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前列腺特异性膜抗原:α标记的放射性药物。

Prostate-specific Membrane Antigen: Alpha-labeled Radiopharmaceuticals.

作者信息

Ndlovu Honest, Mokoala Kgomotso M G, Lawal Ismaheel, Emmett Louise, Sathekge Mike M

机构信息

Nuclear Medicine Research Infrastructure (NuMeRI), Steve Biko Academic Hospital, Pretoria, South Africa; Department of Nuclear Medicine, University of Pretoria & Steve Biko Academic Hospital, Pretoria, South Africa.

Department of Nuclear Medicine, University of Pretoria & Steve Biko Academic Hospital, Pretoria, South Africa; Department of Radiology and Imaging Sciences, Emory University, Atlanta, GA, USA.

出版信息

PET Clin. 2024 Jul;19(3):371-388. doi: 10.1016/j.cpet.2024.03.003. Epub 2024 Apr 23.

Abstract

Novel prostate-specific membrane antigen (PSMA) ligands labeled with α-emitting radionuclides are sparking a growing interest in prostate cancer treatment. These targeted alpha therapies (TATs) have attractive physical properties that deem them effective in progressive metastatic castrate-resistant prostate cancer (mCRPC). Among the PSMA TAT radiopharmaceuticals, [225Ac]Ac-PSMA has been used extensively on a compassionate basis and is currently undergoing phase I trials. Notably, TAT has the potential to improve quality of life and has favorable antitumor activity and outcomes in multiple scenarios other than in mCRPC. In addition, resistance mechanisms to TAT may be amenable to combination therapies.

摘要

标记有发射α粒子放射性核素的新型前列腺特异性膜抗原(PSMA)配体正引发人们对前列腺癌治疗的日益浓厚兴趣。这些靶向α疗法(TATs)具有吸引人的物理特性,使其在进展性转移性去势抵抗性前列腺癌(mCRPC)中被认为是有效的。在PSMA TAT放射性药物中,[225Ac]Ac-PSMA已在同情用药的基础上广泛使用,目前正在进行I期试验。值得注意的是,TAT有可能改善生活质量,并且在mCRPC以外的多种情况下具有良好的抗肿瘤活性和疗效。此外,对TAT的耐药机制可能适用于联合疗法。

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