Moltek A.S. Gebze Organize Sanayi, 41400 Gebze, Kocaeli, Turkey.
Curr Radiopharm. 2022;15(1):76-83. doi: 10.2174/1874471014666210528123936.
The synthesis of Actinium derivatives was afforded by using PSMA- 617, DOTATATE peptides, and EDTMP ligand. Detailed experiments, quality control (QC), and stability studies were also well described. The radiolabelling reactions were performed in mild conditions with desirable radiochemical yields and high radiochemical purities.
PSMA-617, DOTATATE were radiolabelled with Actinium in 0.1 M HCl in the presence of ascorbate buffer solution and passed through the C-18 light cartridge for purification and the product was eluted by ethanol-water solution. EDTMP was also radiolabelled with Actinium without using any stabilizer and purification step. All products were well analyzed by R-TLC and R-HPLC. The stability of those compounds was also studied within the validity period of time.
Ac-DOTATATE and 225Ac-PSMA-617 were obtained at the same condition. The radiochemical yield of 225Ac-DOTATATE was less thanAc-PSMA 617. The stability experiments indicating decay daughters of Actinium appeared after T0 +1 h due to the recoil effect radiolysis. On the other hand, Ac-EDTMP was more stable than DOTA-peptide radiolabelled compounds. Ac-EDTMP was produced with more than 95% radiochemical yield and 99% radiochemical purity.
A detailed chemistry study was presented for the synthesis of Actinium derivatives in mild conditions with absolute radiochemical purities and high yields. The experimental results showed that Ac-EDTMP could be a suitable radiopharmaceutical alternative for bone metastases arising from primer tumors as a cocktail therapy.
使用 PSMA-617、DOTATATE 肽和 EDTMP 配体合成锕系元素衍生物。详细的实验、质量控制 (QC) 和稳定性研究也得到了很好的描述。放射性标记反应在温和条件下进行，具有理想的放射化学产率和高放射化学纯度。
PSMA-617、DOTATATE 在 0.1 M HCl 中用锕系元素标记，在抗坏血酸缓冲溶液存在下进行，并通过 C-18 轻柱进行纯化，产物用乙醇-水溶液洗脱。EDTMP 也无需使用任何稳定剂和纯化步骤即可与锕系元素标记。所有产品均通过 R-TLC 和 R-HPLC 进行了很好的分析。还在有效期内研究了这些化合物的稳定性。
在相同条件下获得了 Ac-DOTATATE 和 225Ac-PSMA-617。225Ac-DOTATATE 的放射化学产率低于 Ac-PSMA 617。稳定性实验表明，由于反冲效应辐射分解，锕系元素的衰变子在 T0 +1 h 后出现。另一方面，Ac-EDTMP 比 DOTA-肽标记化合物更稳定。Ac-EDTMP 的放射化学产率超过 95%，放射化学纯度超过 99%。
在温和条件下，用绝对放射化学纯度和高收率对锕系元素衍生物的合成进行了详细的化学研究。实验结果表明，Ac-EDTMP 可以作为源自原发病灶的骨转移的鸡尾酒疗法的合适放射性药物替代品。
