This review provides the delivery mechanism of FR-mediated antitumor drugs and highlights the novel folate-drug conjugates and their activities.

• 本文对叶酸受体介导的抗肿瘤药物的作用机制进行综述,介绍近几年研究者设计并合成的叶酸-药物缀合物及其活性测试的结果。