Lamb H M, Faulds D
Adis International Limited, Auckland, New Zealand.
Drugs Aging. 1997 Nov;11(5):413-8; discussion 419. doi: 10.2165/00002512-199711050-00007.
Samarium 153Sm lexidronam is a medium energy beta-emitting radioisotope chelated to the tetraphosphate, ethylenediaminetetramethylenephosphonic acid (EDTMP). 153Sm has a physical half-life of 1.9 days. Samarium 153Sm lexidronam concentrates in bone tissue and has a metastatic lesion: normal bone ratio of 4. Clearance of nonskeletal radioactivity after administration of samarium 153Sm lexidronam is rapid, and is almost complete from the blood and urine within 1 and 6 hours, respectively. Some degree of pain relief was achieved in 72% of patients with bone metastases after a single dose of samarium 153Sm lexidronam 1 mCi/kg (37 MBq/kg) compared with 44% of placebo recipients (p < 0.025). Relief was generally attained within 2 weeks and lasted for a median of 8 to 15 weeks. After recurrence of pain, a second dose of samarium 153Sm lexidronam may produce further pain relief in some patients. The dose-limiting toxicity of samarium 153Sm lexidronam is reversible myelosuppression.
钐153Sm-乙二胺四甲基膦酸(153Sm lexidronam)是一种中等能量的β发射放射性同位素,与四磷酸乙二胺四亚甲基膦酸(EDTMP)螯合。153Sm的物理半衰期为1.9天。钐153Sm-乙二胺四甲基膦酸在骨组织中浓聚,转移病灶与正常骨的比例为4。给予钐153Sm-乙二胺四甲基膦酸后,非骨骼放射性的清除很快,分别在1小时和6小时内几乎完全从血液和尿液中清除。单剂量给予钐153Sm-乙二胺四甲基膦酸1 mCi/kg(37 MBq/kg)后,72%的骨转移患者实现了一定程度的疼痛缓解,而安慰剂组为44%(p < 0.025)。缓解通常在2周内实现,持续时间中位数为8至15周。疼痛复发后,第二剂钐153Sm-乙二胺四甲基膦酸可能会使一些患者进一步缓解疼痛。钐153Sm-乙二胺四甲基膦酸的剂量限制性毒性是可逆性骨髓抑制。