Radiosynthesis of 55Co- and 58mCo-labelled DOTATOC for positron emission tomography imaging and targeted radionuclide therapy

Radiosynthesis of 55Co- and 58mCo-labelled DOTATOC for positron emission tomography imaging and targeted radionuclide therapy
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DOI:
10.1002/jlcr.1919
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发表时间:
2011-10-01
影响因子:
1.8
通讯作者:
Dam, Johan Hygum
Dam, Johan Hygum
中科院分区:
医学4区
文献类型:
--
作者:
Thisgaard, Helge;Olesen, Marie Louise;Dam, Johan Hygum

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SPECT化合物Co-57-DOTATOC最近已被证明对生长抑素受体亚型2具有最高的亲和力。此外,肿瘤细胞系AR 42 J的内化率也是所有生长抑素类放射性药物中最高的。我们在这里提出了一种方法来制备正电子发射断层扫描化合物Co-55-DOTATOC作为一个新的有前途的放射性药物的正电子发射断层扫描通过固体靶辐照富集铁金属。此外,新的,有效的俄歇电子发射放射性同位素Co-58 m和所得的治疗化合物Co-58 m-DOTATOC作为生长抑素受体阳性肿瘤的靶向放射性核素治疗的候选者,已经以高产率和高放射化学纯度制备。
The SPECT compound Co-57-DOTATOC has recently been shown to have the highest affinity ever found for somatostatin receptor subtype 2. Moreover, the internalization rate into the tumour cell line AR42J was also the highest found for any somatostatin-based radiopharmaceutical. We here present a method to prepare the positron emission tomography compound Co-55-DOTATOC as a new promising radiopharmaceutical for positron emission tomography via solid target irradiations of enriched Fe-metal. Also, the new, potent Auger-electron-emitting radioisotope Co-58m and the resulting therapeutic compound Co-58m-DOTATOC as candidate for targeted radionuclide therapy of somatostatin receptor-positive tumours have been prepared with high yield and high radiochemical purity.