Molecular imaging (MI) using radiolabeled compounds (radiopharmaceuticals) has become a critical tool in the early detection of disease. The technique can be used to visualize biochemical changes associated with diseases like cancer long before physical symptoms of the disease are evident.

MI is also being used in drug development since it allows for the monitoring of the distribution of a labeled pharmaceutical inside the body at sub-efficacious doses. As a result, drugs that do not reach the site of the disease or that have suboptimal properties can be eliminated from the pipeline prior to costly clinical trials.

As a result, most pharmaceutical companies are actively seeking ways of incorporating radionuclides into new compounds as part of the basic drug discovery process.1

In order to produce a successful radiopharmaceutical, numerous criteria must be met.2 For instance, the compound must preferentially bind to a particular site or biomolecule. The tracer must not influence any biological process and it is best if the compound remains intact at the target organ rather than undergoing metabolism.

The Valliant group confronts these challenges by developing new methods for incorporating radionuclides into compounds, including novel pharmaceutical agents. The aim is to not only develop new probes and labelled rugs, but to identify new reactions and synthetic methods that can become general purpose platform technologies.

 

References:

1. A. F. Armstrong and J. F. Valliant, Dalton Trans. 38, 2007, 4240.

2. W. C. Eckelman, Nucl. Med. Bio. 1998, 25, 169.