Smith M B, Reardon J, Olson E M
James Cancer Hospital and Solove Research Institute, The Ohio State University, Columbus, Ohio 43212, USA.
Drugs Today (Barc). 2012 Nov;48(11):713-22. doi: 10.1358/dot.2012.48.11.1885879.
Pertuzumab is a humanized monoclonal antibody directed at the dimerization domain of the receptor tyrosine-protein kinase erbB-2 (HER2) receptor. It possesses a unique and complimentary mechanism of action compared to trastuzumab, which has historically been the cornerstone of therapy for HER2-amplified breast cancer. Clinical trials demonstrate improved outcomes, with minimal increases in toxicity with the addition of pertuzumab to trastuzumab in patients with HER2-positive metastatic breast cancer, indicating the advantage of dual HER2 receptor blockade. Pertuzumab is approved as first-line therapy in combination with trastuzumab and docetaxel for HER2-positive metastatic breast cancer, with future opportunities to investigate its efficacy in other stages of breast cancer, as well as in the treatment of other malignancies.
帕妥珠单抗是一种人源化单克隆抗体，作用于受体酪氨酸蛋白激酶erbB-2（HER2）受体的二聚化结构域。与曲妥珠单抗相比，它具有独特且互补的作用机制，而曲妥珠单抗一直是HER2扩增型乳腺癌治疗的基石。临床试验表明，在HER2阳性转移性乳腺癌患者中，将帕妥珠单抗与曲妥珠单抗联合使用可改善治疗效果，且毒性增加极小，这表明双重HER2受体阻断具有优势。帕妥珠单抗被批准作为HER2阳性转移性乳腺癌的一线治疗药物，与曲妥珠单抗和多西他赛联合使用，未来还有机会研究其在乳腺癌其他阶段以及其他恶性肿瘤治疗中的疗效。
