Ibrahim Ashraf S, Gebermariam Teclegiorgis, Fu Yue, Lin Lin, Husseiny Mohamed I, French Samuel W, Schwartz Julie, Skory Christopher D, Edwards John E, Spellberg Brad J
Division of Infectious Diseases, Los Angeles Biomedical Research Institute at Harbor-UCLA Medical Center, Torrance, California 90502, USA.
J Clin Invest. 2007 Sep;117(9):2649-57. doi: 10.1172/JCI32338.
Mucormycosis causes mortality in at least 50% of cases despite current first-line therapies. Clinical and animal data indicate that the presence of elevated available serum iron predisposes the host to mucormycosis. Here we demonstrate that deferasirox, an iron chelator recently approved for use in humans by the US FDA, is a highly effective treatment for mucormycosis. Deferasirox effectively chelated iron from Rhizopus oryzae and demonstrated cidal activity in vitro against 28 of 29 clinical isolates of Mucorales at concentrations well below clinically achievable serum levels. When administered to diabetic ketoacidotic or neutropenic mice with mucormycosis, deferasirox significantly improved survival and decreased tissue fungal burden, with an efficacy similar to that of liposomal amphotericin B. Deferasirox treatment also enhanced the host inflammatory response to mucormycosis. Most importantly, deferasirox synergistically improved survival and reduced tissue fungal burden when combined with liposomal amphotericin B. These data support clinical investigation of adjunctive deferasirox therapy to improve the poor outcomes of mucormycosis with current therapy. As iron availability is integral to the pathogenesis of other infections (e.g., tuberculosis, malaria), broader investigation of deferasirox as an antiinfective treatment is warranted.
尽管有目前的一线治疗方法,毛霉菌病在至少50%的病例中仍会导致死亡。临床和动物数据表明,血清中铁含量升高会使宿主易患毛霉菌病。在此,我们证明地拉罗司(一种最近被美国食品药品监督管理局批准用于人类的铁螯合剂)是治疗毛霉菌病的高效药物。地拉罗司能有效地从米根霉中螯合铁,并在体外对29株毛霉目临床分离株中的28株表现出杀菌活性,其浓度远低于临床可达到的血清水平。给患有毛霉菌病的糖尿病酮症酸中毒或中性粒细胞减少的小鼠给药后,地拉罗司显著提高了生存率并降低了组织真菌负荷,其疗效与脂质体两性霉素B相似。地拉罗司治疗还增强了宿主对毛霉菌病的炎症反应。最重要的是,地拉罗司与脂质体两性霉素B联合使用时,能协同提高生存率并减轻组织真菌负荷。这些数据支持对地拉罗司辅助治疗进行临床研究,以改善目前治疗毛霉菌病的不良预后。由于铁的可用性是其他感染(如结核病、疟疾)发病机制的一个组成部分,因此有必要对地拉罗司作为抗感染治疗进行更广泛的研究。