Maschmeyer Georg, Glasmacher Axel
Abt. Hämatologie und Onkologie, Medizinische Klinik, Klinikum Ernst von Bergmann, Potsdam, Germany.
Mycoses. 2005 Jul;48(4):227-34. doi: 10.1111/j.1439-0507.2005.01131.x.
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.
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。