立的抗菌药物交叉耐药的潜力低，以及对许多从 SSSIs 中恢复的常见细菌病原体的高体外活性，瑞他帕林是现有治疗选择的有价值的增强剂。
