Ma Jingyi, Eadie Kimberly, Konings Mickey, Fahal Ahmed, Verbon Annelies, van de Sande Wendy W J
Erasmus MC, University Medical Center Rotterdam, Department of Medical Microbiology and Infectious Diseases, Dr. Molewaterplein 40, Rotterdam 3015GD, The Netherlands.
Mycetoma Research Centre, Khartoum, Sudan.
J Antimicrob Chemother. 2025 Apr 30;80(6):1733-41. doi: 10.1093/jac/dkaf133.
Eumycetoma is a neglected tropical fungal disease of the subcutaneous tissue that is currently not treatable with medication only. Standard itraconazole therapy is combined with surgical excision of the lesion. Recently, ibrexafungerp, a novel oral antifungal agent inhibiting 1,3-β-D-glucan synthesis, was approved by the United States Food and Drug Administration (FDA) for the treatment of vulvovaginal candidiasis. In this study we determined the in vitro activity and in vivo efficacy of ibrexafungerp in eumycetoma causative agents.
In vitro activity of ibrexafungerp and itraconazole was determined against 30 Madurella and 7 Falciformispora isolates by standardized in vitro susceptibility assays. The in vivo efficacy of ibrexafungerp, itraconazole and the combination of ibrexafungerp and itraconazole was determined by measuring the 10 day survival in M. mycetomatis and F. senegalensis grain models in Galleria mellonella larvae. Grain number and size were determined in Grocott- and haematoxylin and eosin-stained sections.
Ibrexafungerp inhibited the growth of Madurella and Falciformispora species with MICs ranging from 4 to 64 mg/L and from 8 to 32 mg/L, respectively. In G. mellonella larvae, ibrexafungerp was not toxic and prolonged the survival in M. mycetomatis-infected larvae 10 days after infection, but not in F. senegalensis-infected larvae. Combining ibrexafungerp with itraconazole prolonged the survival of M. mycetomatis- and F. senegalensis-infected larvae. Treatment with ibrexafungerp alone and in combination resulted in smaller grains in M. mycetomatis-infected larvae.
Ibrexafungerp showed in vitro activity and in vivo efficacy against the two most common eumycetoma causative agents.
足菌肿是一种被忽视的热带皮下组织真菌病,目前仅靠药物治疗无法治愈。标准的伊曲康唑疗法需结合病变的手术切除。最近,新型口服抗真菌药ibrexafungerp,一种抑制1,3-β-D-葡聚糖合成的药物,已获美国食品药品监督管理局(FDA)批准用于治疗外阴阴道念珠菌病。在本研究中,我们测定了ibrexafungerp对足菌肿病原体的体外活性和体内疗效。
通过标准化的体外药敏试验,测定ibrexafungerp和伊曲康唑对30株马杜拉菌和7株镰孢菌分离株的体外活性。通过测量在大蜡螟幼虫的马杜拉足菌肿和塞内加尔镰孢菌颗粒模型中的10天存活率,来确定ibrexafungerp、伊曲康唑以及ibrexafungerp与伊曲康唑联合用药的体内疗效。通过Grocott染色以及苏木精和伊红染色切片来确定颗粒数量和大小。
ibrexafungerp抑制马杜拉菌和镰孢菌属菌种的生长,其最低抑菌浓度(MIC)分别为4至64mg/L和8至32mg/L。在大蜡螟幼虫中,ibrexafungerp无毒,感染后10天可延长感染马杜拉足菌肿幼虫的存活时间,但对感染塞内加尔镰孢菌的幼虫无效。将ibrexafungerp与伊曲康唑联合使用可延长感染马杜拉足菌肿和塞内加尔镰孢菌幼虫的存活时间。单独使用和联合使用ibrexafungerp治疗均使感染马杜拉足菌肿幼虫体内的颗粒变小。
ibrexafungerp对两种最常见的足菌肿病原体显示出体外活性和体内疗效。