Clinical evaluation of kit based Tc-99m-HYNIC-RGD2 for imaging angiogenesis in breast carcinoma patients

Background 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. Methods 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. Results 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. Conclusion 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.