99mTc labeled VIP analog:: evaluation for imaging colorectal cancer
99mTc labeled VIP analog:: evaluation for imaging colorectal cancer
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DOI：
10.1016/s0969-8051(01)00205-0
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发表时间：
2001-05-01
影响因子：
3.1
通讯作者：
Marcus, CS
中科院分区：
文献类型：
--
作者：
Rao, PS;Thakur, ML;Marcus, CS
结直肠癌的早期可靠诊断仍然是一项艰巨而具有挑战性的工作。结肠癌细胞高密度表达血管活性肠肽(VIP)受体。我们已经制备了一种VIP类似物(TP3654)，用~(99)Tc标记它，并在动物实验中评价了它作为结直肠癌显像剂的作用。本文比较了99m-TP3654与In-111-DTPA-Octrebon和Tc-99m-抗CEA在荷人结肠癌LS174T裸鼠体内的组织分布。最后，在4名正常人体内进行了TC-99m-TP3654的药代动力学和组织分布研究。数据表明，在不损失其受体特异性和生物活性的情况下，可以有效地制备TC-99m-TP3654。虽然在所用动物模型中24小时的肿瘤摄取适中(0.21+/-0.07%i.d./g)，但组织分布图比In-111-DTPA-Octrebon或Tc-99m-anti-CEA扫描更有利。人体研究表明，99m-Tp3654对任何受试者均无不良影响。在24小时内，大约70%的注射剂量通过肾脏清除，大约20%通过肝胆系统清除。在这些非禁食志愿者中，肝胆清除缓慢，而在癌症患者中，肿瘤摄取很快。资料表明，~(99m)Tc-TP3654是一种很有前途的结直肠癌显像剂。(C)2001 Elsevier Science Inc.保留所有权利。
Early and reliable diagnosis of colorectal cancer continues to be demanding and challenging. Colorectal cancer cells express Vasoactive Intestinal Peptide (VIP) receptors in high density. We have prepared a VIP analog (TP3654), labeled it with Tc-99m, and evaluated it in experimental animals as an agent for imaging colorectal cancer. The tissue distribution of Tc-99m-TP3654 has been compared with that of In-111-DTPA-Octreotide and Tc-99m-anti-CEA scan in nude mice bearing human colorectal cancer LS174T. Finally, pharmacokinetic and tissue distribution studies of Tc-99m-TP3654 have been performed in four normal human volunteers. Data suggest that Tc-99m-TP3654 can be prepared efficiently without loss of its receptor specificity and biological activity. Although the 24 hr tumor uptake of Tc-99m-TP3654 in the animal model used was modest (0.21 +/- 0.07% I.D./g), the tissue distribution profile was more favorable than that of In-111-DTPA-Octreotide or Tc-99m-anti-CEA scan. Human studies indicated that Tc-99m-TP3654 had no adverse effect in any subject. Within 24 hours, approximately 70% of the injected dose cleared through the kidneys, and approximately 20% through the hepatobiliary system. In these non-fasting Volunteers hepatobiliary clearance was slow and in cancer patients tumor uptake was rapid. Data suggest that Tc-99m-TP3654 is a promising agent for imaging colorectal cancer. (C) 2001 Elsevier Science Inc. All rights reserved.