​[F-18]siPSMA and [F-18]siTATE:


​Ready to substitute Ga-68 Tracers ?

[F-18]siPSMA and [F-18]siTATE:


a pair of SiFA-based ligands ready to compete with the clinically established Ga-68 ligands.




​​​F-18 is ready to compete with Ga-68


​The development of theranostic radiohybrid PSMA inhibitors ​(rhPSMAs) by A.Wurzer and H.J.Wester at the Institute for Pharmaceutical Radiochemistry, Technical University Munich (TUM) and the subsequently clinical evaluation of [F-18]rhPSMAs by M. Eiber and colleagues at the Department of Nuclear Medicine (TUM) demonstrated for the very first time that ​an F-18-labeled silicone fluorine acceptor ​based radiopharmaceutical ​is stable against defluorination in-vivo and​, ​​if carefully designed, can ​​show ​ pharmacokinetics suitable for PET imaging even at early time points ​after injection. ​​Due to the​ outstanding labeling and imaging characteristics, [F-18]rhPSMA are being clinically developed by Blueearth Diagnostics (UK). Based on this initial success story, ​a series of purely diagnostic [F-18]siPSMA inhibitors have been developed by the same group​.

In addition, an automated process has been developed ​allowing to produce F-18-labeled SiFA-cinjugated radiopharmaceuticals in <1000sec (from end of bombardment to end of production/completed formulation). The process was established on a cassette system comprising of two stopcock manifolds. 


Moreover, ​F-18-labeled SiFA-conjugated ​ocreotate, named ​[F-18]SiFAlin-TATE (siTATE), has been successfully ​compared with​ [Ga-68]DOTA-TOC ​in 13 patients with NET. The authors concluded that ​the favorable characteristics of [F-18]SiFAlin-TATE, the ​simple labeling procedure, and the promising clinical performance enable improved logistics and diagnostic possibilities for PET imaging of NET. ​


In summary, and taking into accout that additional SiFA-peptides are being currently evaluated, we can conclude that the number of clinically revevant, SiFA-based F-18-labeled peptide and peptide-like radiopharmaceuticals will rapidly grow. The ease of production of F-18-labeled SiFA-conjugated radiopharmaceuticals will make them   ​enormously competitive. It seems that the time ​has come ​to take a close look whether and to what extend F-18 can substitute Ga-68 in the rapidly-growing field ​of theranostics. ​



References:    

siPSMA: Di Carlo D. et al. Eur J Nucl Med Mol Imaging (2019) 46 (Suppl 1): S16 (
patent application ​been filed)   
siTATE: Ilhan H et al., Eur J Nucl Med Mol Imaging. 2019 Sep 6.  


GMP Production of

[F-18]siPSMA and [F-18]siTATE:


​• very fast production (<15min)


• at room temperature, thus without volatile 18F-activity


• high yields


• small and simple module


• small and simple cassette and reagent kit


• unparalleled cost efficiency


Radiochemical yield:

​50 % (*)

​Synthesis Time :

< 15 min

​Specific activity:

300 GBq/µmol (**)

applicable to:

​all SiFA tracers

** results from >400 clinical GMP production (starting activities from 30-100GBq)

   

*   using 100 GBq [18F]fluoride and 150 nmol precursor (typical value)



References:    

Wurzer A et al. J Nucl Med. 2019 (accepted) 


​​​siGRP Module


​​​For production of the ​[​F-18]siPSMA and [F-18]SiFAlin-TATE and new upcoming SiFA-Tracers we have designed a dedicated GRP Module that provide considerable advantages:

Production of [F-18]SiFA-based radiopharmaceuticals ​

​The labeling process:



​•​ SPE of [18F]F- on QMA


• on-cartridge drying of [F-18]fluoride
(patent protected)


•​ ​elution of QMA 


• labeling at room
temerature for 5 min


•​ ​dilution and SPE


• washing, elution,        filtration
and dilution


• automated on a

module especially designed for SiFA-labeling   

​​​The siGRP Module​



References:    

Wurzer A et al. ​ (manuscript in preparation)

A successful enterprise is in a constant state of change ...




 

                                                                                                            ... that´s why we now have also became pink.

Toronto/Munich, March 2020

POINT Biopharma and SCINTOMICS Announce License Agreement

Munich/Berlin, February 2020

PENTIXAPHARM Secures € 15 Million Series A Financing to Develop CXCR4-Targeted Theranostics

Munich, June 2019

TUM Presidential Entrepreneurship Award 2019 went to Scintomics

Munich,  June 2019

Andrea Maugg appointed CEOs

Munich, December 2019

The year is drawing to a close. We would like to take this opportunity to thank you for your trustand wish you a Merry Christmas and a successful New Year!
Yours Scintomics/ATT – Team

EANM Barcelona, October 2019

At the EANM 2019 att/Scintomics announced that it has started with the installation of siGRP modules. 

We want to thank all visitors at the EANM2019 booth for their intensive interest and the wonderful and useful conversations. 

Munich/Berlin, May 2019

Scintomics and 1717 Life Science Ventures Team up in the Joint Venture PENTIXAPHARM to Develop CXCR4-Targeted Theranostics

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