Anidulafungin is an echinocandin antifungal drug [1]. Anidulafungin inhibits the synthesis of β-(1,3)-D-glucan in the fungal cell wall, thereby disrupting the integrity of the cell wall and causing cell lysis and death [2]. Anidulafungin is primarily used to treat invasive candida infections, including candidemia and other deep candidiasis, and is particularly suitable for patients who cannot tolerate or are resistant to azoles such as fluconazole [3-4].
In erythrocytes, Anidulafungin (1.5-6µg/mL; 48h) can cause morphological changes in red blood cells, manifested as cell shrinkage, decreased forward scattering, and increased hemolysis rate, suggesting that it may affect red blood cell integrity by destroying cell membrane stability [5]. In BV2 microglial cells, Anidulafungin (10nM–5μM, 24h) selectively blocks the primary nucleation of Aβ aggregation, significantly delays fibril formation, and confers potential neuroprotective effects by reducing oligomeric Aβ-induced cytotoxicity [6].
In invasive Candidiasis mice model, signs of improved infection in the kidneys of mice treated with Anidulafungin (0.3mg/kg; iv; 6d) included a reduction in the area of inflammatory cells and the number of fungal hyphae surrounding tubules and glomeruli [7]. In neutropenic murine disseminated Candidiasis model, Anidulafungin (1.25–320mg/kg; ip; 96h) exhibits potent efficacy against multiple Candida species (including C. albicans, C. tropicalis, and C. glabrata), with its activity primarily determined by the C_max/MIC and AUC/MIC ratios, maintaining prolonged antifungal effects even when blood concentrations fall below the MIC, thereby demonstrating sustained activity and favorable pharmacokinetic properties [8].
References:
[1]. Raasch R H. Anidulafungin: review of a new echinocandin antifungal agent[J]. Expert review of anti-infective therapy, 2004, 2(4): 499-508.
[2]. Aderiye B I, Oluwole O A. Antifungal agents that target fungal cell wall components: a review[J]. Agri Biol Sci, 2015, 1: 206-216.
[3]. Vazquez J A, Sobel J D. Anidulafungin: a novel echinocandin[J]. Clinical infectious diseases, 2006, 43(2): 215-222.
[4]. Mayr A, Aigner M, Lass‐Flörl C. Anidulafungin for the treatment of invasive candidiasis[J]. Clinical Microbiology and Infection, 2011, 17: 1-12.
[5]. Peter T, Bissinger R, Liu G, et al. Anidulafungin-induced suicidal erythrocyte death[J]. Cellular Physiology and Biochemistry, 2016, 38(6): 2272-2284.
[6]. Xie S, Liang Y, Song Y, et al. Repurposing Anidulafungin for Alzheimer’s Disease via Fragment-Based Drug Discovery[J]. ACS Chemical Neuroscience, 2024, 15(16): 2995-3008.
[7]. Zhang Y, Liu Y C, Chen S M, et al. Evaluation of the in vitro activity and in vivo efficacy of anidulafungin-loaded human serum albumin nanoparticles against Candida albicans[J]. Frontiers in Microbiology, 2021, 12: 788442.
[8]. Andes D, Diekema DJ, Pfaller MA, et al. In vivo pharmacodynamic characterization of anidulafungin in a neutropenic murine candidiasis model. Antimicrob Agents Chemother. 2008 Feb;52(2):539-50.
Anidulafungin是一种棘白菌素类抗真菌药物 [1]。Anidulafungin抑制真菌细胞壁中β-(1,3)-D-葡聚糖的合成，从而破坏细胞壁的完整性，导致细胞裂解和死亡 [2]。Anidulafungin主要用于治疗侵袭性念珠菌感染，包括念珠菌血症和其他深部念珠菌病，尤其适用于对fluconazole等唑类药物无法耐受或耐药的患者 [3-4]。
在红细胞中，Anidulafungin（1.5-6µg/mL；48h）可引起红细胞形态学改变，表现为细胞皱缩、前向散射降低和溶血率增加，提示其可能通过破坏细胞膜稳定性来影响红细胞完整性 [5]。在BV2小胶质细胞中，Anidulafungin（10nM-5μM，24h）选择性阻断Aβ聚集的初级成核，显著延缓纤维形成，并通过降低寡聚Aβ诱导的细胞毒性发挥潜在的神经保护作用 [6]。
在侵袭性念珠菌病小鼠模型中，经Anidulafungin（0.3mg/kg；iv；6d）治疗的小鼠肾脏感染改善的迹象包括炎症细胞面积减少以及肾小管和肾小球周围真菌菌丝数量的减少 [7]。在中性粒细胞减少性小鼠播散性念珠菌病模型中，Anidulafungin（1.25-320mg/kg；ip；96h）对多种念珠菌（包括白色念珠菌、热带念珠菌和光滑念珠菌）表现出强效疗效，其活性主要由C_max/MIC和AUC/MIC比率决定，即使血液浓度低于MIC也能维持长时间的抗真菌作用，从而表现出持续的活性和良好的药代动力学特性 [8]。