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Preclinical Evaluation of a Companion Diagnostic Radiopharmaceutical, [18F]PSMA-1007, in a Subcutaneous Prostate Cancer Xenograft Mouse Model

 Su Bin Kim  ;  In Ho Song  ;  Seon Yoo Kim  ;  Hae Young Ko  ;  Hee Seup Kil  ;  Dae Yoon Chi  ;  Frederik L Giesel  ;  Klaus Kopka  ;  Alexander Hoepping  ;  Joong-Hyun Chun  ;  Hyun Soo Park  ;  Mijin Yun  ;  Sang Eun Kim 
 MOLECULAR PHARMACEUTICS, Vol.20(2) : 1050-1060, 2023-02 
Journal Title
Issue Date
Animals ; Antigens, Surface / metabolism ; Cell Line, Tumor ; Glutamate Carboxypeptidase II / metabolism ; Heterografts ; Humans ; Male ; Mice ; Oligopeptides ; Prostatic Neoplasms* / diagnostic imaging ; Prostatic Neoplasms* / drug therapy ; Prostatic Neoplasms* / radiotherapy ; Radiopharmaceuticals* / pharmacokinetics
[18F]PSMA-1007 ; biodistribution ; internal radiation dosimetry ; positron emission tomography ; theranostics
Several radiolabeled prostate-specific membrane antigen (PSMA)-targeted agents have been developed for detecting prostate cancer, using positron emission tomography imaging and targeted radionuclide therapy. Among them, [18F]PSMA-1007 has several advantages, including a comparatively long half-life, delayed renal excretion, and compatible structure with alpha-/beta-particle emitter-labeled therapeutics. This study aimed to characterize the preclinical pharmacokinetics and internal radiation dosimetry of [18F]PSMA-1007, as well as its repeatability and specificity for target binding using prostate tumor-bearing mice. In PSMA-positive tumor-bearing mice, the kidney showed the greatest accumulation of [18F]PSMA-1007. The distribution in the tumor attained its peak concentration of 2.8%ID/g at 112 min after intravenous injection. The absorbed doses in the tumor and salivary glands were 0.079 +/- 0.010 Gy/MBq and 0.036 +/- 0.006 Gy/MBq, respectively. The variance of the net influx (Ki) of [18F]PSMA-1007 to the tumor was minimal between scans performed in the same animals (within-subject coefficient of variation = 7.57%). [18F]PSMA-1007 uptake in the tumor was specifically decreased by 32% in Ki after treatment with a PSMA inhibitor 2-(phosphonomethyl)-pentanedioic acid (2-PMPA). In the present study, we investigated the in vivo preclinical characteristics of [18F]PSMA-1007. Our data from [18F]PSMA-1007 PET/computed tomography (CT) studies in a subcutaneous prostate cancer xenograft mouse model supports clinical therapeutic strategies that use paired therapeutic radiopharmaceuticals (such as [177Lu]Lu-PSMA-617), especially strategies with a quantitative radiation dose estimate for target lesions while minimizing radiation-induced toxicity to off-target tissues.
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1. College of Medicine (의과대학) > Dept. of Nuclear Medicine (핵의학교실) > 1. Journal Papers
Yonsei Authors
Yun, Mi Jin(윤미진) ORCID logo https://orcid.org/0000-0002-1712-163X
Chun, Joong-Hyun(전중현) ORCID logo https://orcid.org/0000-0002-9665-7829
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