TY - JOUR T1 - <strong>Preparation and preliminary evaluation of novel prostate cancer diagnosis probe <sup>68</sup>Ga-DOTA-ANCP-PSMA</strong> JF - Journal of Nuclear Medicine JO - J Nucl Med SP - 3121 LP - 3121 VL - 61 IS - supplement 1 AU - Kai Wen AU - Ji Hu AU - Haiping Cui Y1 - 2020/05/01 UR - http://jnm.snmjournals.org/content/61/supplement_1/3121.abstract N2 - 3121Objectives: Prostate cancer has the second highest cancer mortality rate. Early treatment for prostate cancer is better. Therefore, searching effective diagnostic methods for early prostate cancer is the key to improve the cure rate and survival rate. As a specific target antigen for prostate cancer, PSMA has become an ideal target for localization diagnosis and efficacy detection. In order to develop a novel prostate cancer diagnosis probe with better properties both in vivo and in vitro 68Ga labeled PSMA target probe 68Ga-DOTA- ANCP-PSMA was designed and its preliminary evaluation were carried out. Methods: 68Ga nuclide was labeled directly, the labeling conditions such as temperature, pH and precursor concentration were tested respectively. The stability and octanol-water partition coefficient were determined. The biodistribution of normal mice and nude mice bearing LNCaP were determined. PET-CT imging experiments were also carried out. Results: The optimaized labeling conditions were confirmed that pH was 3.0-4.3, labeling temperature was 90-95℃, precursor concentration was not less than 20 μg/mL. The labeling yield could reach to more than 95% under the optimized labeling conditions. The purified l 68Ga-DOTA-ANCP-PSMA showed good vitro stability, radiochemical purity reached up to 95% both in the PBS system and the serum protein system over 2 hours. The octanol-water partition coefficient is -1.42 ± 0.02. The biodistribution showed that the laelled compound clear fast in blood, mainly through kidney metabolism. There were low uptakes in non-target organs such as the heart, lung and spleen. Bladder showed a high uptake, because the labeled compound mainly excreted through urine. Tumor showed high uptake. In PET-CT imaging studies, there was clear imaging in tumor, also showed good sensitivity and specificity in PET-CT block study. Conclusions: 68Ga-DOTA-ANCP-PSMA labelled derictly in 15min with 95% radiochemical purity. 68Ga-DOTA-ANCP-PSMA has good stability and proper lipotropy in vitro. 68Ga-DOTA-ANCP-PSMA shows better metabolism and high uptake in target tumor. This probe has good properties and promising potencial for the diagnosis of prostate cancer. Further studies are required to determine its full properties. ER -