Orhon Pauline, Desruet Marie-Dominique, Piquemal Marie, De Leiris Nicolas, Djaileb Loïc, Vuillez Jean-Philippe, Bedouch Pierrick, Leenhardt Julien
Pharmacy Department, Grenoble Alpes University Hospital, 38000 Grenoble, France.
LRB, CHU Grenoble Alpes, INSERM, Grenoble Alpes University, 38000 Grenoble, France.
Pharmaceuticals (Basel). 2022 Apr 24;15(5):522. doi: 10.3390/ph15050522.
Prostate Specific Membrane Antigen (PSMA) is a highly relevant target in nuclear medicine due to its overexpression in prostate cancer. The Ga/Lu-PSMA-1 combination is a theranostic agent for the detection and treatment of tumors overexpressing the PSMA target. Specifically, Lu-PSMA-1 is used in the treatment of castration-resistant prostate cancer that is ineffective or intolerant to the latest generation of chemotherapy and/or hormone therapy. This radiopharmaceutical is manufactured in a radiopharmaceutical synthesizing unit and must pass a quality control where the radiochemical purity (RCP) is assessed prior to release of the batch. RCP evaluation is performed by high-performance liquid chromatography (HPLC) and thin-layer chromatography (TLC). Since there is no monograph for Lu-PSMA-1 in the European Pharmacopoeia, we validate the analytical methods according to the EANM recommendations adapted from ICH Q2. Specificity, linearity, accuracy, precision, intermediate precision, limit of quantification (LOQ) and robustness were described for HPLC and TLC in this study. The results obtained demonstrated the robustness and reliability of the HPLC and TLC analytical methods for the evaluation of the RCP of Lu-PSMA-1.
前列腺特异性膜抗原（PSMA）因其在前列腺癌中过度表达，成为核医学中一个高度相关的靶点。镓/镥-PSMA-1复合物是一种用于检测和治疗过度表达PSMA靶点肿瘤的诊疗剂。具体而言，镥-PSMA-1用于治疗对最新一代化疗和/或激素治疗无效或不耐受的去势抵抗性前列腺癌。这种放射性药物在放射性药物合成单元中生产，并且在批次放行前必须通过质量控制，其中要评估放射化学纯度（RCP）。RCP评估通过高效液相色谱法（HPLC）和薄层色谱法（TLC）进行。由于欧洲药典中没有镥-PSMA-1的专论，我们根据改编自ICH Q2的欧洲核医学协会（EANM）建议对分析方法进行验证。本研究描述了HPLC和TLC的特异性、线性、准确性、精密度、中间精密度、定量限（LOQ）和稳健性。所得结果证明了HPLC和TLC分析方法在评估镥-PSMA-1的RCP方面的稳健性和可靠性。
