德帕瑞妥單抗是首款靶向人表皮生長因子受體3（HER3）的抗體-藥物偶聯(lián)藥物（ADC），由HER3單克隆抗體Patritumab通過可切割接頭與有效載荷拓撲異構(gòu)酶I抑制劑DX-8951衍生物（DXd）共價連接而成。多項臨床前研究及臨床試驗已證實，德帕瑞妥單抗在HER3表達陽性的實體惡性腫瘤中表現(xiàn)出顯著的抗腫瘤活性及良好的安全性。其臨床價值具體體現(xiàn)在：對于表皮生長因子受體（EGFR）基因突變、且經(jīng)表皮生長因子受體酪氨酸激酶抑制劑（EGFR-TKI）及鉑類治療失敗的非小細胞肺癌患者及各時期乳腺癌患者均能帶來明確獲益；細胞及動物實驗亦證實其對結(jié)直腸癌具有顯著治療作用。值得關(guān)注的是，德帕瑞妥單抗具有中樞神經(jīng)系統(tǒng)穿透性，可有效改善實體瘤腦轉(zhuǎn)移患者的預(yù)后，具有極大的臨床研究價值。對德帕瑞妥單抗的群體藥動學(xué)特征、臨床研究進展以及不良事件等方面進行綜述，以期為非小細胞肺癌、乳腺癌和結(jié)直腸癌患者的治療提供新策略。

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.

R979.1