叶酸受体α（folate receptor α，FRα）是通过糖基磷脂酰肌醇链接的细胞表面糖蛋白，它在正常组织中的表达极度受限，而在包括卵巢癌、肺癌和乳腺癌在内的一系列实体肿瘤中过表达。FRα在肿瘤中的异常表达以及介导大分子复合物内化的能力，吸引了针对该靶点的抗体偶联药物（antibody-drug conjugate，ADC）的开发。此文对FRα在肿瘤学中的意义以及靶向FRα的ADC临床前和临床试验结果进行概述。

Folate receptor α (FRα) is a cell surface glycoprotein linked by glycosyl- phosphatidylinositol. The expression of FRα in normal tissues is extremely limited, but it is overexpressed in a series of solid tumors including ovarian cancer, lung cancer and breast cancer. The abnormal expression of FRα in tumors and its ability to mediate internalization of macromolecular complexes attract the development of antibody-drug conjugate (ADC) for this target. In this review, the significance of FRα in oncology and the preclinical and clinical trials results of ADC targeting FRα are summarized.