Anticancer Potential of Diazepam: Pharmacological Relevance and Clinical Evidence

Cancer treatments such as chemotherapy, radiation, and targeted therapies often face challenges like severe side effects, drug resistance, and high costs. Repurposing existing medications is a promising strategy to improve treatment outcomes. Diazepam (DZP), a benzodiazepine commonly used for anxiety, has recently shown potential anticancer effects. This study explores the anticancer activity of DZP, focusing on its mechanisms of action, pharmacological relevance, immunotherapy, pharmacokinetics profile, toxicological profile, and clinical evidence through literature review from articles and journals in PubMed, Scopus, Google Scholar, and the Web of Science. DZP exerts antitumor effects by inducing apoptosis, inhibiting cell proliferation, and modulating oxidative stress and cell cycle dynamics against various cancers: blood cancer, brain cancer, breast cancer, colorectal cancer, glioblastoma, lung cancer, and skin cancer. DZP also demonstrates synergistic potential with conventional chemotherapeutic agents, enhancing their effectiveness while reducing patient anxiety and stress. Its pharmacokinetic profile, characterized by rapid absorption, extensive tissue distribution, and a prolonged half-life, supports its utility as a sustained anticancer agent. A significant gap in our investigation is the lack of clinical data on DZP; additional clinical evidence is required to validate its anticancer potential and establish it as an anticancer drug in the near future. Its sedative and CNS depressant effects necessitate cautious use, particularly in patients with hepatic or renal impairment. This review highlights the potential of DZP as a cost-effective, repurposed therapeutic option for cancer treatment. Additionally, it demonstrates how DZP may be a viable anticancer medication with a potential mechanism, maybe providing a better safety profile and less serious side effects than traditional treatments like chemotherapy.