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TAT-11: Radio Halogenated Neopentyl Derivatives: A Novel Scaffold for Radioiodinated and Astatinated Compounds of High Stability to In Vivo Dehalogenation

Ottawa, ON, Canada (UroToday.com) To improve on in vivo stability against dehalogenation, two new compounds were developed for labeling with At211 and I125. The two compounds designated BHIN and DEIN are based on two iodinated neopentyl derivatives with a nitroimidazole group. Each showed very well in vitro stability after incubating.

For in vivo mice biodistribution studies, and additional similar compound, BHAN, was prepared for conjugation with At211. In mice, I125-DEIN showed high radioactivity in the neck. This was not observed with either I225-BHIN or At211-BHAN. The BHIN and BHAN were superior in terms of dehalogenation stability 


Presented by: Hiroyuki Suzuki, MD, Chiba University, Graduate School of Pharmaceutical Sciences, Chiba, Japan

Written by: William Carithers, Lawrence Berkeley National Laboratory at the 11th International Symposium on Targeted Alpha Therapy (TAT-10)  April 1 - April 4, 2019 - Ottawa, ON, Canada