Mycology Department, Centro Nacional de Microbiologia, Instituto de Salud Carlos III (ISCIII), Carretera Majadahonda-Pozuelo Km2, Majadahonda, 28220, Madrid, Spain.
Drugs. 2017 Apr;77(6):599-613. doi: 10.1007/s40265-017-0714-4.
Aspergillus species are ubiquitous fungal saprophytes found in diverse ecological niches worldwide. Among them, Aspergillus fumigatus is the most prevalent and is largely responsible for the increased incidence of invasive aspergillosis with high mortality rates in some immunocompromised hosts. Azoles are the first-line drugs in treating diseases caused by Aspergillus spp. However, increasing reports in A. fumigatus azole resistance, both in the clinical setting and in the environment, are threatening the effectiveness of clinical and agricultural azole drugs. The azole target is the 14-α sterol demethylase encoded by cyp51A gene and the main mechanisms of resistance involve the integration of tandem repeats in its promoter and/or single point mutations in this gene. In A. fumigatus, azole resistance can emerge in two different scenarios: a medical route in which azole resistance is generated during long periods of azole treatment in the clinical setting and a route of resistance derived from environmental origin due to extended use of demethylation inhibitors in agriculture. The understanding of A. fumigatus azole resistance development and its evolution is needed in order to prevent or minimize its impact. In this article, we review the current situation of azole resistance epidemiology and the predominant molecular mechanisms described based on the resistance acquisition routes. In addition, the clinical implications of A. fumigatus azole resistance and future research are discussed.
曲霉菌属是一种广泛存在的真菌腐生生物,分布于世界各地的各种生态位。其中,烟曲霉是最常见的一种,也是导致某些免疫功能低下宿主侵袭性曲霉菌病发病率增加和死亡率升高的主要原因。唑类药物是治疗曲霉菌属引起的疾病的一线药物。然而,越来越多的报告表明,烟曲霉对唑类药物的耐药性,无论是在临床环境还是在环境中,都威胁着临床和农业唑类药物的有效性。唑类药物的靶标是由 cyp51A 基因编码的 14-α 甾醇去甲基酶,主要的耐药机制包括其启动子中的串联重复整合和/或该基因中的单点突变。在烟曲霉中,唑类耐药性可以在两种不同的情况下出现:一种是在临床环境中长时间使用唑类药物治疗时产生的医疗途径,另一种是由于农业中广泛使用去甲基化抑制剂而产生的耐药性源于环境的途径。为了预防或最小化其影响,需要了解烟曲霉唑类耐药性的发展及其进化。本文综述了唑类耐药性的流行病学现状和基于耐药获得途径描述的主要分子机制。此外,还讨论了烟曲霉唑类耐药性的临床意义和未来研究方向。