Abstract

Prostate cancer is the most commonly diagnosed malignancy in men and the second leading cause of cancer-related deaths in Western civilization. Although localized prostate cancer can be treated effectively in different ways, almost all patients progress to the incurable metastatic castration-resistant prostate cancer. Due to the significant mortality and morbidity rate associated with the progression of this disease, there is an urgent need for new and targeted treatments. In this review, we summarize the recent advances in research on identification of prostate tissue-specific antigens for targeted therapy, generation of highly specific and selective molecules targeting these antigens, availability of therapeutic radionuclides for widespread medical applications, and recent achievements in the development of new-generation small-molecule inhibitors and antibody-based strategies for targeted prostate cancer therapy with alpha-, beta-, and Auger electron-emitting radionuclides.

Highlights

  • According to the cancer epidemiology databases provided by the International Agency for Research on Cancer and the WHO Cancer Mortality Database, prostate cancer is the most commonly diagnosed malignancy in men and the second leading cause of cancer-related deaths in Western civilization [1].Today, standard primary therapy for patients with localized prostate cancer consists mainly of radical prostatectomy and/or external beam radiotherapy or brachytherapy

  • We summarize the recent advances in research on identification review, we summarize the recent advances in research on identification of prostate tissue-specific of prostategeneration tissue-specific antigens, generation of highlymolecules specific and selective molecules targeting these antigens, of highly specific and selective targeting these antigens, availability antigens, availability of therapeutic radioisotopes for widespread medical applications and recent of therapeutic radioisotopes for widespread medical applications and recent achievements in the achievements development of aofnew generation of antibody-based strategies and small-molecule development in ofthe a new generation antibody-based strategies and small-molecule inhibitors for inhibitors for targeted prostate cancer therapy with alphaand beta-particle radionuclides

  • J415 and J591 manner by anti-PSMA antibody (mAb) competed for binding to Prostate-Specific Membrane Antigen (PSMA) antigen, J533 did not interfered with J415, rapid elimination of 131 I

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Summary

Introduction

According to the cancer epidemiology databases provided by the International Agency for Research on Cancer and the WHO Cancer Mortality Database, prostate cancer is the most commonly diagnosed malignancy in men and the second leading cause of cancer-related deaths in Western civilization [1]. Localized prostate cancer can be treated effectively by these therapies, almost all patients progress to metastatic castration-resistant prostate cancer (mCRPC) [4]. We summarize the recent advances in research on identification review, we summarize the recent advances in research on identification of prostate tissue-specific of prostategeneration tissue-specific antigens, generation of highlymolecules specific and selective molecules targeting these antigens, of highly specific and selective targeting these antigens, availability antigens, availability of therapeutic radioisotopes for widespread medical applications and recent of therapeutic radioisotopes for widespread medical applications and recent achievements in the achievements development of aofnew generation of antibody-based strategies and small-molecule development in ofthe a new generation antibody-based strategies and small-molecule inhibitors for inhibitors for targeted prostate cancer therapy with alphaand beta-particle radionuclides. Targeted prostate cancer therapy with alpha- and beta-particle radionuclides

Potential Therapy Targets for Prostate Cancer
PSMA Ligands for Targeted Radiotherapy
Antibodies
Small-Molecule
Radionuclides Investigated for Use in Targeted Prostate Cancer Therapy
Schematic
Auger Electron Emitters
Main Findings
90 Y-huJ591 mAb
90 Y-huJ591
PSMA-Targeted Antibody-Based Molecules Conjugated to α-Emitters
PSMA-Targeted Small Molecules Conjugated to α-Emitters
PSMA-Targeting Ligands Conjugated to Auger Electron Emitters
PSMA-Targeted Nanoparticle-Based Radiopharmaceuticals
Conclusions

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