Department of Nuclear Medicine, PGIMER, Chandigarh.
Isotope Production and Application Division, Bhabha Atomic Research Centre (BARC), Mumbai.
Nucl Med Commun. 2020 Dec;41(12):1250-1256. doi: 10.1097/MNM.0000000000001282.
Radiolabeled RGD peptide can be used for noninvasive in vivo imaging of αvβ3 integrin receptors leading to early detection of tumor cells and hence improving the clinical outcomes. In the present study single vial kit based HYNIC RGD2 was radiolabeled with Tc-99m and evaluated in patients with breast carcinoma.
Radiolabeling was performed via bifunctional chelator method. Tc-99m 1110-2960 MBq (30-80 mCi) was added to the HYNIC-RGD2 vial. The reaction mixture was heated for 20 minutes at 100°C. After performing the quality checks, whole-body planar imaging was performed in 20 patients at 2-2.5 h post i.v. injection of 555-740 MBq (15-20 mCi) of the radiotracer.
Radiolabeling yield of ≥98% was observed in all the formulations. Quality control tests indicated the suitability of radiopharmaceutical for intravenous administration. Physiological uptake of Tc-99m HYNIC-RGD2 was observed in the nasopharynx, salivary glands, liver, spleen, and intestine. Good uptake of radiotracer was observed in breast lesions of 18 patients. Two patients were observed to be negative. Increased uptake was also seen in metastatic sites in two patients and in lymph nodes in three patients. Scintigraphy findings were in corroboration with pathological observations.
The single vial cold kit based radiolabeling of Tc-99m HYNIC-RGD2 is facile leading to its easy availability. Tc-99m HYNIC-RGD2 is a promising radiopharmaceutical which can be used for the molecular imaging of angiogenesis in breast carcinoma patients.
放射性标记的 RGD 肽可用于 αvβ3 整合素受体的非侵入性体内成像，从而早期检测肿瘤细胞，进而改善临床结局。在本研究中，基于单瓶试剂盒的 HYNIC-RGD2 采用双功能螯合剂法进行放射性标记，并在乳腺癌患者中进行了评估。
放射性标记通过双功能螯合剂法进行。将 Tc-99m 1110-2960MBq（30-80mCi）加入 HYNIC-RGD2 小瓶中。将反应混合物在 100°C 下加热 20 分钟。完成质量检查后，在静脉注射 555-740MBq（15-20mCi）放射性示踪剂后 2-2.5 小时，对 20 例患者进行全身平面显像。
所有配方均观察到放射性标记产率≥98%。质量控制测试表明放射性药物适合静脉给药。Tc-99m HYNIC-RGD2 在鼻咽、唾液腺、肝脏、脾脏和肠道中观察到生理性摄取。18 例患者的乳腺病变观察到良好的摄取。2 例患者观察为阴性。在 2 例患者的转移部位和 3 例患者的淋巴结中也观察到摄取增加。闪烁显像结果与病理观察结果相符。
基于单瓶冷试剂盒的 Tc-99m HYNIC-RGD2 放射性标记简便易行，易于获得。Tc-99m HYNIC-RGD2 是一种有前途的放射性药物，可用于乳腺癌患者血管生成的分子成像。
