RT Journal Article
SR Electronic
T1 <strong>Preliminary Results on the Synthesis of </strong><sup><strong>18</strong></sup><strong>F-PSMA-1007 by Direct One-Step Fluorination</strong>
JF Journal of Nuclear Medicine
JO J Nucl Med
FD Society of Nuclear Medicine
SP 334
OP 334
VO 58
IS supplement 1
A1 Cardinale, Jens
A1 Martin, Rene
A1 Smits, Rene
A1 Schaefer, Martin
A1 Neels, Oliver
A1 Remde, Yvonne
A1 Hoepping, Alexander
A1 Mueller, Marco
A1 Giesel, Frederik
A1 Kopka, Klaus
YR 2017
UL http://jnm.snmjournals.org/content/58/supplement_1/334.abstract
AB 334Objectives: In recent years radiolabeled ligands targeting the prostate-specific membrane antigen (PSMA) have gained a significant impact on the diagnosis and therapy of prostate cancer [1]. Therefore, we have developed a fluorine-18 labeled PSMA-targeted imaging probe, 18F-PSMA-1007, which has been successfully applied in first-in-man study [2]. So far, the tracer is only available by a two-step procedure with approx. 10 % RCY [3]. Currently, we are aiming towards a GMP-compliant routine-production of this novel tracer using direct radiofluorination.Methods: A precursor for nucleophilic [18F]fluoride substitution (quarternized ammonium salt) without protection of the carboxylic groups has been developed (Scheme 1). Until now, radiofluorinations have been carried out on a cassette-based automated radiosynthesizer with integrated HPLC have been carried out. Based on those experiments a simplified process on a TRACERlab FX synthesis module has been established. Product purification in the simplified procedure is accomplished by cartridge extraction. A GMP-compliant quality control comparable to the Eur. Ph. monograph of FDG has been established for the first-in-man study.Results: In preliminary experiments the radiofluorination was accomplished successfully with RCY of approx. 20 % and a total synthesis time of one hour. The radiochemical purity of the product was approx. 95 % after HPLC separation. Based on these preliminary experiments a process suitable for our TRACERlab FX modules has been elaborated. This straight-forward and fully GMP-compliant process on the TRACERlab FX Module is currently under evaluation. The final purification of the product is carried out by simple cartridge extraction. The radiochemical purity is &gt;95% while all chemical impurities are below 0.1 mg / V.Conclusion: A process for the radiolabeling of a novel precursor for the synthesis of [18F]PSMA-1007 by direct radiofluorination has been established. The product is obtained in good radiochemical yields of approx. 20% (final injection solution, corrected for decay) after short synthesis time. Currently this process is applied for the routine production of 18F-PSMA-1007 for future clinical trials (phases 1 and 2). Research Support: [1] Rowe, SP, Gorin, MA, Allaf, ME, et al., Prostate Cancer and Prostatic Disease 2016, 19, 223-230. [2] Giesel, F. L., Hadaschik, B., Cardinale, J., et al. et al. Eur. J. Nucl. Med. Mol. Imaging, (Doi: 10.1007/s00259-016-3573-4).[3] Cardinale, J., Schäfer, M., Benesova, M., et al., J. Nucl. Med., (Doi: 10.2967/jnumed.116.181768).