肿瘤显像药物18F-FLT的制备及其在早期肺癌与炎症鉴别中的应用研究

The Synthesis of 18F-FLT and its Application in the Differential Diagnosis of Early Lung Cancer and Inflammation

目的 早期肺癌与炎症的鉴别一直是困扰临床的一大难题,目前常用的反映糖代谢的显像药物18F-FDG难以满足临床需求。本研究拟合成反映肿瘤增殖的显像药物18F-FLT,用于早期肺癌与炎症的鉴别诊断。方法 以3-N-t-叔丁氧羰基-1-[5’-O-(4,4’-二甲氧基三苯甲基)-2’-脱氧-3’-O-(4-硝基苯磺酰基)-β-D-苏型-呋喃戊糖基]胸苷为前体,通过TracerlabFXNPro合成模块自动化合成18F-FLT并进行完整的质量控制。筛选5例早期肺癌患者进行18F-FLT和18F-FDG的对比显像。结果 18F-FLT放化产率为(12.2±1.5)%(n=5),纯度>99%,其它质控项目均满足临床要求。PET显像结果显示,有3例患者18F-FLT和18F-FDG显像结果一致,2例患者显像结果有显著差异,活检病理证实18F-FLT对肺癌组织显像,而对炎症不敏感。结论 本研究合成的18F-FLT质量符合放射性药物注射要求,并具有鉴别早期肺癌和炎症的临床价值。

Objective It's difficult to differentiate early lung cancer and inflammation in clinical practice but 18F-FDG cannot meet the clinical needs now. This study intends to synthesize 18F-FLT, a tumor proliferation imaging drug, to research its potential in differentiating early lung cancer and inflammation. Methods In this study,(5'-O-DMTr-2'-deoxy-3'-O-nosyl-β-D-threo-pentofuranosyl)-3-N-BOCthymine was used as the precursor, and 18F-FLT was synthesized automatically by Tracerlab FXN Pro synthesis module. After quality control was carried out, 5 early lung cancer patients were screened out for 18F-FLT and 18F-FDG PET imaging contrast. Results The radiochemical yield of 18F-FLT was (12.2±1.5, n=5)%, and the radiochemical purity was more than 99%. Comparing the 18F-FLT and 18F-FDG PET images, the imaging results of 3 patients were coincident but different of 2 patients. Moreover, pathology results confirmed that 18F-FLT was sensitive to early lung cancer, but not sensitive to inflammation. Conclusion 18F-FLT was synthesized successfully. It has the potential of distinguishing early lung cancer from inflammation.