Early diagnosis and precise surgical intervention are crucial for cancer patients. We aimed to develop a novel positron emission tomography (PET)/fluorescence dual-modality probe for preoperative diagnosis, intraoperative guidance, and postoperative monitoring of fibroblast activation protein (FAP)-positive tumors. FAPI-FAM was synthesized and labeled with gallium-68. [Ga]Ga-FAPI-FAM showed favorable in vivo and in vitro characteristics, specific binding affinity, and excellent tumor accumulation in FAP-positive cells and mice xenografts. Excellent tumor-to-background contrast was found owing to high tumor uptake, prolonged retention, and rapid renal clearance of [Ga]Ga-FAPI-FAM. Moreover, a specific fluorescence signal was detected in FAP-positive tumors during ex vivo fluorescence imaging, demonstrating the feasibility of whole-body tumor detection and intraoperative tumor delineation.

中文翻译：

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一种新型PET/荧光双模态探针成纤维细胞活化蛋白的合成及临床前评价

早期诊断和精确的手术干预对于癌症患者至关重要。我们的目标是开发一种新型正电子发射断层扫描（PET）/荧光双模态探针，用于成纤维细胞激活蛋白（FAP）阳性肿瘤的术前诊断、术中指导和术后监测。合成FAPI-FAM并用镓68标记。 [Ga]Ga-FAPI-FAM 在 FAP 阳性细胞和小鼠异种移植物中表现出良好的体内和体外特性、特异性结合亲和力以及出色的肿瘤积累。由于 [Ga]Ga-FAPI-FAM 的高肿瘤摄取、长时间保留和快速肾脏清除，发现了优异的肿瘤与背景对比度。此外，在离体荧光成像过程中，在FAP阳性肿瘤中检测到特异性荧光信号，证明了全身肿瘤检测和术中肿瘤勾画的可行性。