College of Pharmacy, University of New Mexico, Albuquerque, NM 87131, USA.
Bioorg Med Chem Lett. 2013 Apr 15;23(8):2319-23. doi: 10.1016/j.bmcl.2013.02.069. Epub 2013 Feb 24.
The purpose of this study was to determine the melanoma targeting property of (177)Lu-DOTA-GGNle-CycMSHhex in B16/F1 melanoma-bearing C57 mice. (177)Lu-DOTA-GGNle-CycMSHhex exhibited high receptor-mediated melanoma uptake and fast urinary clearance. The tumor uptake of (177)Lu-DOTA-GGNle-CycMSHhex was 20.25 ± 4.59 and 21.63 ± 6.27% ID/g at 0.5 and 2h post-injection, respectively. Approximately 83% of injected dose cleared out the body via urinary system at 2h post-injection. (177)Lu-DOTA-GGNle-CycMSHhex showed high tumor to normal organ uptake ratios except for the kidneys. The tumor/kidney uptake ratios of (177)Lu-DOTA-GGNle-CycMSHhex were 2.76 and 1.74 at 2 and 24h post-injection. The melanoma lesions were clearly visualized by SPECT/CT using (177)Lu-DOTA-GGNle-CycMSHhex as an imaging probe at 2h post-injection. Overall, high melanoma uptake coupled with fast urinary clearance of (177)Lu-DOTA-GGNle-CycMSHhex underscored its potential for melanoma treatment in the future.
这项研究的目的是确定 (177)Lu-DOTA-GGNle-CycMSHhex 在 B16/F1 黑色素瘤荷瘤 C57 小鼠中的黑色素瘤靶向特性。(177)Lu-DOTA-GGNle-CycMSHhex 表现出高受体介导的黑色素瘤摄取和快速尿液清除。(177)Lu-DOTA-GGNle-CycMSHhex 在 0.5 和 2 小时时的肿瘤摄取率分别为 20.25 ± 4.59 和 21.63 ± 6.27% ID/g。大约 83%的注射剂量在 2 小时后通过泌尿系统排出体外。(177)Lu-DOTA-GGNle-CycMSHhex 除肾脏外，对肿瘤与正常器官的摄取比值均较高。(177)Lu-DOTA-GGNle-CycMSHhex 在 2 和 24 小时时的肿瘤/肾脏摄取比值分别为 2.76 和 1.74。使用 (177)Lu-DOTA-GGNle-CycMSHhex 作为成像探针，在 2 小时时 SPECT/CT 可清晰显示黑色素瘤病灶。总之，(177)Lu-DOTA-GGNle-CycMSHhex 具有较高的黑色素瘤摄取率和快速的尿液清除率，这突出了其在未来用于黑色素瘤治疗的潜力。
