School of Pharmacy, University of Pittsburgh, Pittsburgh, PA, U.S.A.
Life Science Department, University of Science and Technology of Hanoi, Hanoi, Vietnam.
Anticancer Res. 2024 Sep;44(9):3725-3735. doi: 10.21873/anticanres.17197.
Fenbendazole is a benzimidazole anthelmintic agent commonly used to treat animal parasitic infections. In humans, other benzimidazoles, such as mebendazole and albendazole, are used as antiparasitic agents. Since fenbendazole is not currently approved by the FDA or EMA, its pharmacokinetics and safety in humans have yet to be well-documented in medical literature. Despite this, insights can be drawn from existing in vitro and in vivo animal studies on its pharmacokinetics. Given the low cost of fenbendazole, its high safety profile, accessibility, and unique anti-proliferative activities, fenbendazole would be the preferred benzimidazole compound to treat cancer. To ensure patient safety in the repurposing use of fenbendazole, it is crucial to perform clinical trials to assess its potential anticancer effects, optimal doses, therapeutic regimen, and tolerance profiles. This review focuses on the pharmacokinetics of orally administered fenbendazole and its promising anticancer biological activities, such as inhibiting glycolysis, down-regulating glucose uptake, inducing oxidative stress, and enhancing apoptosis in published experimental studies. Additionally, we evaluated the toxicity profile of fenbendazole and discussed possibilities for improving the bioavailability of the drug, enhancing its efficacy, and reducing potential toxicity.
芬苯达唑是一种苯并咪唑类驱虫药，常用于治疗动物寄生虫感染。在人类中，其他苯并咪唑类药物，如甲苯咪唑和阿苯达唑，被用作驱虫药。由于芬苯达唑目前尚未获得 FDA 或 EMA 的批准，其在人类中的药代动力学和安全性尚未在医学文献中得到很好的记录。尽管如此，仍可以从现有的体外和体内动物研究中了解其药代动力学。鉴于芬苯达唑成本低廉、安全性高、易于获得且具有独特的抗增殖活性，它将是治疗癌症的首选苯并咪唑化合物。为了确保在重新利用芬苯达唑时患者的安全，进行临床试验以评估其潜在的抗癌作用、最佳剂量、治疗方案和耐受谱至关重要。本综述重点介绍了口服芬苯达唑的药代动力学及其在已发表的实验研究中具有抑制糖酵解、下调葡萄糖摄取、诱导氧化应激和增强细胞凋亡等有前途的抗癌生物学活性。此外，我们评估了芬苯达唑的毒性概况，并讨论了提高药物生物利用度、增强其疗效和降低潜在毒性的可能性。
