[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)
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Yours Scintomics/ATT – Team
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