Mather Stephen J, Nock Berthold A, Maina Theodosia, Gibson Vickie, Ellison David, Murray Iain, Sobnack Ravin, Colebrook Steve, Wan Susan, Halberrt Gavin, Szysko Teresa, Powles Thomas, Avril Norbert
Centre for Molecular Oncology, Barts Cancer Institute, London, EC1M 6BQ, UK,
Mol Imaging Biol. 2014 Dec;16(6):888-95. doi: 10.1007/s11307-014-0754-z.
We explored the imaging of bombesin receptors and evaluated the clinical use of [(99m)Tc]Demobesin 4 ([(99m)Tc]DB4) in prostate cancer patients.
[(99m)Tc]DB4 was prepared according to Good Manufacturing Practice. Patients with prostate cancer underwent serial planar and SPECT imaging up to 3 h after administration. Blood and urine samples were taken to assess pharmacokinetics.
[(99m)Tc]DB4 is safe and clears rapidly from the bloodstream via the kidneys resulting in low background activity. The tracer binds strongly to the gastrin-releasing peptide receptor (GRPR) in vivo as indicated by the high uptake in the pancreas seen in all patients. In patients who had undergone hormone therapy, [(99m)Tc]DB4 did not efficiently image metastatic prostate cancer. In contrast, in newly diagnosed patients local disease was visualised.
The GRPR is an unsuitable target for imaging refractory prostate cancer but may be useful in untreated disease. [(99m)Tc]DB4 is a promising radiopharmaceutical which merits further exploration in this specific group of patients.
我们研究了蛙皮素受体的成像，并评估了[（99m）Tc]去甲蛙皮素4（[（99m）Tc]DB4）在前列腺癌患者中的临床应用。
[（99m）Tc]DB4按照药品生产质量管理规范制备。前列腺癌患者在给药后3小时内接受了系列平面和SPECT成像。采集血液和尿液样本以评估药代动力学。
[（99m）Tc]DB4安全，通过肾脏迅速从血液中清除，导致本底活性较低。如所有患者胰腺中高摄取所示，该示踪剂在体内与胃泌素释放肽受体（GRPR）强烈结合。在接受过激素治疗的患者中，[（99m）Tc]DB4不能有效地对转移性前列腺癌进行成像。相比之下，在新诊断的患者中，局部疾病可以显影。
GRPR不是难治性前列腺癌成像的合适靶点，但可能对未治疗的疾病有用。[（99m）Tc]DB4是一种有前景的放射性药物，值得在这一特定患者群体中进一步探索。
