Frampton James E, Scott Lesley J
Wolters Kluwer Health, Adis, Auckland, New Zealand.
Drugs. 2008;68(7):993-1016. doi: 10.2165/00003495-200868070-00008.
Posaconazole is a second-generation triazole antifungal agent with a broad spectrum of activity that includes Aspergillus spp., Candida spp. and the Zygomycetes. In the US, posaconazole oral suspension administered three times daily is indicated for prophylaxis against invasive Aspergillus and Candida infections in patients aged > or =13 years who are at high risk of developing these infections because of immunosuppression, such as haematopoietic stem cell transplant (HSCT) recipients with graft-versus-host disease (GVHD), or those with haematological malignancies with prolonged neutropenia as a result of chemotherapy. EU-approved prophylactic indications for posaconazole are similar to those in the US. Posaconazole provided effective prophylaxis against invasive fungal infections and was generally well tolerated in two large, well designed trials in HSCT recipients with GVHD, or patients receiving induction-remission chemotherapy for acute myeloid leukaemia (AML) or myelodysplastic syndrome (MDS) that was expected to result in prolonged neutropenia. It offers coverage of clinically relevant pathogens and is potentially associated with fewer drug-drug interactions than other licensed triazole antifungal agents. Its usefulness in some patients may be limited by the lack of an intravenous formulation, although one is currently being developed. As with other antifungal agents, concerns remain regarding the potential emergence of resistance to broad-spectrum antifungal prophylaxis with posaconazole. Despite this, posaconazole is a valuable emerging option for use as prophylaxis against invasive fungal infections in immunocompromized patients who are at high risk of developing these infections.
泊沙康唑是一种第二代三唑类抗真菌药物,具有广泛的活性谱,包括曲霉属、念珠菌属和接合菌纲。在美国,对于年龄≥13岁、因免疫抑制而有发生侵袭性曲霉和念珠菌感染高风险的患者,如患有移植物抗宿主病(GVHD)的造血干细胞移植(HSCT)受者,或因化疗导致长期中性粒细胞减少的血液系统恶性肿瘤患者,每日口服三次的泊沙康唑口服混悬液可用于预防侵袭性曲霉和念珠菌感染。泊沙康唑在欧盟获批的预防适应症与美国相似。在两项针对患有GVHD的HSCT受者,或接受急性髓系白血病(AML)或骨髓增生异常综合征(MDS)诱导缓解化疗且预计会导致长期中性粒细胞减少的患者进行的大型、设计良好的试验中,泊沙康唑有效预防了侵袭性真菌感染,且总体耐受性良好。它能覆盖临床相关病原体,与其他已获许可的三唑类抗真菌药物相比,潜在的药物相互作用较少。尽管目前正在研发静脉制剂,但在一些患者中其应用可能因缺乏静脉制剂而受到限制。与其他抗真菌药物一样,对于泊沙康唑广谱抗真菌预防可能出现耐药性的问题仍存在担忧。尽管如此,对于有发生侵袭性真菌感染高风险的免疫功能低下患者,泊沙康唑作为预防此类感染的药物是一个有价值的新选择。