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恶性黑色素瘤患者中黑色素靶向[F]DMPY2的首次人体PET成像及评估

First-in-human PET imaging and evaluation of melanin-targeted [F]DMPY2 in malignant melanoma patients.

作者信息

Yang Yi, Zhou Ming, Zhao Shuang, Long Tingting, Chen Na, Wang Xingming, Li Yulai, Chen Xiaozhen, Chen Junchen, Huang Xinqiong, Chen Dengming, Su Juan, Hu Shuo, Chen Xiang

机构信息

Department of Nuclear Medicine, Xiangya Hospital, Central South University, Changsha, Hunan, China.

Department of Dermatology, Xiangya Hospital, Central South University, Changsha, Hunan, China.

出版信息

Theranostics. 2025 May 7;15(13):6100-6110. doi: 10.7150/thno.109243. eCollection 2025.

DOI:10.7150/thno.109243
PMID:40521209
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12159754/
Abstract

Early diagnosis and accurate malignant melanoma (MM) staging are significant and decisive in clinical practice. [F]DMPY2 is a promising PET tracer with high affinity and selectivity for melanin. The study aims to investigate the biodistribution and radiation dosimetry in healthy volunteers, and the potential clinical application of [F]DMPY2 in MM patients. : [F]DMPY2 was synthesized via a one-pot reaction. The biodistribution, radiation dosimetry, and probe safety were estimated in three healthy volunteers. Thirty-one MM patients underwent [F]DMPY2 and/or [F]FDG PET/CT scans to explore the clinical use in early detection of melanoma metastasis. Diagnostic performance was assessed in fifty-one LN basins of twenty-seven MM patients after surgery, comparing PET uptake with pathological results. : [F]DMPY2 was well tolerated by healthy volunteers and MM patients. The calculated effective dose of [F]DMPY2 was 0.0122 mSv/MBq. In MM patients, we observed prominent [F]DMPY2 tumor uptake and high tumor-to-background ratios in primary tumors. [F]DMPY2 showed superior diagnostic performance in lymph node metastases compared to [F]FDG, with sensitivity, specificity, accuracy, positive and negative predictive values of 66.7%, 100%, 88.9%, 100% and 85.7%, respectively, versus 50%, 42.9%, 46.7%, 50% and 42.9% for [F]FDG. Additionally, [F]DMPY2 PET imaging had a unique advantage in distinguishing [F]FDG false-positive lesions. : [F]DMPY2 is a safe and well-tolerated melanin PET tracer and can be a powerful imaging tool for early detection and clinical staging of patients with MM.

摘要

早期诊断和准确的恶性黑色素瘤(MM)分期在临床实践中具有重要的决定性意义。[F]DMPY2是一种对黑色素具有高亲和力和选择性的有前景的PET示踪剂。本研究旨在调查[F]DMPY2在健康志愿者中的生物分布和辐射剂量学,以及其在MM患者中的潜在临床应用。:[F]DMPY2通过一锅法反应合成。在三名健康志愿者中评估了其生物分布、辐射剂量学和探针安全性。31例MM患者接受了[F]DMPY2和/或[F]FDG PET/CT扫描,以探索其在黑色素瘤转移早期检测中的临床应用。对27例MM患者术后的51个淋巴结区域进行诊断性能评估,将PET摄取情况与病理结果进行比较。:健康志愿者和MM患者对[F]DMPY2耐受性良好。计算得出的[F]DMPY2有效剂量为0.0122 mSv/MBq。在MM患者中,我们观察到原发性肿瘤中[F]DMPY2有显著的肿瘤摄取和高肿瘤与背景比值。与[F]FDG相比,[F]DMPY2在淋巴结转移方面显示出更好的诊断性能,其敏感性、特异性、准确性、阳性和阴性预测值分别为66.7%、100%、88.9%、100%和85.7%,而[F]FDG的相应值分别为50%、42.9%、46.7%、50%和42.9%。此外,[F]DMPY2 PET成像在区分[F]FDG假阳性病变方面具有独特优势。:[F]DMPY2是一种安全且耐受性良好的黑色素PET示踪剂,可成为MM患者早期检测和临床分期的有力成像工具。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/43c5/12159754/9fb117facb05/thnov15p6100g007.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/43c5/12159754/9fb117facb05/thnov15p6100g007.jpg

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