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Drugs. 2019 Feb;79(3):315-324. doi: 10.1007/s40265-019-01067-3.
Eravacycline (Xerava™), a novel fully synthetic fluorocycline, consists of the tetracyclic core scaffold with unique modifications in the tetracyclic D ring; consequently, it exhibits potent in vitro activity against Gram-positive and -negative bacterial strains expressing certain common tetracycline-specific acquired resistance mechanisms. In vitro, eravacycline exhibits potent activity against a broad spectrum of clinically relevant Gram-positive and -negative aerobic and anaerobic bacteria. Intravenous eravacycline is approved in several countries for the treatment of complicated intra-abdominal infections (cIAIs) in adult patients. In two pivotal double-blind, multinational trials in this patient population, eravacycline (infusion ≈ 1 h) was noninferior to intravenous ertapenem or meropenem at the test-of-cure visit in terms of clinical response rates in all prespecified populations. Eravacycline had an acceptable tolerability profile, with infusion site reactions, nausea, vomiting and diarrhoea the most commonly reported adverse reactions, most of which were of mild to moderate severity. Given its broad spectrum of activity against common clinically relevant pathogens (including those expressing certain tetracycline- and other antibacterial-specific acquired resistance mechanisms) and its more potent in vitro activity and better tolerability profile than tigecycline, eravacycline provides a novel emerging option for the treatment of adult patients with cIAIs, especially as empirical therapy when coverage of resistant pathogens is required.
依拉环素(XeravaTM),一种新型全合成氟环素,由四环核心支架组成,在四环 D 环上进行了独特的修饰;因此,它对表达某些常见四环素特异性获得性耐药机制的革兰氏阳性和阴性细菌菌株具有强大的体外活性。体外,依拉环素对广谱临床相关的革兰氏阳性和阴性需氧和厌氧细菌具有强大的活性。静脉用依拉环素已在多个国家获得批准,用于治疗成人复杂腹腔内感染(cIAIs)。在该患者人群中进行的两项关键性、双盲、多中心试验中,依拉环素(输注≈1 小时)在治愈期访视时在所有预设人群中的临床应答率方面与静脉用厄他培南或美罗培南无差异。依拉环素具有可接受的耐受性,输注部位反应、恶心、呕吐和腹泻是最常见的不良反应,大多数为轻度至中度严重程度。鉴于其对常见临床相关病原体(包括表达某些四环素和其他抗菌特异性获得性耐药机制的病原体)具有广泛的活性,以及其比替加环素更强的体外活性和更好的耐受性,依拉环素为治疗成人复杂腹腔内感染提供了一种新的治疗选择,尤其是在需要覆盖耐药病原体时作为经验性治疗。