Citation: Ming Zhou, Xiaoqin Yin, Yi Yang, Jian Li, Peng Liu, Jinhui Yang, Pengfei Xu, Shuo Hu, Feifei An. An Evans blue-modified melanin-targeting theranostic agent for improved PET imaging and radionuclide therapy of malignant melanoma[J]. Chinese Chemical Letters, ;2026, 37(12): 112361. doi: 10.1016/j.cclet.2026.112361 shu

An Evans blue-modified melanin-targeting theranostic agent for improved PET imaging and radionuclide therapy of malignant melanoma

Ming Zhou ^{a, b, 1} ,
Xiaoqin Yin ^{b, f, 1} ,
Yi Yang ^b ,
Jian Li ^b ,
Peng Liu ^b ,
Jinhui Yang ^b ,
Pengfei Xu ^{c, *,} ,
Shuo Hu ^{b, d, e, *,} ,
Feifei An ^{a, *,}

a.
School of Public Health, Health Science Center, Xi’an Jiaotong University, Xi’an 710061, China
b.
Department of Nuclear Medicine, Xiangya Hospital, Central South University, Changsha 410008, China
c.
Department of Nuclear Medicine, The First Afliated Hospital of Weifang Medical University, Weifang 261031, China
d.
National Clinical Research Center for Geriatric Disorders (Xiangya), Changsha 410008, China
e.
Key Laboratory of Biological Nanotechnology of National Health Commission, Xiangya Hospital, Central South University, Changsha 410008, China
f.
Department of Nuclear Medicine, Changsha Central Hospital Affiliated to Nanhua University, Changsha 410004, China

pengfeixucsu@outlook.com

hushuo2018@163.com

anfeifei@xjtu.edu.cn

Received Date: 18 September 2025
Revised Date: 25 December 2025
Accepted Date: 3 January 2026
Available Online: 5 January 2026

Figures(4)

Melanin is the characteristic product of the vast majority of melanomas which is the most lethal and invasive type of skin cancer. We synthesized a new probe that target melanin, H-3, and its variant that connected to the Evans blue, H-3-EB, were radiolabeled with [⁶⁸Ga]Ga and [¹⁷⁷Lu]Lu, respectively. Both [⁶⁸Ga]Ga-H-3 and [⁶⁸Ga]Ga-H-3-EB have favorable affinity and specificity for melanin, and good diagnostic efficacy for melanoma. [¹⁷⁷Lu]Lu-H-3-EB showed a more pronounced therapeutic effect than [¹⁷⁷Lu]Lu-H-3 in B16 tumors since its extended effective half life in vivo by its ability binding to albumin. [⁶⁸Ga]Ga-H-3-EB was well tolerated by malignant melanoma (MM) patients, and detected all primary melanoma lesions and lymph node metastases. This suggests that [¹⁷⁷Lu]Lu-H-3-EB could become a highly promising therapeutic option for patients with advanced melanoma.
- Melanoma,
- PET/CT,
- Evans blue,
- First-in-human study,
- Radionuclide therapy,
- Melanin,
- Molecular image
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