Although HER2-targeted therapy has been shown to prolong the survival of patients with HER2-positive breast cancer, most patients eventually progress due to drug resistance. Novel treatment options are urgently needed to overcome resistance to HER2-targeted therapy. The VEGF/VEGFR (Vascular endothelial growth factor and its receptors) pathway is essential in tumor angiogenesis, which may be a promising target in HER2-positive breast cancer providing a rationale for the use of tyrosine kinase inhibitors (TKIs) targeting VEGFR. Here, we present a case of a heavily pretreated advanced breast cancer patient who did not respond to HER2-targeted therapy and developed resistance to multiple lines of HER2-targeted treatment. The patient was treated with apatinib at a dose of 500 mg daily, and obtained partial remission (PR) with a progression-free-stage (PFS) of 6 months. Our case indicates that apatinib might have anti-tumor activity in patients with HER2-positive breast cancer with HER2-targeted resistance. This case is of value which may provide new insights into strategies for HER2-targeted therapy resistance options in the clinic.

尽管 HER2 靶向治疗已被证明可以延长 HER2 阳性乳腺癌患者的生存期，但大多数患者最终会因耐药性而进展。迫切需要新的治疗方案来克服对 HER2 靶向治疗的耐药性。VEGF/VEGFR（血管内皮生长因子及其受体）通路在肿瘤血管生成中是必不可少的，这可能是 HER2 阳性乳腺癌的一个有希望的靶点，为使用靶向 VEGFR 的酪氨酸激酶抑制剂 (TKI) 提供了基本原理。在这里，我们介绍了一个经过大量预处理的晚期乳腺癌患者的案例，该患者对 HER2 靶向治疗没有反应，并对多种 HER2 靶向治疗产生耐药性。该患者每天服用 500 毫克阿帕替尼，并获得部分缓解（PR），无进展期（PFS）为 6 个月。我们的案例表明，阿帕替尼可能对 HER2 靶向耐药的 HER2 阳性乳腺癌患者具有抗肿瘤活性。这个案例很有价值，可以为临床中 HER2 靶向治疗耐药性选择的策略提供新的见解。