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一种最近获批的全身性抗真菌药物卡泊芬净的药理特性及临床疗效。

Pharmacological properties and clinical efficacy of a recently licensed systemic antifungal, caspofungin.

作者信息

Maschmeyer Georg, Glasmacher Axel

机构信息

Abt. Hämatologie und Onkologie, Medizinische Klinik, Klinikum Ernst von Bergmann, Potsdam, Germany.

出版信息

Mycoses. 2005 Jul;48(4):227-34. doi: 10.1111/j.1439-0507.2005.01131.x.

Abstract

Caspofungin, a semisynthetic derivative of the pneumocandin B(0), is the first licensed compound of a new class of antifungal agents, the echinocandins. It attacks the fungal cell by selective inhibition of the beta-(1,3)-d-glucan synthase, which is not present in mammalian cells. In vitro studies have indicated a potent fungicidal effect on Candida species, and in vivo studies in immunocompromised animals with invasive candidiasis demonstrated a favourable outcome. In randomized clinical trials in patients with oropharyngeal/oesophageal and invasive candidiasis, caspofungin was at least as effective as amphotericin B deoxycholate, yet showed a significantly superior safety profile. Of patients with invasive aspergillosis refractory to or intolerant of other antifungal agents, 45% showed a partial or complete response to caspofungin given as a salvage treatment. Also, it demonstrated comparable clinical efficacy but superior tolerability in the empirical antifungal therapy in neutropenic patients compared with liposomal amphothericin B. Caspofungin has an excellent tolerability and a low potential for drug interactions. Thus, caspofungin represents an interesting and clinically valuable new antifungal drug that broadens the available therapeutic armamentarium for the treatment of invasive fungal infections.

摘要

卡泊芬净是喷他脒菌素B(0)的半合成衍生物,是一类新型抗真菌药物棘白菌素类中的首个获许可的化合物。它通过选择性抑制β-(1,3)-D-葡聚糖合酶来攻击真菌细胞,而该酶不存在于哺乳动物细胞中。体外研究表明其对念珠菌属具有强大的杀菌作用,在免疫受损的侵袭性念珠菌病动物体内研究显示出良好的效果。在口咽/食管念珠菌病和侵袭性念珠菌病患者的随机临床试验中,卡泊芬净至少与两性霉素B脱氧胆酸盐一样有效,但安全性显著更优。在对其他抗真菌药物难治或不耐受的侵袭性曲霉病患者中,45%的患者接受卡泊芬净挽救治疗后出现部分或完全缓解。此外,在中性粒细胞减少患者的经验性抗真菌治疗中,与脂质体两性霉素B相比,它显示出相当的临床疗效但耐受性更佳。卡泊芬净耐受性良好,药物相互作用的可能性低。因此,卡泊芬净是一种有趣且具有临床价值的新型抗真菌药物,拓宽了治疗侵袭性真菌感染的可用治疗手段。

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