新型亲骨性α发射体镭溶液在乳腺癌骨转移模型中的抗肿瘤活性
Antitumor Activity of Novel Bone-seeking, α-emitting Ra-solution in a Breast Cancer Skeletal Metastases Model.
作者信息
Juzeniene Asta, Bernoulli Jenni, Suominen Mari, Halleen Jussi, Larsen Roy Hartvig
机构信息
Department of Radiation Biology, Institute for Cancer Research, Norwegian Radium Hospital, Oslo University Hospital, Oslo, Norway.
Pharmatest Services Ltd, Turku, Finland.
出版信息
Anticancer Res. 2018 Apr;38(4):1947-1955. doi: 10.21873/anticanres.12432.
BACKGROUND/AIM: Bone metastases are associated with increased morbidity and poor prognosis in a variety of cancers. The present study investigated the effects of targeted radionuclide therapy with α-emitting, bone-seeking radium-224 (Ra) on osteolytic bone metastasis of MDA-MB-231(SA)-GFP human breast cancer cells injected intracardially into nude mice.
MATERIALS AND METHODS
Vehicle, ethylenediamine tetra (methylene phosphonic acid) (EDTMP) and Ra-solution (45, 91 or 179 kBq/kg) with EDTMP were intravenously administered to mice two days after cell injection. The bone-seeking EDTMP was added to the Ra-solution to improve bone targeting of Pb, which is a progeny of Ra.
RESULTS
Radium-224 solution treatment decreased in a dose-dependent manner the areas of osteolytic lesions in the hind limbs and the number of tumor foci in the whole skeleton, and extended survival. Paraplegia was not observed in 179 kBq/kg Ra-solution group.
CONCLUSION
Radium-224-solution containing chelated Pb is a promising candidate for the treatment of breast cancer patients with bone metastases.
背景/目的：骨转移与多种癌症的发病率增加和预后不良相关。本研究调查了用发射α粒子、亲骨性的镭-224（Ra）进行靶向放射性核素治疗对经心内注射到裸鼠体内的MDA-MB-231（SA）-GFP人乳腺癌细胞溶骨性骨转移的影响。
材料与方法
在细胞注射两天后，给小鼠静脉注射赋形剂、乙二胺四（亚甲基膦酸）（EDTMP）以及含EDTMP的Ra溶液（45、91或179 kBq/kg）。将亲骨性的EDTMP添加到Ra溶液中，以改善Ra的子代铅（Pb）的骨靶向性。
结果
镭-224溶液治疗以剂量依赖性方式减少了后肢溶骨性病变的面积和全骨骼肿瘤灶的数量，并延长了生存期。179 kBq/kg Ra溶液组未观察到截瘫现象。
结论
含螯合铅的镭-224溶液是治疗骨转移乳腺癌患者的一个有前景的候选方案。
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