乳腺癌患者曲妥珠单抗治疗失败后Margetuximab的应用研究进展

Progress on Margetuximab for Breast Cancer Patients with Trastuzumab Failure

人表皮生长因子受体2(human epidermal growth factor receptor 2,HER2)阳性乳腺癌是乳腺癌中最具侵袭性的亚型,恶性程度高且易发生转移。尽管曲妥珠单抗作为HER2阳性晚期乳腺癌一线靶向药物取得了巨大成功,但仍有部分患者存在心脏毒性及耐药性问题。相比曲妥珠单抗,Margetuximab的Fc段得到优化,其对曲妥珠单抗治疗后进展的HER2阳性乳腺癌也有一定作用,在后曲妥珠时代仍有一席之地。全文对Margetuximab的结构特点、作用机制、药效学、药物代谢动力学及临床研究作一综述,为其临床用药提供参考。

Human epidermal growth factor receptor 2(HER2)positive breast cancer is one of the most aggressive subtypes of breast cancer,with high malignancy and metastatic tendency.Despite the great success of trastuzumab as a first-line targeted agent for HER2-positive advanced breast cancer,cardiotoxicity and drug resistance are still problems in some patients.Compared to trastuzumab,the Fc segment of margetuximab is optimized.Margetuximab can be used in HER2 positive breast cancer patients who have progressed after trastuzumab treatment and it would be a new anti-HER2 targeted drug in the post-trastuzumab era.This review summarizes the structural characteristics,mechanism of action,pharmacodynamics,pharmacokinetics and clinical trials of margetuximab.