3/10 : D. Perrin – Complex molecules for PET imaging 🗓 🗺
Kit 18F-labeling of complex molecules for PET imaging: Rapid, Wet, One-Step, Late Stage
In seeking a water-friendly fluorination reaction, we have explored the use of several organoborate-bioconjugates that are 18F-labeled in a single step. Molar activities of 15-16 Ci/µmol can be attained. To streamline labeling, we use isotope exchange for time-efficient radiolabeling in ~20 min at >3 Ci/mmol in radiochemical yields of 10-40% using 1Ci of NCA 18F-fluoride. We have used this approach to label RGD, bombesin, octreotate, bradykinin, PSMA etc…
Preclinical animal data with 18F-RBF3-octreotate are comparable with 68Ga-DOTA-TATE. In pursuit of dual-mode fluorescent PET tracers, we have conceived of a “radiosynthon” that provides for fluorescent tracers that combine the sensitivity of PET with the brilliance of fluorescence.
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