德帕瑞妥单抗是首款靶向人表皮生长因子受体3（HER3）的抗体-药物偶联药物（ADC），由HER3单克隆抗体Patritumab通过可切割接头与有效载荷拓扑异构酶I抑制剂DX-8951衍生物（DXd）共价连接而成。多项临床前研究及临床试验已证实，德帕瑞妥单抗在HER3表达阳性的实体恶性肿瘤中表现出显著的抗肿瘤活性及良好的安全性。其临床价值具体体现在：对于表皮生长因子受体（EGFR）基因突变、且经表皮生长因子受体酪氨酸激酶抑制剂（EGFR-TKI）及铂类治疗失败的非小细胞肺癌患者及各时期乳腺癌患者均能带来明确获益；细胞及动物实验亦证实其对结直肠癌具有显著治疗作用。值得关注的是，德帕瑞妥单抗具有中枢神经系统穿透性，可有效改善实体瘤脑转移患者的预后，具有极大的临床研究价值。对德帕瑞妥单抗的群体药动学特征、临床研究进展以及不良事件等方面进行综述，以期为非小细胞肺癌、乳腺癌和结直肠癌患者的治疗提供新策略。

Patritumab deruxtecan is the first antibody-drug conjugate (ADC) targeting human epidermal growth factor receptor 3 (HER3). It is formed by covalently linking the HER3 monoclonal antibody Patritumab to the payload DXd (a derivative of the topoisomerase I inhibitor DX-8951) through a cleavable linker. Multiple preclinical studies and clinical trials have demonstrated that patritumab deruxtecan exhibits significant anti-tumor activity and good safety in solid malignancies with HER3 expression. It can bring clear benefits to patients with non-small cell lung cancer with epidermal growth factor receptor (EGFR) gene mutations and who have failed epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) and platinum-based treatments, as well as patients with breast cancer at all stages. In addition, both cell and animal experiments have confirmed that it has a significant therapeutic effect on colorectal cancer. Notably, Patritumab deruxtecan has central nervous system penetration and can effectively improve the prognosis of patients with brain metastases from solid tumors, demonstrating great clinical research value. This article reviews the population pharmacokinetic characteristics, clinical research progress, and adverse events of Patritumab deruxtecan, with the aim of providing new treatment strategies for patients with non-small cell lung cancer, breast cancer, and colorectal cancer.

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