Shirasawa Hiromichi, Nagino Kenji
Pfizer Japan Inc. Clinical Research Department, Tokyo, Japan.
Nihon Ishinkin Gakkai Zasshi. 2005;46(4):223-8. doi: 10.3314/jjmm.46.223.
Voriconazole (VRCZ) is an azole-class antifungal agent with a broad spectrum. VRCZ shows high antifungal activity to Candida spp. including fluconazole less-susceptible species., Aspergillus spp. and Cryptococcus spp. VRCZ shows fungicidal activity to Aspergillus spp. In addition, voriconazole shows activity to rare pathogens like Fusarium spp. or Scedosporium spp. VRCZ is available in both IV and oral formulation. The oral formulation shows stable and almost 100% bioavailability. The protein binding ratio is approximately 58% and over 40% exists as unbound form. VRCZ shows a good tissue distribution including brain and CSF. Outside Japan, several RCTs were conducted for the treatment of deep seated mycosis. The results show a very good drug profile superior to the existing antifungal agents. VRCZ was approved by the FDA and EMEA in 2002. As of September 2004, it has been approved in over 50 countries worldwide.
伏立康唑（VRCZ）是一种具有广谱抗菌活性的唑类抗真菌药物。VRCZ对念珠菌属，包括对氟康唑敏感性较低的念珠菌属、曲霉菌属和隐球菌属均表现出较高的抗真菌活性。VRCZ对曲霉菌属具有杀菌活性。此外，伏立康唑对镰刀菌属或赛多孢子菌属等罕见病原体也有活性。VRCZ有静脉注射和口服两种剂型。口服剂型显示出稳定且几乎100%的生物利用度。蛋白结合率约为58%，超过40%以未结合形式存在。VRCZ在包括脑和脑脊液在内的组织中分布良好。在日本以外，进行了多项治疗深部真菌病的随机对照试验（RCT）。结果显示其药物特性非常好，优于现有的抗真菌药物。VRCZ于2002年获得美国食品药品监督管理局（FDA）和欧洲药品管理局（EMEA）批准。截至2004年9月，它已在全球50多个国家获得批准。
