申请人:Amersham plc
公开号:US06534488B1
公开(公告)日:2003-03-18
The present invention relates to 32P or 33P-labelled bisphosphonates as radiotherapeutic radiopharmaceuticals. The 32P- or 33P-labelled bisphosphonates, which are chemically identical to the unlabelled agent, are expected to target the lesion site in an identical manner, but also deliver a significant radiocytotoxic effect to the surrounding cells. This should result, given the favorable energetics of the &bgr; particle emission from the 33P nuclide, in a loss of proliferative capacity of cells associated with the tumor lesion. The relative stability and in vivo localisation of bisphosphonates makes them good candidates as 32P/33P delivery vehicles.
本发明涉及32P或33P标记的双磷酸盐作为放射性治疗放射性药物。32P或33P标记的双磷酸盐与未标记的药物在化学上是相同的,预计它们将以相同的方式靶向病变部位,但也会对周围细胞产生显著的放射性细胞毒作用。鉴于33P核素从β粒子发射的有利能量学特性,这应该导致与肿瘤病变相关的细胞的增殖能力下降。双磷酸盐的相对稳定性和体内定位使它们成为32P/33P输送载体的良好候选者。