Letscher-Bru Valérie, Herbrecht Raoul
Institut de Parasitologie et de Pathologie Tropicale, Faculté de Médecine, 3 rue Koeberlé, 67000 Strasbourg, France.
J Antimicrob Chemother. 2003 Mar;51(3):513-21. doi: 10.1093/jac/dkg117.
Caspofungin (MK-0991; L-743,872) belongs to the echinocandin family, a new class of antifungal agents that act on the fungal cell wall by inhibiting glucan synthesis. Data in vitro, and experimental studies, have demonstrated that caspofungin has antifungal activity against yeasts of the genus Candida (including isolates resistant to azoles and amphotericin B), several species of filamentous fungi, including Aspergillus, and certain dimorphic fungi, such as Histoplasma, Blastomyces and Coccidioides. In vitro and in animals, caspofungin shows additive or synergic antifungal activity with amphotericin B and triazoles. It also possesses activity against Pneumocystis carinii. Clinical trials have shown caspofungin to be well tolerated and effective in invasive aspergillosis in patients refractory or intolerant to standard treatment (45% favourable responses), in oropharyngeal and oesophageal candidiasis (67-93% favourable responses with an efficacy similar to those of amphotericin B and fluconazole), and in invasive candidiasis with efficacy equivalent to that of amphotericin B, and better tolerability. The results of these first clinical trials were promising, and led to the approval of caspofungin for invasive aspergillosis after failure of, or intolerance to, standard therapy. Further studies are required to define the exact role of caspofungin in the antifungal armamentarium.
卡泊芬净(MK-0991;L-743,872)属于棘白菌素类,是一类新型抗真菌药物,通过抑制葡聚糖合成作用于真菌细胞壁。体外数据和实验研究表明,卡泊芬净对念珠菌属酵母(包括对唑类和两性霉素B耐药的菌株)、几种丝状真菌(包括曲霉菌)以及某些双相真菌(如组织胞浆菌、芽生菌和球孢子菌)具有抗真菌活性。在体外和动物实验中,卡泊芬净与两性霉素B和三唑类药物显示出相加或协同的抗真菌活性。它对卡氏肺孢子菌也有活性。临床试验表明,卡泊芬净在对标准治疗难治或不耐受的患者的侵袭性曲霉病中耐受性良好且有效(45%有良好反应),在口咽和食管念珠菌病中(67 - 93%有良好反应,疗效与两性霉素B和氟康唑相似),以及在侵袭性念珠菌病中疗效与两性霉素B相当且耐受性更好。这些首批临床试验的结果很有前景,并导致卡泊芬净在标准治疗失败或不耐受后被批准用于侵袭性曲霉病。还需要进一步研究来确定卡泊芬净在抗真菌药物库中的确切作用。