Kinetics of 76Br-labeled anti-CEA antibodies in pigs; Aspects of dosimetry and PET imaging properties

1999 ◽  
Vol 26 (2) ◽  
pp. 249-258 ◽  
Author(s):  
Anna Lövqvist ◽  
Hans Lundqvist ◽  
Mark Lubberink ◽  
Vladimir Tolmachev ◽  
Jörgen Carlsson ◽  
...  
The Prostate ◽  
2014 ◽  
Vol 74 (7) ◽  
pp. 743-755 ◽  
Author(s):  
Stefan Wiehr ◽  
Patrick Bühler ◽  
Dorothee Gierschner ◽  
Philipp Wolf ◽  
Anna-Maria Rolle ◽  
...  

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Sara S. Rinne ◽  
Charles Dahlsson Leitao ◽  
Joshua Gentry ◽  
Bogdan Mitran ◽  
Ayman Abouzayed ◽  
...  

AbstractUpregulation of the human epidermal growth factor receptor type 3 (HER3) is a common mechanism to bypass HER-targeted cancer therapy. Affibody-based molecular imaging has the potential for detecting and monitoring HER3 expression during treatment. In this study, we compared the imaging properties of newly generated 68Ga-labeled anti-HER3 affibody molecules (HE)3-ZHER3-DOTA and (HE)3-ZHER3-DOTAGA with previously reported [68Ga]Ga-(HE)3-ZHER3-NODAGA. We hypothesized that increasing the negative charge of the gallium-68/chelator complex would reduce hepatic uptake, which could lead to improved contrast of anti-HER3 affibody-based PET-imaging of HER3 expression. (HE)3-ZHER3-X (X = DOTA, DOTAGA) were produced and labeled with gallium-68. Binding of the new conjugates was specific in HER3 expressing BxPC-3 and DU145 human cancer cells. Biodistribution and in vivo specificity was studied in BxPC-3 xenograft bearing Balb/c nu/nu mice 3 h pi. DOTA- and DOTAGA-containing conjugates had significantly higher concentration in blood than [68Ga]Ga-(HE)3-ZHER3-NODAGA. Presence of the negatively charged 68Ga-DOTAGA complex reduced the unspecific hepatic uptake, but did not improve overall biodistribution of the conjugate. [68Ga]Ga-(HE)3-ZHER3-DOTAGA and [68Ga]Ga-(HE)3-ZHER3-NODAGA had similar tumor-to-liver ratios, but [68Ga]Ga-(HE)3-ZHER3-NODAGA had the highest tumor uptake and tumor-to-blood ratio among the tested conjugates. In conclusion, [68Ga]Ga-(HE)3-ZHER3-NODAGA remains the favorable variant for PET imaging of HER3 expression.


2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Nedim C. M. Gulaldi ◽  
Jinsong Xia ◽  
Tao Feng ◽  
Kelvin Hong ◽  
William B. Mathews ◽  
...  

Purpose. The radioligand [11C]KR31173 has been introduced for PET imaging of the angiotensin II subtype 1 receptor (AT1R). The purpose of the present project was to employ and validate a compartmental model for quantification of the kinetics of this radioligand in a porcine model of renal ischemia followed by reperfusion (IR).Procedures. Ten domestic pigs were included in the study: five controls and five experimental animals with IR of the left kidney. To achieve IR, acute ischemia was created with a balloon inserted into the left renal artery and inflated for 60 minutes. Reperfusion was achieved by deflation and removal of the balloon. Blood chemistries, urine specific gravity and PH values, and circulating hormones of the renin angiotensin system were measured and PET imaging was performed one week after IR. Cortical time-activity curves obtained from a 90 min [11C]KR31173 dynamic PET study were processed with a compartmental model that included two tissue compartments connected in parallel. Radioligand binding quantified by radioligand retention (80 min value to maximum value ratio) was compared to the binding parameters derived from the compartmental model. A binding ratio was calculated asDVR=DVS/DVNS, whereDVSandDVNSrepresented the distribution volumes of specific binding and nonspecific binding. Receptor binding was also determined by autoradiographyin vitro.Results. Correlations between rate constants and binding parameters derived by the convolution and deconvolution curve fittings were significant(r>0.9). Also significant was the correlation between the retention parameter derived from the tissue activity curve (Yret) and the retention parameter derived from the impulse response function (fret). Furthermore, significant correlations were found between these two retention parameters and DVR. Measurements with PET showed no significant changes in the radioligand binding parameters caused by IR, and thesein vivofindings were confirmed by autoradiography performedin vitro.Conclusions. Correlations between various binding parameters support the concept of the parallel connectivity compartmental model. If an arterial input function cannot be obtained, simple radioligand retention may be adequate for estimation ofin vivoradioligand binding.


