Page 24 - 分子轉譯影像中心季刊 IX
P. 24

討論與結論:

          本實驗設計的6種正子放射性追蹤劑在LNCaP細胞上皆表現很高的親和性(4-
     36nM),並在LNCaP異種移植老鼠的腫瘤上有很高的吸收值(>5%ID/g)。此6種
                                                                                    68
     新的正子放射性追蹤劑與目前臨床廣泛使用的PSMA影像探針:[ Ga]Ga-PSMA-
     HBEDCC,和現行正在進行臨床試驗的放射性追蹤劑:                                         18 F-DCFPyL相比較,             18 F-
     RPS-040和 F-RPS-041展示很高的腫瘤吸收(>10%ID/g)與很高的腫瘤/背景比
                    18
     值和腫瘤/腎臟比值。本篇研究使用簡單放射合成方法得到高產率 F標誌PSMA
                                                                                       18
     受體,並在體內體外試驗中皆得到很有希望的結果,使得此種新藥值得在臨床前
     列腺癌正子影像上發展研究。



     參考文獻:

     1. Nikolopoulou A, Amor-Coarasa A, Kelly J, Vallabhajosula V,Babich J. Comparative
         evaluation of 68Ga-labeled urea-based PSMA ligands in LNCaP tumor bearing mice.
         J Nucl Med.2015;56(no. supplement 3):114.

     2. Hillier SM, Maresca KP, Lu G, Merkin RD, Marquis JC,Zimmerman CN, et al. 99mTc-
         labeled small-molecule inhibitors of prostate-specific membrane antigen for
         molecular imaging of prostate cancer. J Nucl Med. 2013;54:1369–76.

     3. Maresca KP, Hillier SM, Femia FJ, Barone DKC, Joyal JL, Zimmerman CN, et al. A Series
         of halogenated heterodimeric inhibitors of prostate specific membrane antigen
         (PSMA)     as    radiolabeled     probes    for   targeting     prostate    cancer.    J  Med
         Chem.2009;52:347–57.


     4. Srinivasarao M, Galliford CV, Low PS. Principles in the design of ligand-targeted
         cancer therapeutics and imaging agents. Nat Rev Drug Discov. 2015;14:203–19.
   19   20   21   22   23   24   25   26   27   28   29