99mTc-labeled vasoactive intestinal peptide analog for rapid localization of tumors in humans.
99mTc-labeled vasoactive intestinal peptide analog for rapid localization of tumors in humans.
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发表时间：
2000
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通讯作者：
Mathew L. Thakur;Carol S. Marcus;S. Saeed;V. Pallela;C. Minami;L. Diggles;H. Pham;R. Ahdoot;E. Kalinowski
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作者：
Mathew L. Thakur;Carol S. Marcus;S. Saeed;V. Pallela;C. Minami;L. Diggles;H. Pham;R. Ahdoot;E. Kalinowski
近年来，利用受体特异性生物分子对肿瘤进行成像已成为人们日益关注的焦点。血管活性肠肽（VIP）对在大量恶性肿瘤上高密度表达的特定受体具有高亲和力。 VIP 经过修饰 (TP 3654)，但不影响其生物活性，并用 99mTc 标记。在 3 名健康志愿者和 11 名有癌症病史的患者中进行了药代动力学和可行性研究。注射后进行长达 2 小时的成像。注射 99mTc-TP 3654 (370-555 MBq/5 microg) 后 24 小时内，大约 70% 的示踪剂通过肾脏清除，20% 通过肝脏清除。血液清除速度很快。任何受试者均未发现不良反应。所有已知肿瘤均在 20 分钟内清晰描绘。研究结果与 99mTc-甲氧基异丁基异腈、CT、MRI 或组织学结果进行比较。 9 名患者存在一致性。在另外 2 名患者中，只有 VIP 扫描对已知表达 VIP 受体的肿瘤呈阳性。使用 99mTc-VIP 进行肿瘤成像的早期结果令人鼓舞，值得进一步研究。
In recent years, imaging tumors with receptor-specific biomolecules has been the focus of increasing interest. Vasoactive intestinal peptide (VIP) has a high affinity for specific receptors that are expressed in high density on a large number of malignant tumors. VIP was modified (TP 3654) without compromising its biologic activity and labeled with 99mTc. Pharmacokinetics and feasibility studies were performed in 3 healthy volunteers and 11 patients with a history of cancer. Imaging was performed for up to 2 h after injection. Within 24 h after injection of 99mTc-TP 3654 (370-555 MBq/5 microg), approximately 70% of the tracer cleared through the kidneys and 20% through the liver. Blood clearance was rapid. No adverse reaction was noted in any subject. All known tumors were clearly delineated within 20 min. Findings were compared with the results of 99mTc-methoxyisobutyl isonitrile, CT, MRI, or histology. There was concordance in 9 patients. In the other 2 patients, only the VIP scan was positive for tumors known to express VIP receptors. The early results of imaging tumors with 99mTc-VIP are promising and warrant further study.