a Universidad Nacional de Rosario , CONICET, Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas , Rosario , Santa Fe , Argentina.
b Universidad Nacional del Litoral , CONICET, Cátedra de Cultivos Intensivos, Facultad de Ciencias Agrarias , Esperanza , Santa Fe , Argentina.
Expert Opin Ther Pat. 2017 Apr;27(4):415-426. doi: 10.1080/13543776.2017.1261113. Epub 2016 Nov 29.
Superficial infections involving the skin and mucosa are the most common fungal disease in humans. Fungi can also produce invasive infections (IFI), which are increasing in incidence among the growing population of immunocompromised patients, and are characterized by a high mortality rate. Amphotericin B, new triazoles and echinocandins have improved treatment options in IFI. However, the frequency of less common and more resistant fungi, the limited activity of available antifungal drugs and their undesirable side effects reflect the urgent need for the development of new therapeutic strategies. Areas covered: This review summarizes the patents granted from August 2013 to June 2016 for antifungal compounds, reflecting the advances made by pharmaceutical companies and research groups in the discovery of new natural or synthetic antifungal compounds as well as the improvement of previously patented structures with antifungal activity. Expert opinion: in the period covered here, progress has been in the development of new antifungal compounds or analogs of existing drugs with broad spectrum of activity, more favorable pharmacokinetic profiles or better bioavailability. However, the development of more promising approaches as antifungal compounds with broader antifungal activity and fungal-specific mechanisms of action are a high priority.
皮肤和黏膜的浅部感染是人类最常见的真菌感染。真菌还会引起侵袭性感染(IFI),在免疫功能低下患者人群不断增加的情况下,IFI 的发病率也在上升,其死亡率很高。两性霉素 B、新型三唑类药物和棘白菌素类药物改善了 IFI 的治疗选择。但是,不常见和耐药真菌的出现频率、现有抗真菌药物的活性有限以及它们的不良副作用都反映出迫切需要开发新的治疗策略。
本综述总结了 2013 年 8 月至 2016 年 6 月期间授予的抗真菌化合物专利,反映了制药公司和研究小组在发现新的天然或合成抗真菌化合物以及改进具有抗真菌活性的现有专利结构方面的进展。
在本文所述期间,研究进展主要集中在开发具有广谱活性、更有利的药代动力学特征或更好生物利用度的新型抗真菌化合物或现有药物的类似物上。但是,作为具有更广泛抗真菌活性和真菌特异性作用机制的抗真菌化合物,开发更有前途的方法是当务之急。