乳腺癌脑转移（BCBM）的发生率仅次于肺癌，是导致脑转移癌的第二大常见病因。随着乳腺癌患者生存期的不断延长，脑转移的发生率呈持续上升趋势。手术及局部放疗是目前脑转移的主要治疗手段，化疗及靶向药物的全身治疗也发挥着重要作用。然而，血脑屏障的存在会降低大多数抗肿瘤药物的递送效率，进而导致脑转移病情不断进展，因此，迫切需要探寻具有针对性的治疗新方法。但目前，BCBM患者往往被明确排除在大部分临床试验之外，致使该领域缺乏相关临床研究。小分子激酶抑制剂（SMKIs）具有相对分子质量小、脂溶性高、侵入性较小的特点，且能特异性靶向乳腺癌细胞相关激酶，可有效预防和治疗脑转移。对目前正在研究的用于治疗BCBM的SMKIs进行总结，旨在为BCBM的临床治疗实践提供参考。

Breast cancer brain metastasis (BCBM) is the second most common cause of brain metastasis after lung cancer. With the continuous extension of survival time for breast cancer patients, the incidence of brain metastasis is on the rise. Surgery and local radiotherapy are the main treatment methods for brain metastasis at present, and systemic treatment with chemotherapy and targeted drugs also plays an important role. However, the existence of the blood-brain barrier reduces the delivery efficiency of most anti-tumor drugs, leading to the continuous progression of brain metastasis. Therefore, it is urgent to explore new targeted treatment methods. However, at present, BCBM patients are often explicitly excluded from most clinical trials, resulting in a lack of relevant clinical research in this field. Small molecule kinase inhibitors (SMKIs) have the characteristics of small molecular weight, high lipid solubility, and low invasiveness, and can specifically target breast cancer cell-related kinases, effectively preventing and treating brain metastasis. This review summarizes the SMKIs currently under study for the treatment of BCBM, aiming to provide a reference for the clinical treatment of BCBM.

R979.1

国家自然科学基金资助项目（82104553）