Medical Radiology and Radiation Safety. 2017. Vol. 62. No. 6. P. 58-74

REVIEW

DOI: 10.12737/article_5a2542f7216cb3.01677610

Radionuclide Diagnosis of Prostate Cancer: Positron Emission Tomography with 68Ga-PSMA Inhibitors and Their Pharmaceutical Development

A.A. Larenkov1,2, G.E. Kodina1

1. A.I. Burnasyan Federal Medical Biophysical Center of FMBA, Moscow, Russia. E-mail: This email address is being protected from spambots. You need JavaScript enabled to view it. ; 2. M.V. Lomonosov Moscow State University, Moscow, Russia

A.A. Larenkov – PhD in Chem., Head of the Laboratory for Technology and Methods Of Monitoring Radiopharmaceuticals; G.E. Kodina – PhD in Chem., Head of the Department of Radiation Technologies for Medical Purposes

Abstract

This review is devoted to the synthesis of the main and most relevant data on the development and clinical use of radiopharmaceuticals (RPs) based on PSMA-inhibitors labeled with 68Ga for the diagnosis of prostate cancer (PC).

The generator method of 68Ga production, which ensures the wide availability of this radionuclide for medical organizations, is the reason for the permanent interest to the RPs based on 68Ga. The development of RPs based on inhibitors of the prostate-specific membrane antigen became the second wave of global excitement about 68Ga-RPs, after labeled derivates of the ocreotide for the diagnosis of neuroendocrine tumors.

PC is one of the most urgent problems of modern oncology. The place of prostate cancer in the structure of the oncological morbidity of the male population, as well as the significance of radionuclide diagnostics in the clinical staging of the disease and the strategy of therapy are considered.

Data on the structure and properties of the prostate-specific membrane antigen (PSMA), its role in the body and expression in the foci of pathological processes are presented. Known PSMA inhibitors and the dependence of their properties on structure are considered.

The main part of the review is devoted to the key results of the pharmaceutical development of RPs based on PSMA-inhibitors labeled with 68Ga. The effect of the fragments (ligand, linker and chelator) on the final radiopharmaceutical molecule on the pharmacokinetics is considered. The review also includes data on the clinical efficacy of PET with 68Ga-PSMA in the diagnosis of PC. Data on the availability of 68Ga-RPs in Russia today, as well as references to regulatory documents that allow the use of such RPs, are presented.

In conclusion, a brief summary of the literature data and conclusions on the most promising radiopharmaceuticals for the diagnosis and therapy of prostate cancer and further perspectives are presented.

Key words: PET, 68Ga, radiopharmaceuticals, PSMA, prostate cancer

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For citation: Larenkov AA, Kodina GE. Radionuclide Diagnosis of Prostate Cancer: Positron Emission Tomography with 68Ga-PSMA Inhibitors and Their Pharmaceutical Development. Medical Radiology and Radiation Safety. 2017;62(6):58-74. Russian. DOI: 10.12737/article_5a2542f7216cb3.01677610

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