Melanoma targeting property of a Lu-177-labeled lactam bridge-cyclized alpha-MSH peptide |
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| Authors: | Haixun Guo Yubin Miao |
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| Institution: | 1. College of Pharmacy, University of New Mexico, Albuquerque, NM 87131, USA;2. Cancer Research and Treatment Center, University of New Mexico, Albuquerque, NM 87131, USA;3. Department of Dermatology, University of New Mexico, Albuquerque, NM 87131, USA |
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| Abstract: | The purpose of this study was to determine the melanoma targeting property of 177Lu-DOTA-GGNle-CycMSHhex in B16/F1 melanoma-bearing C57 mice. 177Lu-DOTA-GGNle-CycMSHhex exhibited high receptor-mediated melanoma uptake and fast urinary clearance. The tumor uptake of 177Lu-DOTA-GGNle-CycMSHhex was 20.25 ± 4.59 and 21.63 ± 6.27% ID/g at 0.5 and 2 h post-injection, respectively. Approximately 83% of injected dose cleared out the body via urinary system at 2 h post-injection. 177Lu-DOTA-GGNle-CycMSHhex showed high tumor to normal organ uptake ratios except for the kidneys. The tumor/kidney uptake ratios of 177Lu-DOTA-GGNle-CycMSHhex were 2.76 and 1.74 at 2 and 24 h post-injection. The melanoma lesions were clearly visualized by SPECT/CT using 177Lu-DOTA-GGNle-CycMSHhex as an imaging probe at 2 h post-injection. Overall, high melanoma uptake coupled with fast urinary clearance of 177Lu-DOTA-GGNle-CycMSHhex underscored its potential for melanoma treatment in the future. |
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