Fenbendazole (FBZ), a benzimidazole-based anthelmintic, has recently gained attention for its promising anticancer properties. Multiple studies have demonstrated that FBZ exerts potent antiproliferative effects across diverse cancer types by disrupting microtubule dynamics, inducing G2/M phase arrest, and triggering apoptosis through p53 activation, caspase cascade initiation, and mitochondrial outer membrane permeabilization. It also promotes oxidative stress via enhanced reactive oxygen species (ROS) generation, contributing to mitochondrial dysfunction and cell death. Despite its therapeutic potential, FBZ’s poor aqueous solubility (0.3 µg/mL) and low bioavailability significantly restrict its clinical application. To address these limitations, recent advancements in drug delivery systems such as including PEGylated mesoporous nanoparticles, PLGA-based nanocarriers, β-cyclodextrin inclusion complexes, chitosan-crosslinked microparticles, and sulfonic acid salt formation have shown marked improvements in solubility, stability, and cytotoxic efficacy. Furthermore, pH-responsive and polymer-based formulations have enabled controlled drug release and enhanced tumour targeting, while maintaining biocompatibility and minimal systemic toxicity. Human evidence is presently anecdotal and includes case reports of self-administration with variable outcomes and rare but serious hepatotoxicity signals. Case series of human self-administration also report responses in metastatic cancers, though confounded by concomitant therapies and lack of controls. Taken together, the bench literature includes findings that establish fenbendazole as a strong candidate for drug repurposing in oncology, with innovative formulation approaches paving the way for future preclinical and clinical investigations. The accumulating preclinical evidence supports further translational inquiry into FBZ for oncology. However, critical gaps in human pharmacokinetics