Maxon H R, Schroder L E, Washburn L C, Thomas S R, Samaratunga R C, Biniakiewicz D, Moulton J S, Cummings D, Ehrhardt G J, Morris V
Department of Radiology, University of Cincinnati Medical Center, Ohio 45267-0577, USA.
J Nucl Med. 1998 Apr;39(4):659-63.
Rhenium-188 (tin) hydroxyethylidine diphosphonate [188Re(Sn)HEDP] is a new radiopharmaceutical that localizes in skeletal metastases and emits beta particles that may be therapeutically beneficial.
It was evaluated by in vitro and in vivo testing in the laboratory, in animals and in humans using 188Re from a variety of sources. It may be produced by a desk-top method developed previously for 186Re(Sn)HEDP using 188Re produced through neutron irradiation of either enriched 187Re or naturally occurring rhenium targets or the use of a 188W/188Re generator.
So long as the mass of rhenium in the 188Re-perrhenate to be processed into 188Re(Sn)HEDP is at least 100 microg, satisfactory radiochemical yields and purity may be obtained by all methods. The 188Re(Sn)HEDP has biodistribution and radiation dosimetry characteristics that are similar to those noted previously for 186Re(Sn)HEDP and appears to result in similar benefits and toxicities in patients with skeletal metastases. External radiation exposure monitoring indicates that, only 4 hr after a therapeutic administration of 1110 MBq (30 mCi) of 188Re(Sn)HEDP, average exposure rates at 1 meter from the patient would be only 0.5 mR/hr.
Same-day, on-demand, outpatient therapy of disseminated skeletal metastases appears to be feasible with 188Re(Sn)HEDP.
铼-188(锡)羟乙二膦酸盐[188Re(Sn)HEDP]是一种新型放射性药物,可定位于骨转移灶并发射β粒子,可能具有治疗益处。
在实验室、动物和人体中使用来自多种来源的188Re进行体外和体内测试对其进行评估。它可以通过先前为186Re(Sn)HEDP开发的台式方法生产,该方法使用通过对富集的187Re或天然铼靶进行中子辐照产生的188Re,或者使用188W/188Re发生器。
只要要加工成188Re(Sn)HEDP的高铼酸盐中铼的质量至少为100微克,所有方法均可获得令人满意的放射化学产率和纯度。188Re(Sn)HEDP具有与先前报道的186Re(Sn)HEDP相似的生物分布和辐射剂量学特征,并且在骨转移患者中似乎产生相似的益处和毒性。外部辐射暴露监测表明,在治疗性给予1110 MBq(30 mCi)的188Re(Sn)HEDP后仅4小时,距患者1米处的平均暴露率仅为0.5 mR/小时。
使用188Re(Sn)HEDP对播散性骨转移进行当日按需门诊治疗似乎是可行的。