Synthesis and evaluation of a novel 68Ga-labeled DOTA-benzamide derivative for malignant melanoma imaging

Malignant melanoma displays a highly aggressive metastasis. Thus, early diagnosis of malignant melanoma is important for patient survival. We designed and synthesized a novel 68Ga-labeled benzamide derivative that specifically binds to melanoma as demonstrated by its ability to bind to melanin. 68Ga-SCN-DOTA-PCA was synthesized with a radiochemical yield of ∼80% and a radiochemical purity of >97% by analytical HPLC. The in vitro binding of 68Ga-SCN-DOTA-PCA to melanin and its cellular uptake demonstrated the selective uptake in melanin. In addition, the biodistribution and micro-PET imaging of 68Ga-SCN-DOTA-PCA in B16F10 tumor models showed the specific accumulation in melanoma. These results suggest that 68Ga-SCN-DOTA-PCA would be a promising agent for melanoma diagnosis.

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