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腾讯登录JNM：新型分子成像药物有助更好地诊断前列腺癌
| 导读 | 一项刊登于国际杂志The Journal of Nuclear Medicine上的论文中，研究人员开发了一种新型分子成像药物可以对早期前列腺癌进行检测及成像，文章中研究人员对比了两种Tc-99m标记配体：MIP-1404及MIP-1405的生物分布及肿瘤吸收的动力学数据，这几种药物用于单光子发射计算机化断层显像（SPECT）及平面成像。 |
一项刊登于国际杂志The Journal of Nuclear Medicine上的研究论文中，研究人员开发了一种新型分子成像药物可以对早期前列腺癌进行检测及成像，文章中研究人员对比了两种Tc-99m标记配体：MIP-1404及MIP-1405的生物分布及肿瘤吸收的动力学数据，这几种药物用于单光子发射计算机化断层显像（SPECT）及平面成像。
前列腺癌是美国最为常见的非皮肤类癌症，其也是引发美国男性因癌死亡的第二大杀手，据估计2014年美国有23.3万前列腺癌新增病例，而大约有2.9万人死于该疾病；目前在美国有超过200万前列腺癌患者。文章中研究人员通过对6名健康男性及6名X线影像确证的转移性前列腺癌患者进行研究，对比了两种Tc-99m标记配体：MIP-1404及MIP-1405在研究对象机体中的药代动力学、生物分布及肿瘤吸收的动力学数据，随后研究人员在10分钟、1小时、2小时、4小时及24小时对研究对象进行全身照像，在药物注射后3-4小时进行SPECT显像，在本文研究之前，基于SPECT及平面成像技术并没有单一靶向特殊的Tc-99m放射性药物可以对软组织、淋巴结、骨组织（转移性癌细胞）中的前列腺癌进行成像。
研究者Shankar Vallabhajosula说道，本文研究展示了一种创新性的前列腺癌平面和SPECT成像技术，其可以满足当前临床中所需的敏感性及选择性成像的要求。对于成像而言，健康志愿者中正常前列腺组织病灶药物摄入的缺失或可阐明前列腺特异性膜抗原(Prostate Specific Membrane Antigen)或许可以作为前列腺癌检测和成像的一种新型靶点。
研究者表示，Tc-99m MIP-1404或许具有更好的药代动力学及生物分布性，其可以对淋巴结、软组织及骨组织中的前列腺癌进行精确地成像。目前研究人员已经完成了对100名患者进行的Tc-99m MIP-1404多中心II期临床研究，后期研究人员计划进行III期临床试验来进行更为深入的研究。（转化医学网360zhyx.com）
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转化医学网推荐的原文摘要：
The Journal of Nuclear Medicine doi: 10.2967/jnumed.114.140426
Shankar Vallabhajosula1, Anastasia Nikolopoulou1, John W. Babich2, Joseph R. Osborne1, Scott T. Tagawa1, Irina Lipai1, Lilja Solnes1, Kevin P. Maresca2, Thomas Armor2, John L. Joyal2, Robert Crummet2, James B. Stubbs3 and Stanley J. Goldsmith1
Prostate-specific membrane antigen (PSMA) is a well-established target for developing radiopharmaceuticals for imaging and therapy of prostate cancer (PCa). We have recently reported that novel 99mTc-labeled small-molecule PSMA inhibitors bind with high affinity to PSMA-positive tumor cells in vitro and localize in PCa xenografts. This study reports the first, to our knowledge, human data in men with metastatic PCa and in healthy male subjects. Methods: Under an exploratory investigational new drug, using a cross-over design, we compared the pharmacokinetics, biodistribution, and tumor uptake of 99mTc-MIP-1404 and 99mTc-MIP-1405 in 6 healthy men and 6 men with radiographic evidence of metastatic PCa. Whole-body images were obtained at 10 min and 1, 2, 4, and 24 h. SPECT was performed between 3 and 4 h after injection. Results: Both agents cleared the blood rapidly, with MIP-1404 demonstrating significantly lower urinary activity (7%) than MIP-1405 (26%). Both agents showed persistent uptake in the salivary, lacrimal, and parotid glands. Uptake in the liver and kidney was acceptable for imaging at 1–2 h. In men with PCa, both agents rapidly localized in bone and lymph node lesions as early as 1 h. SPECT demonstrated excellent lesion contrast. Good correlation was seen with bone scanning; however, more lesions were demonstrated with 99mTc-MIP-1404 and 99mTc-MIP-1405. The high-contrast images exhibited tumor-to-background ratios from 3:1 to 9:1 at 4 and 20 h. Conclusion: Compared with the standard-of-care bone scanning, 99mTc-MIP-1404 and 99mTc-MIP-1405 identified most bone metastatic lesions and rapidly detected soft-tissue PCa lesions including subcentimeter lymph nodes. Because 99mTc-MIP-1404 has minimal activity in the bladder, further work is planned to correlate imaging findings with histopathology in patients with high-risk metastatic PCa.
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