CEA, I2BM, LDM-TEP, UMR 6301 ISTCT, GIP Cyceron, 14074 Caen, France.
Mol Imaging Biol. 2013 Feb;15(1):12-8. doi: 10.1007/s11307-012-0574-y.
[(18)F]ML-10 is the most advanced radiopharmaceutical for the clinical imaging of the apoptosis phenomenon by PET. The preparation of this radiopharmaceutical on a commercial radiosynthesis module and the requested quality controls for its release are presented herein.
ML-10 as reference and its mesyloxy derivative as precursor for labelling with fluorine-18 were prepared. [(18)F]ML-10 was synthesized via a [(18)F]fluorine-de-mesyloxy aliphatic nucleophilic substitution via a GE TRACERLab® FX-FN module. Quality controls were performed.
The labelling precursor was obtained in a four step synthesis in 28 % overall yield affording ML-10 in two steps (88 % yield). Pure [(18)F]ML-10 was obtained with a decay corrected yield of 39.8 % ± 8.4 % (n = 7) in 70 min and a specific activity of 235 ± 85 GBq/μmol at the end of synthesis.
[(18)F]ML-10 was prepared on a widely available automated module and passed the quality control. A LC/MS method was developed to measure specific radioactivity.
[(18)F]ML-10 是通过正电子发射断层扫描（PET）对细胞凋亡现象进行临床成像的最先进的放射性药物。本文介绍了该放射性药物在商业放射性合成模块上的制备以及放行所需的质量控制。
制备 ML-10 作为参考品及其甲氧基衍生物作为氟-18 标记的前体。通过 GE TRACERLab® FX-FN 模块，通过[(18)F]氟去甲氧基脂肪族亲核取代反应合成[(18)F]ML-10。进行了质量控制。
在四步合成中，以 28%的总收率获得标记前体，两步（88%收率）即可获得 ML-10。在合成结束时，经过衰变校正的[(18)F]ML-10 产率为 39.8%±8.4%（n=7），放射性比活度为 235±85GBq/μmol，获得了纯度[(18)F]ML-10。
[(18)F]ML-10 可在广泛应用的自动化模块上制备，并通过了质量控制。开发了一种 LC/MS 方法来测量比放射性活度。
