Pettit Natasha N, Carver Peggy L
University of Chicago Medicine, University of Chicago Medical Center, Chicago, IL, USA.
University of Michigan College of Pharmacy, Ann Arbor, MI, USA University of Michigan Health System, Ann Arbor, MI, USA
Ann Pharmacother. 2015 Jul;49(7):825-42. doi: 10.1177/1060028015581679. Epub 2015 May 4.
To review the pharmacology, chemistry, in vitro susceptibility, pharmacokinetics, clinical efficacy, safety, tolerability, dosage, and administration of isavuconazole, a triazole antifungal agent.
Studies and reviews were identified through an English language MEDLINE search (1978 to March 2015) and from http://www.clinicaltrials.gov, Food and Drug Administration (FDA) briefing documents, program abstracts from international symposia, and the manufacturer's Web site.
All published and unpublished trials, abstracts, in vitro and preclinical studies, and FDA briefing documents were reviewed.
Isavuconazole has activity against a number of clinically important yeasts and molds, including Candida spp, Aspergillus spp, Cryptococcus neoformans, and Trichosporon spp and variable activity against the Mucorales. Isavuconazole, available for both oral and intravenous administration, is characterized by slow elimination allowing once-daily dosing, extensive tissue distribution, and high (>99%) protein binding. The most commonly reported adverse events, which are mild and limited in nature, include nausea, diarrhea, and elevated liver function tests. Its drug interaction potential appears to be similar to other azole antifungals but less than those observed with voriconazole. Comparative trials are under way or have been recently completed for the treatment of candidemia, invasive candidiasis and aspergillosis, and rare mold infections.
Isavuconazole has a broad spectrum of activity and favorable pharmacokinetic properties, providing an advantage over other currently available broad-spectrum azole antifungals and a clinically useful alternative to voriconazole for the treatment of invasive aspergillosis. It may also prove useful for the treatment of candidemia and invasive mold infections; however, these indications await the results of clinical trials.
综述三唑类抗真菌药物艾沙康唑的药理学、化学性质、体外敏感性、药代动力学、临床疗效、安全性、耐受性、剂量及给药方式。
通过检索英文MEDLINE数据库（1978年至2015年3月）、美国国立医学图书馆临床试验数据库（http://www.clinicaltrials.gov）、美国食品药品监督管理局（FDA）简报文件、国际研讨会会议摘要以及药品生产商网站获取相关研究和综述。
对所有已发表和未发表的试验、摘要、体外及临床前研究以及FDA简报文件进行了综述。
艾沙康唑对多种临床上重要的酵母菌和霉菌具有活性，包括念珠菌属、曲霉属、新型隐球菌和毛孢子菌属，对毛霉目真菌的活性各异。艾沙康唑有口服和静脉注射两种剂型，其特点是消除缓慢，允许每日给药一次，组织分布广泛，蛋白结合率高（>99%）。最常报告的不良事件性质轻微且有限，包括恶心、腹泻和肝功能检查指标升高。其药物相互作用潜力似乎与其他唑类抗真菌药相似，但低于伏立康唑。目前正在进行或最近已完成针对念珠菌血症、侵袭性念珠菌病和曲霉病以及罕见霉菌感染治疗的对比试验。
艾沙康唑具有广泛的活性和良好的药代动力学特性，相较于其他现有的广谱唑类抗真菌药具有优势，是治疗侵袭性曲霉病的一种临床上有用的替代伏立康唑的药物。它可能对念珠菌血症和侵袭性霉菌感染的治疗也有用；然而，这些适应证尚需临床试验结果验证。
