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18F Labeling By Chelate Approach

January 23, 2012 | A version of this story appeared in Volume 90, Issue 4

The news on “Fluoride Catch and Release” describes an elegant electrophilic fluorination for 18F positron emission tomography that was published in Science (C&EN, Nov. 7, 2011, page 7). The importance of the featured work cannot be overstated, as fast and efficient labeling procedures are crucial to the success of utilizing this PET radionuclide with a short 110-minute half-life.

However, other significant strides have been made in the field as well, most notably by my colleagues William J. McBride et al., at Immunomedics. They have developed a conceptually new and innovative approach to 18F labeling based on fast chelation of [18F] aluminum fluoride to NOTA-derivatized targeting molecules (termed AlF method). This is a process that is complete within 20–30 minutes including purification, does not require preparative HPLC, leads to high-yield radiolabelings and clinically relevant specific activities, and is amenable to kit formulation. The method has been applied for tagging a number of receptor-targeted agents with 18F and is being expanded for application to monoclonal antibody fragments (Bioconjugate Chem., DOI: 10.1021/bc200175c and 10.1021/bc100137x; J. Nucl. Med., DOI: 10.2967/jnumed.108.060418).

This work has also been presented at numerous nuclear medicine meetings in the U.S. and Europe and is now being embraced by other research groups involved in 18F labeling for PET imaging. More recently, this work was honored with the 2011 Thomas Alva Edison Patent Award by the Research & Development Council of New Jersey.

By Serengulam V. Govindan
Summit, NJ


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