报道了MC1-R靶向α-黑色素细胞刺激激素类似物(α-MSH)生物分子标记的α放射性金属的抗肿瘤体内治疗评估，用于治疗MC1-R阳性的黑色素瘤恶性(MM)。在MC1-R阳性的B16-F10黑色素瘤携带的C57BL/6J小鼠体内，对MC1-R亲和[213Bi]Bi-DOTA-NAPamide和HOLDamide治疗进行了抗肿瘤评估。在接种肿瘤细胞后的第6、8和10天，治疗组小鼠静脉注射约5MBq的两种酰胺衍生物。除了体重和肿瘤体积评估外，还进行了基于[68Ga]Ga-DOTA-HOLDamide和NAPamide的PET/MRI扫描和体外生物分布研究，分别在注射后的30分钟和90分钟进行。在PET/MRI成像研究中，B16-F10肿瘤以两种68Ga标记示踪剂清晰可见，然而通过使用[68Ga]Ga-DOTA-HOLDamide观察到明显较低的肿瘤-肌肉(T/M)比。α放射治疗后，对照组肿瘤的大小相对较大，而NAPamide治疗亚组在第10天观察到最小的肿瘤体积。相对较高的[213Bi]Bi-DOTA-NAPamide积聚在B16-F10肿瘤中(%ID/g: 2.71±0.15)，离散的背景活性导致出色的T/M比，特别是注射后90分钟。总的来说，MC1-R选择性的[213Bi]Bi-DOTA-NAPamide的治疗应用在MC1-R阳性MM管理中似乎是可行的。版权所有 © 2023. Elsevier B.V.发表。

Melanocortin-1 receptor (MC1-R) targeting alpha-melanocyte stimulating hormone-analogue (α-MSH) biomolecules labelled with α-emitting radiometal seem to be valuable in the targeted radionuclide therapy of MC1-R positive melanoma malignum (MM). Herein is reported the anti-tumor in vivo therapeutic evaluation of MC1-R-affine [213Bi]Bi-DOTA-NAPamide and HOLDamide treatment in MC1-R positive B16-F10 melanoma tumor-bearing C57BL/6J mice. On the 6th, 8th and 10th days post tumor cell inoculation; the treated groups of mice were intravenously injected with approximately 5 MBq of both amide derivatives. Beyond body weight and tumor volume assessment, [68Ga]Ga-DOTA-HOLDamide and NAPamide-based PET/MRI scans, and ex vivo biodistribution studies were executed 30,- and 90 minutes postinjection. In the PET/MRI imaging studies the B16-F10 tumors were clearly visualized with both 68Ga-labelled tracers, however, significantly lower tumor-to-muscle (T/M) ratios were observed by using [68Ga]Ga-DOTA-HOLDamide. After alpha-radiotherapy treatment the tumor size of the control group was larger relative to both treated cohorts, while the smallest tumor volumes were observed in the NAPamide-treated subclass on the 10th day. Relatively higher [213Bi]Bi-DOTA-NAPamide accumulation in the B16-F10 tumors (%ID/g: 2.71±0.15) with discrete background activity led to excellent T/M ratios, particularly 90 minutes postinjection. Overall, the therapeutic application of receptor selective [213Bi]Bi-DOTA-NAPamide seems to be feasible in MC1-R positive MM management.Copyright © 2023. Published by Elsevier B.V.