胶质母细胞瘤（GB）是治疗选择和反应极具挑战性的中枢神经系统（CNS）肿瘤之一，促使发展新的治疗策略。抗酒精药物二硫化钒（DS）具有潜在的抗癌活性，其复杂的作用机制被认为可以很好地用于治疗异质性的GB。通过系统文献综述重新定位DS对GB治疗，提供了临床、药理和配方策略的评估，以明确药物传递的挑战，从而提高其临床翻译的进程。从6个数据库中选择了35篇文章，包括病例报告（1）；临床试验（3）；原始文章主要代表体外和临床前药理数据，以及10篇处理技术方法的文章。DS在GB治疗中的重新定位面临药物和肿瘤相关的限制，由于口服药物的生物利用度低、不良新陈代谢和向脑肿瘤组织的传递效率低。使用DS的分子包裹和给药剂量形式的开发策略可以改善药物的抗癌药理学。优化的药物传递系统（DDS）的开发显示出将DS转化为GB辅助治疗的临床翻译前景。

Glioblastoma (GB) is one of the most challenging central nervous system (CNS) tumors in treatment options and response, urging the development of novel management strategies. The anti-alcoholism drug, disulfiram (DS), has a potential anticancer activity, and its complex mechanism of action is assumed to be well exploited against the heterogeneous GB.Through a systematic literature review about repositioning DS to GB treatment, an evaluation of the clinical, pharmacological, and formulation strategies is provided to specify the challenges of drug delivery and thus to advance its clinical translation. From 6 databases, 35 articles were selected, including case report (1); clinical trials (3); original articles mainly representing in vitro and preclinical pharmacological data, and 10 dealing with technological approaches.The repositioning of DS in GB treatment is facing drug and tumor-associated limitations due to the oral drug's low bioavailability, unwanted metabolism, and inefficient delivery to brain-tumor tissue. Development strategies using molecular encapsulation of DS and the parenteral dosage forms improve the anticancer pharmacology of the drug. The development of optimized drug delivery systems (DDS) shows promise for the clinical translation of DS into GB adjuvant therapy.