首页|A PET probe targeting polyamine transport system for precise tumor diagnosis and therapy

A PET probe targeting polyamine transport system for precise tumor diagnosis and therapy

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Polyamine metabolism dysregulation is a hallmark of many cancers,offering a promising avenue for early tumor theranostics.This study presents the development of a nuclear probe derived from spermidine(SPM)for dual-purpose tumor PET imaging and internal radiation therapy.The probe,radiolabeled with either[68Ga]Ga for diagnostic applications or[177Lu]Lu for therapeutic use,was synthesized with exceptional purity,stability,and specific activity.Extensive testing involving 12 different tumor cell lines revealed remarkable specificity towards B16 melanoma cells,showcasing outstanding tumor localization and target-to-non-target ratio.Mechanistic investigations employing polyamines,non-labeled precursor,and polyamine transport system(PTS)inhibitor,consistently affirmed the probe's targetability through recognition of the PTS.Notably,while previous reports indicated PTS upregulation in various tumor types for targeted therapy,this study observed no positive signals,highlighting a concentration-dependent discrepancy between targeting for therapy and diagnosis.Furthermore,when labeled with[177Lu],the probe demonstrated its therapeutic potential by effectively controlling tumor growth and extending mouse survival.Investigations into biodistribution,excretion,and biosafety in healthy humans laid a robust foundation for clinical translation.This study introduces a versatile SPM-based nuclear probe with applications in precise tumor theranostics,offering promising prospects for clinical implementation.

PET imagingPolyamine metabolismSpermineRadiopharmaceuticalMelanoma

Ming Zhou、Xiaoqin Yin、Bei Chen、Shuo Hu、Wenhu Zhou

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Department of Nuclear Medicine,Xiangya Hospital,Central South University,Changsha 410008,China

Xiangya School of Pharmaceutical Sciences,Central South University,Changsha 410013,China

Key Laboratory of Biological Nanotechnology of National Health Commission,Changsha 410008,China

National Clinical Research Center for Geriatric Disorders(Xiangya),Changsha 410008,China

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Science and Technology Innovation Team Talent Project of Hunan Provinceclinical research foundation of the National Clinical Research Center for Geriatric Diseases(XIANGYA)Natural Science Foundation of Hunan Province in ChinaScience and Technology Innovation Program of Hunan Province

2021 RC40562020LNJJ012021JJ200842021RC3020

2024

10.1016/j.ajps.2024.100924

亚洲药物制剂科学(英文版)
沈阳药科大学

亚洲药物制剂科学(英文版)

ISSN：1818-0876
年,卷(期)：2024.19(3)