Prostate-specific Membrane Antigen: Alpha-labeled Radiopharmaceuticals - 28/05/24

Doi : 10.1016/j.cpet.2024.03.003

Honest Ndlovu, MBChB, MMed ^a,^b, Kgomotso M.G. Mokoala, MBChB, MMed, PhD ^a,^b, Ismaheel Lawal, MBBS, MMed, PhD ^b,^c, Louise Emmett, MD, PhD ^d,^{^{1
Contributed equally.}}, Mike M. Sathekge, MD, PhD ^a,^b,^⁎,^{^{1
Contributed equally.}}
^a Nuclear Medicine Research Infrastructure (NuMeRI), Steve Biko Academic Hospital, Pretoria, South Africa
^b Department of Nuclear Medicine, University of Pretoria & Steve Biko Academic Hospital, Pretoria, South Africa
^c Department of Radiology and Imaging Sciences, Emory University, Atlanta, GA, USA
^d Theranostics and Nuclear Medicine, St Vincent’s Hospital Sydney, Australia

^∗Corresponding author. Department of Nuclear Medicine, University of Pretoria and Steve Biko Academic Hospital, Private Bag X169, Pretoria 0001, South Africa.Department of Nuclear MedicineUniversity of Pretoria and Steve Biko Academic HospitalPrivate Bag X169Pretoria0001South Africa

Résumé

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.

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Keywords : Targeted alpha therapy, Prostate cancer, PSMA, [²²⁵Ac]Ac-PSMA-617, Clinical practice

Plan

Key points

Introduction

Prostate-specific membrane antigen

Alpha-emitting radionuclides for prostate-specific membrane antigen: physics and radiobiology

[¹⁴⁹ Tb]Tb

[²¹² Pb] Pb

[²¹¹At]At

[²²⁷Th]Th

Clinical experience with targeted alpha therapy for prostate cancer

[²¹³Bi]Bi

[²²⁵Ac]Ac

Current evidence for the efficacy of [²²⁵Ac]Ac-prostate-specific membrane antigen therapy in metastatic castrate-resistant prostate cancer

Efficacy of [²²⁵Ac]Ac-prostate-specific membrane antigen in the post−[¹⁷⁷Lu]Lu-prostate-specific membrane antigen therapy setting

[²²⁵Ac]Ac-prostate-specific membrane antigen: in the prechemotherapy and/or postandrogen deprivation therapy settings

[²²⁵Ac]Ac-prostate-specific membrane antigen: application in the hormone-sensitive setting

Side-effect Profile of [²²⁵Ac]Ac-prostate-specific Membrane Antigen

Resistance and Mutations

Rechallenge options

Summary

Clinics care points

Author contributions: All authors contributed equally.

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Vol 19 - N° 3

P. 371-388 - juillet 2024 Retour au numéro

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Prostate Cancer Radioligand Therapy : Beta-labeled Radiopharmaceuticals
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Prostate-specific Membrane Antigen: Alpha-labeled Radiopharmaceuticals - 28/05/24

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