Key Laboratory of Study and Discovery of Small Targeted Molecules of Hunan, Department of Pharmacy, School of Medicine, Hunan Normal University, Changsha, Hunan 410013, P.R. China.
Oncol Rep. 2024 Nov;52(5). doi: 10.3892/or.2024.8810. Epub 2024 Sep 20.
Phenformin, a biguanide compound, has attracted increased attention due to its prominent antitumor activity. As a multi‑target agent, the antitumor effects of phenformin involve a wide range of factors, including inhibition of mitochondrial complex I, activation of AMP‑activated protein kinase, impact on the tumor microenvironment, suppression of cancer stem cells and others. In addition, phenformin has been shown to markedly augment the effectiveness of various clinical treatment methods, including radiotherapy, chemotherapy, targeted therapy and immunotherapy. It is noteworthy that breakthrough progress has been made in the treatment of cancer with phenformin with application in clinical trials for the treatment of melanoma. Phenformin not only reduces the lesion area of patients, but also enhances the efficacy of dalafinib/trimetinib. In the present review, the novel breakthroughs in the antitumor effects and mechanisms of phenformin were discussed. In addition, the current review focuses on the clinical development value of phenformin, striving to provide new insights into the future research direction of phenformin in the field of tumor treatment.
苯乙双胍，一种双胍类化合物，由于其突出的抗肿瘤活性而引起了越来越多的关注。作为一种多靶点药物，苯乙双胍的抗肿瘤作用涉及广泛的因素，包括抑制线粒体复合物 I、激活 AMP 激活的蛋白激酶、影响肿瘤微环境、抑制肿瘤干细胞等。此外，苯乙双胍已被证明可以显著提高放疗、化疗、靶向治疗和免疫治疗等各种临床治疗方法的效果。值得注意的是，苯乙双胍在治疗癌症方面取得了突破性进展，已应用于黑色素瘤的临床试验。苯乙双胍不仅减少了患者的病变面积，而且增强了达拉非尼/曲美替尼的疗效。在本综述中，讨论了苯乙双胍的抗肿瘤作用和机制的新突破。此外，本综述还重点关注了苯乙双胍的临床开发价值，力求为肿瘤治疗领域苯乙双胍的未来研究方向提供新的见解。
