Biguanides have attracted much attention a century ago and showed resurgent interest in recent years after a long period of dormancy. They constitute an important class of therapeutic agents suitable for the treatment of a wide spectrum of diseases. Therapeutic indications of biguanides include antidiabetic, antimalarial, antiviral, antiplaque, and bactericidal applications.

This review presents an extensive overview of the biological activity of biguanides and different mechanisms of action of currently marketed biguanide-containing drugs, as well as their pharmacological properties when applicable. We highlight the recent developments in research on biguanide compounds, with a primary focus on studies on metformin in the field of oncology. We aim to provide a critical overview of all main bioactive biguanide compounds and discuss future perspectives for the design of new drugs based on the biguanide fragment.

双胍类药物在一个世纪前就引起了广泛的关注，并且在经过长时间的休眠后，近年来表现出重新燃起的兴趣。它们构成了适用于治疗广谱疾病的一类重要的治疗剂。双胍的治疗适应症包括抗糖尿病、抗疟疾、抗病毒、抗斑块和杀菌应用。

本综述广泛概述了双胍的生物活性和目前市售的含双胍药物的不同作用机制，以及适用时的药理特性。我们重点介绍双胍类化合物研究的最新进展，主要关注肿瘤学领域的二甲双胍研究。我们旨在提供对所有主要生物活性双胍化合物的批判性概述，并讨论基于双胍片段设计新药的未来前景。