Caspofungin Acetate, a member of echinocandins, is a lipopeptide anti-fungal compound targeting Aspergillus and Candida by inhibiting β(1,3)-D-Glucan synthase of the fungal cell wall[1]. Caspofungin Acetate has both fungistatic and fungicidal effects by inhibiting the synthesis of β(1,3)-D-glucan in a non-competitive manner, suppressing the proliferation of fungus and causing cell destruction[2]. Caspofungin Acetate has been approved as an anti-fungal drug named Cancidas by the FDA(2001, USA), EMA(2001, EU), and PMDA (2012, Japan)[2].
In vitro, Caspofungin Acetate kills growing cells of Aspergillus fumigatus (0.2 μg/ml; 15h)[1], and against Candida auris planktonic cells and biofilms (0.03 to 2mg/L; 48h)[3]. Caspofungin Acetate-induced β(1,3)-glucan exposure in Candida albicans is driven by increased chitin levels (46.9ng/mL; 30min)[4]. Caspofungin Acetate is also widely tested combined with other compounds such as voriconazole (0.03-4μg/ml)[5] and fluconazole(0.25 or 0.5MIC)[6].
In vivo, the Caspofungin Acetate activity against Candida glabrata biofilms (10mg/kg; i.p) is tested by bioluminescence imaging in BALB/c mice[7], and in vivo efficiency of Caspofungin Acetat is also tested (3mg/kg; i.p) in a neutropenic mouse bloodstream infection model[8].
References:
[1] Bowman, J C et al. “The antifungal echinocandin caspofungin acetate kills growing cells of Aspergillus fumigatus in vitro.” *Antimicrobial agents and chemotherapy* vol. 46,9 (2002): 3001-12. doi:10.1128/AAC.46.9.3001-3012.2002
[2] Hashemian SM, Farhadi T, Velayati AA. Caspofungin: a review of its characteristics, activity, and use in intensive care units. Expert Rev Anti Infect Ther. 2020 Dec;18(12):1213-1220. doi: 10.1080/14787210.2020.1794817. Epub 2020 Jul 23. PMID: 32662712.
[3] Nagy, Fruzsina et al. “In vitro and in vivo interaction of caspofungin with isavuconazole against Candida auris planktonic cells and biofilms.” *Medical mycology*vol. 59,10 (2021): 1015-1023. doi:10.1093/mmy/myab032
[4] Wagner, Andrew S et al. “Caspofungin-induced β(1,3)-glucan exposure in *Candida albicans* is driven by increased chitin levels.” *mBio* vol. 14,4 (2023): e0007423. doi:10.1128/mbio.00074-23
[5] Perea, Sofia et al. “In vitro interaction of caspofungin acetate with voriconazole against clinical isolates of Aspergillus spp.” *Antimicrobial agents and chemotherapy* vol. 46,9 (2002): 3039-41. doi:10.1128/AAC.46.9.3039-3041.2002
[6] Pesee, Siripen et al. “In vitro activity of Caspofungin combined with Fluconazole on mixed Candida albicans and Candida glabrata biofilm.” *Medical mycology* vol. 54,4 (2016): 384-93. doi:10.1093/mmy/myv108
[7] Persyn, Aranka et al. “Monitoring of Fluconazole and Caspofungin Activity against *In Vivo* Candida glabrata Biofilms by Bioluminescence Imaging.” *Antimicrobial agents and chemotherapy* vol. 63,2 e01555-18. 29 Jan. 2019, doi:10.1128/AAC.01555-18
Balázsi, Dávid et al. “In Vivo Efficacy of Rezafungin, Anidulafungin, Caspofungin, and Micafungin against Four *Candida auris* Clades in a Neutropenic Mouse Bloodstream Infection Model.” *Journal of fungi (Basel, Switzerland)* vol. 10,9 617. 29 Aug. 2024, doi:10.3390/jof10090617
Caspofungin Acetate是棘白菌素（echinocandins）成员，是一种通过抑制真菌细胞壁β(1,3)- d -葡聚糖合成酶而靶向曲霉和念珠菌的脂肽类抗真菌化合物[1]。Caspofungin Acetate通过非竞争方式抑制β(1,3)- d -葡聚糖的合成，抑制真菌的增殖并引起细胞破坏，具有抑菌和杀真菌双重作用[2]。Caspofungin Acetate（商品名Cancidas）已被FDA（2001年，美国）、EMA（2001年，欧盟）和PMDA（2012年，日本）批准为抗真菌药物[2]。
体外实验中，Caspofungin Acetate对Aspergillus fumigatus（0.2μg/ml; 15h）具有杀伤作用[1]，对Candida auris细胞和生物膜（0.03~2 mg/L; 48h）具有杀伤作用[3]。Caspofungin Acetate诱导的β(1,3)-葡聚糖暴露在白色念珠菌中是由几丁质水平升高（46.9 ng/mL; 30min）引起的[4]。Caspofungin Acetate也广泛与伏立康唑（0.03~4μg/ml）[5]和氟康唑（0.25~0.5MIC）[6]等其它化合物联合试验。
在体内实验中，通过生物发光成像检测Caspofungin Acetate对光念珠菌生物膜（10 mg/kg; i.p）的活性[7]，并在中性粒细胞减少小鼠血流感染模型中检测Caspofungin Acetate（3mg/kg; i.p）的体内效率[8]。