Unit of Nuclear Medicine, Fondazione Policlinico Universitario A. Gemelli IRCCS, Roma, Italy.
Institute of Nuclear Medicine, Università Cattolica del Sacro Cuore, Roma, Italy.
Curr Radiopharm. 2022;15(1):32-39. doi: 10.2174/1874471013999210104220031.
Nimotuzumab is a humanized anti-epidermal growth factor receptor (EGFR) monoclonal antibody, nowadays used for tumour immunochemotherapy. This study aimed to label the conjugate DOTA-nimotuzumab with yttrium-90, in order to provide a β- emitting radioimmunoconjugate (Y-DOTA-nimotuzumab) potentially useful to assess the feasibility of a new radio-guided surgery approach.
The synthesis of 90Y-DOTA-nimotuzumab was performed in two days. Nimotuzumab was conjugated with a 50-fold excess of DOTA and then labelled with 90Y3+. The Y-DOTA-nimotuzumab preparation was optimized considering several parameters such as pH, temperature and reaction volume. Moreover, the Y-DOTA-nimotuzumab stability was evaluated in human plasma.
The radioimmunoconjugate Y-DOTA-nimotuzumab was obtained with a radiochemical purity greater than 96%, and showed a good stability at 20°C as well as at 37°C in human plasma.
The optimized conditions for a mild and easy preparation of Y-DOTA-nimotuzumab joined to a promising stability under physiological conditions suggest to propose this radioimmunoconjugate as a potential diagnostic radiopharmaceutical for β- radio-guided surgery.
尼妥珠单抗是一种人源化抗表皮生长因子受体（EGFR）单克隆抗体，目前用于肿瘤免疫化疗。本研究旨在标记偶联物 DOTA-尼妥珠单抗与钇-90，以提供一种可能有用的β发射放射性免疫偶联物（Y-DOTA-尼妥珠单抗），用于评估新的放射性引导手术方法的可行性。
在两天内完成了 90Y-DOTA-尼妥珠单抗的合成。尼妥珠单抗与 DOTA 的 50 倍过量偶联，然后用 90Y3+标记。考虑到 pH 值、温度和反应体积等多个参数，对 Y-DOTA-尼妥珠单抗的制备进行了优化。此外，还评估了 Y-DOTA-尼妥珠单抗在人血浆中的稳定性。
放射性免疫偶联物 Y-DOTA-尼妥珠单抗的放射化学纯度大于 96%，在 20°C 以及在 37°C 下的人血浆中均表现出良好的稳定性。
优化的条件用于温和且易于制备 Y-DOTA-尼妥珠单抗，并在生理条件下具有有前途的稳定性，这表明该放射性免疫偶联物可作为β放射性引导手术的潜在诊断放射性药物。
