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新型抗真菌化合物马尼芬净(APX001)对三种临床最相关申克孢子丝菌的体外作用

In vitro effects of the new antifungal compound manogepix (APX001) against the three most clinically relevant species of Sporothrix.

作者信息

Almeida-Silva Fernando, Marques Fernanda Praça Nogueira, Tenório-Alvarenga Pedro Henrique, Poester Vanice Rodrigues, Xavier Melissa Orzechowski, Zancopé-Oliveira Rosely Maria, Almeida-Paes Rodrigo

机构信息

Laboratório de Micologia, Instituto Nacional de Infectologia Evandro Chagas (INI), Fundação Oswaldo Cruz (Fiocruz), Av. Brasil, 4365, Manguinhos, Rio de Janeiro, 21040-360, Brazil.

Programa de Pós-Graduação em Ciências da Saúde, Faculdade de Medicina (FAMED), Universidade Federal Do Rio Grande (FURG), Rio Grande, RS, Brasil.

出版信息

Braz J Microbiol. 2025 Jul 15. doi: 10.1007/s42770-025-01711-z.

Abstract

Sporotrichosis is an endemic mycosis that pose significant public health challenges, particularly in Brazil, where zoonotic transmission has increased the number of cases in several regions of the country. The disease is caused by Sporothrix genus, with S. brasiliensis, S. schenckii, and S. globosa as the major agents. The currently available therapies may face limitations such as varying cure rates, long and expensive treatment, and adverse effects. Fosmanogepix, a prodrug converted into manogepix within the host, has demonstrated broad-spectrum antifungal activity, including other thermodimorphic fungal species. Thus, this study aimed to evaluate the in vitro antifungal efficacy of manogepix against three clinically relevant Sporothrix species. Minimal inhibitory and fungicidal concentrations were determined against 24 Sporothrix spp. isolates, as well as potential synergism with antifungal drugs, induction of resistance and growth kinetics of the fungus in the presence of the new antifungal drug. Manogepix exhibited fungicidal activity against the three Sporothrix species tested, with minimum inhibitory concentrations (MIC) ranging from 0.06 to 1 µg/ml. Furthermore, manogepix demonstrated a lower geometric mean of MIC values compared to the antifungal drugs and indifferent interactions with itraconazole, terbinafine and amphotericin B. Prolonged exposure to subinhibitory manogepix concentrations did not induce resistance in the tested strains. These findings indicate manogepix as a promising candidate for the treatment of sporotrichosis, offering a potential alternative in cases of resistance or treatment failure with current antifungals. Further studies are needed to confirm this activity in clinical settings, particularly in diverse geographic regions and against a broader range of Sporothrix strains.

摘要

孢子丝菌病是一种地方性真菌病,对公共卫生构成重大挑战,尤其是在巴西,人畜共患传播增加了该国多个地区的病例数量。该疾病由孢子丝菌属引起,其中巴西孢子丝菌、申克孢子丝菌和球形孢子丝菌是主要病原体。目前可用的治疗方法可能面临各种限制,如治愈率不同、治疗时间长且费用高以及不良反应。福沙那韦,一种在宿主体内转化为吗啉胍的前体药物,已显示出广谱抗真菌活性,包括对其他双态真菌物种。因此,本研究旨在评估吗啉胍对三种临床相关孢子丝菌物种的体外抗真菌疗效。测定了对24株孢子丝菌属分离株的最小抑菌和杀菌浓度,以及与抗真菌药物的潜在协同作用、耐药性诱导和在新抗真菌药物存在下真菌的生长动力学。吗啉胍对所测试的三种孢子丝菌物种均表现出杀菌活性,最小抑菌浓度(MIC)范围为0.06至1μg/ml。此外,与抗真菌药物相比,吗啉胍的MIC值几何平均数更低,并且与伊曲康唑、特比萘芬和两性霉素B无相互作用。长时间暴露于亚抑菌浓度的吗啉胍不会诱导受试菌株产生耐药性。这些发现表明吗啉胍是治疗孢子丝菌病的有前景的候选药物,在目前抗真菌药物耐药或治疗失败的情况下提供了一种潜在的替代方案。需要进一步研究以在临床环境中证实这种活性,特别是在不同地理区域和针对更广泛的孢子丝菌菌株。

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