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用于治疗侵袭性真菌感染的新型棘白菌素类药物

Emerging echinocandins for treatment of invasive fungal infections.

作者信息

Turner Michelle S, Drew Richard H, Perfect John R

机构信息

Duke University Medical Center, Box 3089, Durham, NC 27710, USA.

出版信息

Expert Opin Emerg Drugs. 2006 May;11(2):231-50. doi: 10.1517/14728214.11.2.231.

Abstract

The echinocandins are a new class of antifungals, developed in response to the need for safe and effective antifungals for the treatment of invasive fungal infections. These agents work by inhibiting 1,3-beta-d-glucan synthase, an enzyme essential for production of cell walls in select fungi. Echinocandins appear to demonstrate favourable activity in vitro against a variety of yeasts (including both Candida albicans and non-albicans Candida) as well as select moulds (including Aspergillus spp.) In general, all echninocandins demonstrate a favourable safety profile and require once-daily parenteral administration. Caspofungin is the first of these agents to be available in the US, and is approved for empirical antifungal therapy in febrile neutropenic patients, candidaemia and select forms of invasive candidiasis, and for management of invasive aspergillosis in patients refractory to or intolerant of other therapies. Micafungin was recently approved by the FDA for treatment of oesophageal candidiasis, and for the prophylaxis of fungal infections in haematopoietic stem cell transplant recipients. Emerging data indicate micafungin may have an important role in the treatment of invasive forms of candidiasis. Anidulafungin is an echinocandin approved in the US for treatment of candidaemia and oesophageal candidiasis. Aminocandin (HMR-3702, IP-960) is an investigational agent, with published experience limited to in vitro studies and animal models of infection.

摘要

棘白菌素类是一类新型抗真菌药物,是为满足治疗侵袭性真菌感染所需的安全有效的抗真菌药物而研发的。这些药物通过抑制1,3-β-D-葡聚糖合成酶发挥作用,该酶是某些真菌细胞壁生成所必需的一种酶。棘白菌素类在体外对多种酵母菌(包括白色念珠菌和非白色念珠菌)以及某些霉菌(包括曲霉属)似乎都具有良好的活性。一般来说,所有棘白菌素类都具有良好的安全性,且需要每日一次胃肠外给药。卡泊芬净是这类药物中首个在美国上市的药物,被批准用于发热性中性粒细胞减少患者的经验性抗真菌治疗、念珠菌血症和某些侵袭性念珠菌病,以及用于对其他治疗难治或不耐受的患者的侵袭性曲霉病的治疗。米卡芬净最近被美国食品药品监督管理局批准用于治疗食管念珠菌病,以及预防造血干细胞移植受者的真菌感染。新出现的数据表明米卡芬净在侵袭性念珠菌病的治疗中可能发挥重要作用。阿尼芬净是一种在美国被批准用于治疗念珠菌血症和食管念珠菌病的棘白菌素。氨苯芬净(HMR-3702,IP-960)是一种研究性药物,已发表的经验仅限于体外研究和感染动物模型。

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