An improved synthesis of the radiolabeled prostate-specific membrane antigen inhibitor, [¹⁸F]DCFPyL

Abstract

The radiosynthesis of [18F]DCFPyL on 2 distinct automated platforms with full regulatory compliant quality control specifications is described. The radiotracer synthesis was performed on a custom-made radiofluorination module and the Sofie Biosciences ELIXYS. The radiofluorination module synthesis was accomplished in an average of 66 minutes from end of bombardment with an average specific activity at end of synthesis (EOS) of 4.4 TBq/μmol (120 Ci/μmol) and an average radiochemical yield of 30.9% at EOS. The ELIXYS synthesis was completed in an average of 87 minutes with an average specific activity of 2.2 TBq/μmol (59.3 Ci/μmol) and an average radiochemical yield of 19% at EOS. Both synthesis modules produced large millicurie quantities of [18F]DCFPyL while conforming to all standard US Pharmacopeia Chapter <823> acceptance testing criteria.

Fast indirect fluorine-18 labeling of protein/peptide using the useful 6-fluoronicotinic acid-2,3,5,6-tetrafluorophenyl prosthetic group: A method comparable to direct fluorination

“…Synthesis of [ 18 F]DCFPyL was first reported by an indirect method using 3. Recently synthesis of [ 18 F]DCFPyL has been reported by a direct fluorination method using a single precursor . In this report, we prepared [ 18 F]DCFPyL by an indirect labeling method.…”

Prostate Specific Membrane Antigen Targeted 18 F-DCFPyL Positron Emission Tomography/Computerized Tomography for the Preoperative Staging of High Risk Prostate Cancer: Results of a Prospective, Phase II, Single Center Study

“…Of note, patients were asked to void prior to imaging to decrease bladder activity. Radiotracer for this study was synthesized locally at our center using the method previously described by Ravert et al 24 …”

Radiosynthesis and validation of [5‐cyano‐N‐(4‐(4‐[11C]methylpiperazin‐1‐yl)‐2‐(piperidin‐1‐yl)phenyl) furan‐2‐carboxamide] ([11C]CPPC), a PET radiotracer for imaging CSF1R, a microglia‐specific marker

“…Radiochemical, chemical purity, and specific activity (also known as molar activity) were determined by analytical HPLC with reference to a calibration curve. The previously described specification for chemical purity notes removal of 99.5% of starting precursor and setting the all other UV absorbing peaks in the QC HPLC to be less than 0.5% total (0.3 μg/mL) as the standard used.…”