PET Radiopharmaceutical Development

2021 ◽  
pp. 9-16
Author(s):  
Peter M. Smith-Jones
Author(s):  
Simona Malaspina ◽  
Vesa Oikonen ◽  
Anna Kuisma ◽  
Otto Ettala ◽  
Kalle Mattila ◽  
...  

Abstract Purpose This phase 1 open-label study evaluated the uptake kinetics of a novel theranostic PET radiopharmaceutical, 18F-rhPSMA-7.3, to optimise its use for imaging of prostate cancer. Methods Nine men, three with high-risk localised prostate cancer, three with treatment-naïve hormone-sensitive metastatic disease and three with castration-resistant metastatic disease, underwent dynamic 45-min PET scanning of a target area immediately post-injection of 300 MBq 18F-rhPSMA-7.3, followed by two whole-body PET/CT scans acquired from 60 and 90 min post-injection. Volumes of interest (VoIs) corresponding to prostate cancer lesions and reference tissues were recorded. Standardised uptake values (SUV) and lesion-to-reference ratios were calculated for 3 time frames: 35–45, 60–88 and 90–118 min. Net influx rates (Ki) were calculated using Patlak plots. Results Altogether, 44 lesions from the target area were identified. Optimal visual lesion detection started 60 min post-injection. The 18F-rhPSMA-7.3 signal from prostate cancer lesions increased over time, while reference tissue signals remained stable or decreased. The mean (SD) SUV (g/mL) at the 3 time frames were 8.4 (5.6), 10.1 (7) and 10.6 (7.5), respectively, for prostate lesions, 11.2 (4.3), 13 (4.8) and 14 (5.2) for lymph node metastases, and 4.6 (2.6), 5.7 (3.1) and 6.4 (3.5) for bone metastases. The mean (SD) lesion-to-reference ratio increases from the earliest to the 2 later time frames were 40% (10) and 59% (9), respectively, for the prostate, 65% (27) and 125% (47) for metastatic lymph nodes and 25% (19) and 32% (30) for bone lesions. Patlak plots from lesion VoIs signified almost irreversible uptake kinetics. Ki, SUV and lesion-to-reference ratio estimates showed good agreement. Conclusion 18F-rhPSMA-7.3 uptake in prostate cancer lesions was high. Lesion-to-background ratios increased over time, with optimal visual detection starting from 60 min post-injection. Thus, 18F-rhPSMA-7.3 emerges as a very promising PET radiopharmaceutical for diagnostic imaging of prostate cancer. Trial Registration NCT03995888 (24 June 2019).


2019 ◽  
Vol 152 ◽  
pp. 30-36 ◽  
Author(s):  
Zonghua Luo ◽  
Jiwei Gu ◽  
Robert C. Dennett ◽  
Gregory G. Gaehle ◽  
Joel S. Perlmutter ◽  
...  

2020 ◽  
Vol 13 (1) ◽  
pp. 431-435 ◽  
Author(s):  
Zuzana Balážová ◽  
Igor Černý ◽  
Petr Vyškovský

18F-fluciclovine is a PET radiopharmaceutical used for the detection of recurrent prostate cancer in adult men after primary curative treatment with suspicion of recurrence based on elevated prostate-specific antigen level. Several incidental uptakes of 18F-fluciclovine in other tumour types have been described in the literature so far – in breast cancer, hepatocellular carcinoma, and malignant melanoma. Our case report presents a patient with oncological duplicity (prostate gland carcinoma and newly diagnosed neuroendocrine tumour) and with accumulation of fluciclovine in pathologically proved neuroendocrine tumour, later imagined also by octreotide SPECT/CT. To our knowledge, this is the first case of fluciclovine accumulated in a neuroendocrine tumour described in the literature.


Molecules ◽  
2020 ◽  
Vol 25 (4) ◽  
pp. 982
Author(s):  
Cassis Varlow ◽  
Emily Murrell ◽  
Jason P. Holland ◽  
Alina Kassenbrock ◽  
Whitney Shannon ◽  
...  

[18F]FPEB is a positron emission tomography (PET) radiopharmaceutical used for imaging the abundance and distribution of mGluR5 in the central nervous system (CNS). Efficient radiolabeling of the aromatic ring of [18F]FPEB has been an ongoing challenge. Herein, five metal-free precursors for the radiofluorination of [18F]FPEB were compared, namely, a chloro-, nitro-, sulfonium salt, and two spirocyclic iodonium ylide (SCIDY) precursors bearing a cyclopentyl (SPI5) and a new adamantyl (SPIAd) auxiliary. The chloro- and nitro-precursors resulted in a low radiochemical yield (<10% RCY), whereas both SCIDY precursors and the sulfonium salt precursor produced [18F]FPEB in the highest RCYs of 25% and 36%, respectively. Preliminary PET/CT imaging studies with [18F]FPEB were conducted in a transgenic model of Alzheimer’s Disease (AD) using B6C3-Tg(APPswe,PSEN1dE9)85Dbo/J (APP/PS1) mice, and data were compared with age-matched wild-type (WT) B6C3F1/J control mice. In APP/PS1 mice, whole brain distribution at 5 min post-injection showed a slightly higher uptake (SUV = 4.8 ± 0.4) than in age-matched controls (SUV = 4.0 ± 0.2). Further studies to explore mGluR5 as an early biomarker for AD are underway.


2019 ◽  
Vol 19 (17) ◽  
pp. 7702-7707 ◽  
Author(s):  
Blas Salvador ◽  
Diego Andres Escalante Pineda ◽  
Laura Fernandez-Maza ◽  
Ariadna Corral ◽  
Sergio Camacho-Leon ◽  
...  

2010 ◽  
Vol 51 (2) ◽  
pp. 282-287 ◽  
Author(s):  
A. M. Elizarov ◽  
R. M. van Dam ◽  
Y. S. Shin ◽  
H. C. Kolb ◽  
H. C. Padgett ◽  
...  

Neurology ◽  
2012 ◽  
Vol 78 (Meeting Abstracts 1) ◽  
pp. IN7-2.005-IN7-2.005
Author(s):  
M. Yoneda ◽  
M. Ikawa ◽  
Y. Yoshii ◽  
Y. Nakamoto ◽  
Y. Fujibayashi ◽  
...  

Sign in / Sign up

Export Citation Format

Share Document