NVLS / FX-18A

Cardiovascular disease is the leading killer for both men and women in the United States, accounting for more than one-third of all U.S. deaths. There is a critical demand for the development of novel techniques which are able to early detect cardiovascular disease and accurately evaluate treatment efficacy.

Positron emission tomography/computed tomography (PET/CT) imaging holds the promise of becoming a key diagnostic modality for cardiovascular diseases by allowing visualization and quantification of specific targets and pathways in their physiology and pathology, so that clinical decision making can occur at earlier stages of the disease process.

Currently, the options for functional clinical imaging of cardiovascular disease employ radiopharmaceuticals such as 18F-fludeoxyglucose that localizes based upon the general metabolic activity, lacking specificity for molecular events associated with cardiovascular disease. Accumulating experimental evidence indicates the expressions of adenosine receptors (ARs) are important and prescient signals involved in a variety of cardiovascular diseases. Therefore, quantitative in vivo imaging of ARs may become a useful approach for the management of cardiovascular diseases.

The development of the F-18 labeled ARs analogs for PET/CT imaging, and subsequent mapping in the heart will serve as new and unique biomarkers of cardiovascular disease. Preliminary studies of our proprietary lead compound – [18F]FXA (an adenosine analog), showed very promising results in rodents and primates.

We believe the exploration of biological mechanism of [18F]FXA will lead us to develop a series of novel ARs-targeted molecular imaging probes, which have the strong potential of being translated into clinical trials and help further the steps toward personalized cardiovascular medicine.