Springer Nature, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand.
Drugs. 2021 Apr;81(5):599-604. doi: 10.1007/s40265-021-01485-2. Epub 2021 Mar 24.
The second-generation anti-human epidermal growth factor receptor2 protein (HER2) monoclonal antibody margetuximab (MARGENZA™, margetuximab-cmkb) is being developed for the treatment of HER2-positive breast cancer, gastric cancer and gastro-oesophageal junction cancer. The antibody has been engineered for increased binding to activating Fcγ receptor IIIA (CD16A) and decreased binding to inhibitory Fcγ receptor IIB (CD32B) relative to trastuzumab with the aim of improving response rates. Based on the results of the phase III SOPHIA trial margetuximab has been approved in the USA for use in combination with chemotherapy as treatment of previously-treated metastatic HER2-positive breast cancer. This article summarizes the milestones in the development of margetuximab leading to this first approval.
第二代抗人表皮生长因子受体 2 蛋白（HER2）单克隆抗体玛格妥昔单抗（Margetuximab，MARGENZA™，玛格妥昔单抗-cmkb）正在开发用于治疗 HER2 阳性乳腺癌、胃癌和胃食管交界处癌。与曲妥珠单抗相比，该抗体经过工程改造，增加了与激活型 Fcγ 受体 IIIA（CD16A）的结合，减少了与抑制型 Fcγ 受体 IIB（CD32B）的结合，目的是提高反应率。基于 III 期 SOPHIA 试验的结果，玛格妥昔单抗已在美国获得批准，与化疗联合用于治疗先前治疗的转移性 HER2 阳性乳腺癌。本文总结了玛格妥昔单抗开发过程中的重要里程碑，最终促成了该药的首次批准。
