Abstract:
UNASSIGNED: Prostate cancer (PC) is the most common type of cancer in elderly men, with a positive correlation with age. As resistance to treatment has developed, particularly in the progressive stage of the disease and in the presence of microfocal multiple bone metastases, new generation radionuclide therapies have emerged. Recently, [161Tb], a radiolanthanide introduced for treating micrometastatic foci, has shown great promise for treating prostate cancer.
UNASSIGNED: In this study, Terbium-161 [161Tb]Tb was radiolabeled with prostate-specific membrane antigen (PSMA)-617 ([161Tb]-PSMA-617) and the therapeutic efficacy of the radiolabeled compound investigated in vitro and in vivo. [161Tb]-PSMA-617 was found to have a radiochemical yield of 97.99 ± 2.01% and was hydrophilic. [161Tb]-PSMA-617 was also shown to have good stability, with a radiochemical yield of over 95% up to 72 hours. In vitro, [161Tb]-PSMA-617 showed a cytotoxic effect on LNCaP cells but not on PC-3 cells. In vivo, scintigraphy imaging visualized the accumulation of [161Tb]-PSMA-617 in the prostate, kidneys, and bladder.
UNASSIGNED: The results suggest that [161Tb]-PSMA-617 can be an effective radiolabeled agent for the treatment of PSMA positive foci in prostate cancer.
摘要:
背景前列腺癌(PC)是老年男性最常见的癌症类型,与年龄呈正相关。随着对治疗的抵抗力的发展,特别是在疾病的进展阶段和存在微病灶多发性骨转移的情况下,新一代放射性核素疗法已经出现。最近,[161TB],一种为治疗微转移灶而引入的radiolanthanide,在治疗前列腺癌方面显示出巨大的希望。结果在这项研究中,用前列腺特异性膜抗原(PSMA)-617([161Tb]-PSMA-617)放射性标记and161[161Tb]Tb,并在体外和体内研究放射性标记化合物的治疗功效。发现[161Tb]-PSMA-617具有97.99±2.01%的放射化学产率并且是亲水性的。[161TB]-PSMA-617也显示出良好的稳定性,长达72小时的放射化学产率超过95%。体外,[161Tb]-PSMA-617对LNCaP细胞但对PC-3细胞不显示细胞毒性作用。在体内,闪烁扫描成像显示[161Tb]-PSMA-617在前列腺中的积累,肾脏,和膀胱。结论[161Tb]-PSMA-617是一种有效的前列腺癌PSMA阳性病灶的放射性标记药物。