乳腺癌前哨淋巴结活检术新型荧光靶向示踪剂的研发进展

Research and Development Progress of a New Targeted-fluorescent Tracer for Sentinel Lymph Node Biopsy in Breast Cancer

前哨淋巴结活检术是临床腋窝淋巴结阴性的早期乳腺癌患者腋窝的标准处理模式,但由于传统示踪剂(蓝染料、核素和荧光示踪剂等)定位特异性差及药物准入等问题,限制了其在临床的推广应用。蓝染料和荧光示踪剂由于分子颗粒较小导致其易通过前哨淋巴结使次级淋巴结显像。核素示踪剂虽然可以特异性定位前哨淋巴结,但存在药品准入和放射安全性等问题。利妥昔单抗是一种针对淋巴结中B淋巴细胞膜上CD20分子的特异性人源化单克隆抗体,新型荧光靶向示踪剂将吲哚菁绿偶联于利妥昔单抗,将兼顾荧光显像与靶向定位的优点,其单抗的分子完整性和免疫活性无破坏,为无菌、无致热原、无急性毒性的示踪剂。

Sentinel lymph node biopsy has become the standard procedure for the axillary staging in early breast cancer patients;however,the extensive application of sentinel lymph node biopsy has been restricted by the poor specificity and access issue of the traditional tracers.In clinical practice,the dye and the fluorescence tracer exists the disadvantage that they could easily pass through the sentinel lymph node to the distal or second echelon lymph nodes.Radiotracer could specifically locate the sentinel lymph node,but its wildly clinical application has been limited with the access to sulfur colloid in China and radiation safety.Rituximab is a lymph-targeted humanized monoclonal antibody against the CD20 molecule in the B-lymphocyte membrane.A new targeted-fluorescent tracer was developed with the combine of the fluorescence tracer to rituximab,and might have the advantages of both fluorescence imaging and target locating.The new targeted-fluorescent tracer has kept the molecular integrity and the immune activity of the monoclonal antibody without bacteria,pyogen and acute toxicity.