2013 ◽  
Vol 2013 ◽  
pp. 1-9
Author(s):  
Pallavi Lagisetty ◽  
Hrushikesh Agashe ◽  
Vibhudutta Awasthi

Synthesis of 2-[3,5-bis-(2-fluorobenzylidene)-4-piperidon-1-yl]-N-(4-fluorobenzyl)-acetamide, a derivative of 3,5-bis-(2-fluorobenzylidene)-4-piperidone (EF24), as an antiproliferative and imageable compound is described. The radioactive derivative was synthesized in 40–45% radiochemical yield using N-[4-fluoro(18F)benzyl]-2-bromoacetamide (NFLOBA) as a radiolabeled synthon for coupling with EF24. Cell proliferation assays showed that 2-[3,5-bis-(2-fluorobenzylidene)-4-piperidon-1-yl]-N-(4-fluorobenzyl)-acetamide (NFLOBA-EF24) had antiproliferative efficacy similar to that of EF24 in lung adenocarcinoma H441 cells.18F-NFLOBA-EF24 was investigated in normal rats for whole-body PET imaging and biodistribution. At necropsy after 1 h of injection, about 12% of injected compound was still circulating in blood; liver, kidney, and muscle were other tissues with moderate amounts of accumulation. In order to assess the tumor-suppressive activity, nonradioactive NFLOBA-EF24 was administered in nude rats carrying xenograft H441 tumor. After 15 days of treatment, the tumor size decreased by approximately 83% compared to the tumors in control rats. The tumor regression was also confirmed by molecular imaging of glucose metabolism with18F- fluorodeoxyglucose. The results suggest that EF24 could be efficiently modified with18F-labeled synthon NFLOBA for convenient PET imaging without altering the antitumor efficacy of the original compound. This study provides visual kinetics of synthetic curcuminoid EF24 by positron emission tomography for the first time.


2020 ◽  
Vol 59 (43) ◽  
pp. 19126-19132
Author(s):  
Leon Z. Wang ◽  
Tristan L. Lim ◽  
Prashanth K. Padakanti ◽  
Sean D. Carlin ◽  
Abass Alavi ◽  
...  

2018 ◽  
Vol 34 (10) ◽  
pp. S117-S118 ◽  
Author(s):  
J. Zelt ◽  
J. Renaud ◽  
L. Mielniczuk ◽  
L. Garrard ◽  
C. Orlandi ◽  
...  

2018 ◽  
Vol 8 (1) ◽  
Author(s):  
Dorra Amor ◽  
Sébastien Goutal ◽  
Solène Marie ◽  
Fabien Caillé ◽  
Martin Bauer ◽  
...  

2015 ◽  
Vol 103 (6) ◽  
Author(s):  
Sebastian Kuhn ◽  
Ingo Spahn ◽  
Bernhard Scholten ◽  
Heinz H. Coenen

AbstractTo evaluate the PET-imaging properties of the promising positron emitter


2019 ◽  
Vol 47 (5) ◽  
pp. 1314-1325 ◽  
Author(s):  
Stefanie Pektor ◽  
Janine Schlöder ◽  
Benedikt Klasen ◽  
Nicole Bausbacher ◽  
Daniel-Christoph Wagner ◽  
...  

2019 ◽  
Vol 60 (7) ◽  
pp. 985-991 ◽  
Author(s):  
Nicolas Tournier ◽  
Martin Bauer ◽  
Verena Pichler ◽  
Lukas Nics ◽  
Eva-Maria Klebermass ◽  
...  

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