Novel Preclinical and Radiopharmaceutical Aspects of [68Ga]Ga-PSMA-HBED-CC: A New PET Tracer for Imaging of Prostate Cancer.
Novel Preclinical and Radiopharmaceutical Aspects of [68Ga]Ga-PSMA-HBED-CC: A New PET Tracer for Imaging of Prostate Cancer.
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[68Ga]Ga-PSMA-HBED-CC 的新临床前和放射性药物方面：一种用于前列腺癌成像的新 PET 示踪剂。
DOI：
10.3390/ph7070779
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发表时间：
2014-06-30
期刊：
影响因子：
--
通讯作者：
Kopka K
中科院分区：
文献类型：
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作者：
Eder M;Neels O;Müller M;Bauder-Wüst U;Remde Y;Schäfer M;Hennrich U;Eisenhut M;Afshar-Oromieh A;Haberkorn U;Kopka K
通过前列腺特异性膜抗原（PSMA）的PET成像检测前列腺癌病变在过去几年中获得了最高的临床影响。68Ga标记的gluu -urea- lys (Ahx)-HBED-CC （[68Ga]Ga-PSMA-HBED-CC）代表了一种成功的新型PSMA抑制剂放射性示踪剂，最近在个体首次人体研究中证明了其适用性。该分子中使用的放射性金属螯合剂HBED-CC是一种很少使用的无环络合剂，其化学特性有利于影响PSMA抑制剂的生物功能。用放射性金属螯合剂DOTA简单地替代HBED-CC，可以显著降低相应68ga标记的PSMA靶向示踪剂的体内成像质量，证明HBED-CC本质上有助于PSMA与gluu -urea- lys （Ahx）药效团的结合。由于临床影响日益明显，本研究旨在反映HBED-CC作为无环放射性金属螯合剂的特性，并介绍[68Ga]Ga-PSMA-HBED-CC放射药物生产过程的新临床前数据和相关方面。
The detection of prostate cancer lesions by PET imaging of the prostate-specific membrane antigen (PSMA) has gained highest clinical impact during the last years. 68Ga-labelled Glu-urea-Lys(Ahx)-HBED-CC ([68Ga]Ga-PSMA-HBED-CC) represents a successful novel PSMA inhibitor radiotracer which has recently demonstrated its suitability in individual first-in-man studies. The radiometal chelator HBED-CC used in this molecule represents a rather rarely used acyclic complexing agent with chemical characteristics favourably influencing the biological functionality of the PSMA inhibitor. The simple replacement of HBED-CC by the prominent radiometal chelator DOTA was shown to dramatically reduce the in vivo imaging quality of the respective 68Ga-labelled PSMA-targeted tracer proving that HBED-CC contributes intrinsically to the PSMA binding of the Glu-urea-Lys(Ahx) pharmacophore. Owing to the obvious growing clinical impact, this work aims to reflect the properties of HBED-CC as acyclic radiometal chelator and presents novel preclinical data and relevant aspects of the radiopharmaceutical production process of [68Ga]Ga-PSMA-HBED-CC.