Automated production of 1-(2-[18F]fluoroethyl)-l-tryptophan for imaging of tryptophan metabolism

Abstract

Automated production of an fluorine-18 labeled tryptophan analogue, 1-(2-[¹⁸F]fluoroethyl)-l-tryptophan (1-L-[¹⁸F]FETrp) in a current Good Manufacturing Practice facility was achieved. 1-L-[¹⁸F]FETrp was produced by a one-pot, two-step strategy with an overall synthesis time of approximately 100 min, a radiochemical yield of 20 ± 5% (decay corrected), radiochemical purity and enantiomeric excess over 90%, and a molar activity of 103 ± 15 GBq/μmol at the end of synthesis (EOS). The dose mass of 1-L-FETrp in four consecutive batches was less than 5 μg. The radiopharmaceutical product met all quality control criteria for clinical use.

Keywords: 1-(2-[(18)F]Fluoroethyl)-l-tryptophan; Current good manufacturing practice; Radiosynthesis; Tryptophan metabolism.