Louw W K, Dormehl I C, van Rensburg A J, Hugo N, Alberts A S, Forsyth O E, Beverley G, Sweetlove M A, Marais J, Lötter M G, van Aswegen A
Atomic Energy Corporation of South Africa Limited.
Nucl Med Biol. 1996 Nov;23(8):935-40. doi: 10.1016/s0969-8051(96)00117-5.
Bone-seeking radiopharmaceuticals such as ethylenediaminetetramethylene phosphonate (EDTMP) complexes of samarium-153 and holmium-166 are receiving considerable attention for therapeutic treatment of bone metastases. In this study, using the baboon experimental model, multicompartmental analysis revealed that with regard to pharmacokinetics, biodistribution, and skeletal localisation, 166Ho-EDTMP was significantly inferior to 153Sm-EDTMP and 99mTc-MDP. A more suitable 166Ho-bone-seeking agent should thus be sought for closer similarity to 153Sm-EDTMP to exploit fully the therapeutic potential of its shorter half-life and more energetic beta radiation.
诸如钐-153和钬-166的乙二胺四亚甲基膦酸盐（EDTMP）络合物等亲骨性放射性药物在骨转移瘤的治疗中受到了广泛关注。在本研究中，使用狒狒实验模型，多室分析显示，在药代动力学、生物分布和骨骼定位方面，166Ho-EDTMP明显不如153Sm-EDTMP和99mTc-MDP。因此，应该寻找一种更合适的166Ho亲骨剂，使其更接近153Sm-EDTMP，以充分发挥其较短半衰期和更高能量β辐射的治疗潜力。
