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首个棘白菌素类药物:卡泊芬净。

The first echinocandin: caspofungin.

作者信息

Cornely O A, Schmitz Karina, Aisenbrey Sabine

机构信息

Klinik I für Innere Medizin, Klinikum der Universität Köln, 50924 Köln, Germany.

出版信息

Mycoses. 2002;45 Suppl 3:56-60. doi: 10.1111/j.1439-0507.2002.tb04771.x.

Abstract

The antifungal agent caspofungin is the first echinocandin that has been approved in the US and in Europe for treatment of invasive aspergillosis in adult patients who are refractory to or intolerant of conventional amphotericin B, its lipid-based formulations, and/or itraconazole. It is given as a 70 mg loading dose and a 50 mg daily maintainance dose as a one hour infusion. Due to low intestinal absorption an oral formulation has not been developed. Caspofungin is active against Candida spp. and Aspergillus spp. by inhibition the synthesis of beta-(1,3)-D-glucan, a cell wall component. The drug is inactive against Cryptococcus spp., Fusarium spp., Trichosporon spp., Rhizopus spp., and Pseudoallescheria spp. In invasive aspergillosis caspofungin resulted in higher response rates compared to a historic control under standard therapy. Efficacy data on persistently febrile neutropenic patients are pending. In several multicenter randomised double blind trials on candida infections caspofungin proved to be at least non-inferior to standard therapies. Reports of combination therapy or highly effective antifungal treatment (HEAT) in limited patient numbers are promising. New trials of combination therapy are warranted.

摘要

抗真菌药物卡泊芬净是首个在美国和欧洲获批用于治疗侵袭性曲霉病的棘白菌素类药物,适用于对传统两性霉素B、其脂质体制剂和/或伊曲康唑难治或不耐受的成年患者。它的给药方式为70mg负荷剂量,随后每日50mg维持剂量,静脉输注1小时。由于肠道吸收低,尚未开发口服制剂。卡泊芬净通过抑制β-(1,3)-D-葡聚糖(一种细胞壁成分)的合成,对念珠菌属和曲霉属具有活性。该药物对隐球菌属、镰刀菌属、毛孢子菌属、根霉属和拟阿利什菌属无活性。在侵袭性曲霉病中,与标准治疗下的历史对照相比,卡泊芬净的缓解率更高。持续发热性中性粒细胞减少患者的疗效数据尚未确定。在几项关于念珠菌感染的多中心随机双盲试验中,卡泊芬净被证明至少不劣于标准治疗。有限数量患者的联合治疗或高效抗真菌治疗(HEAT)报告很有前景。有必要开展新的联合治疗试验。

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