抗真菌药物艾沙康唑研究进展

发布时间：2018-05-04 22:30

本文选题：艾沙康唑 + 体外抗真菌活性　；参考：《中国新药杂志》2015年03期

【摘要】：艾沙康唑是一种新的三唑类广谱抗真菌药,已被美国FDA授予快速审批资格、合格传染病产品资格认定和孤儿药地位认定。体外研究显示,艾沙康唑具有广谱抗真菌作用,包括酵母菌(如念珠菌属)和霉菌(如曲霉属、毛霉属)。艾沙康唑以水溶性前药(isavuconazonium sulfate)的形式静脉注射或口服给药,其半衰期较长(静脉注射为76~104 h和口服为56~77 h),仅需每日给药1次。一项治疗侵袭性曲霉菌病的III期临床试验显示,艾沙康唑的疗效不劣于伏立康唑,艾沙康唑治疗相关的肝胆、皮肤以及眼部等器官紊乱的不良反应发生率明显少于伏立康唑。艾沙康唑分子中含有两个手性中心,目前已有多篇文献报道了相关合成方法。本文综述了艾沙康唑的体外抗菌活性、药动学、临床研究以及化学合成研究进展。
[Abstract]:Isa Con is a new three azole broad-spectrum antifungal agent, which has been granted rapid approval qualification, qualification of qualified infectious disease products and status identification of orphan drugs. In vitro studies have shown that isazazol has a broad spectrum of antifungal effects, including yeast (such as Candida) and fungi (aspergillus, Mucor). Alasconazole is water-soluble. The prodrug (isavuconazonium sulfate) is administered intravenously or orally, with a longer half life (intravenous injection of 76~104 h and oral 56~77 h), only 1 times a day. A III phase clinical trial for the treatment of invasive aspergillosis shows that the curative effect of estazazol is not inferior to voriconazole, and isazazol is treated with the associated hepatobiliary and skin. The incidence of adverse reactions in skin and eye disorders is significantly less than voriconazole. There are two chiral centers in the isopazolazole molecule, and many literature has reported related synthesis methods. In this paper, the in vitro antibacterial activity, pharmacokinetics, clinical research and chemical synthesis of alisazolazole are reviewed.

【作者单位】：江苏奥赛康药业股份有限公司;
【分类号】：R978.1

【共引文献】