Summary of Invention
One important facet of individualized patient care has been kinase inhibitor therapy, a signal transduction modulation which is revolutionizing disease treatment. Also key to personalized medicine is the ability to use noninvasive medical-imaging techniques such as positron emission tomography (PET) to assess disease status and determine the optimal course of treatment for an individual patient, particularly in cancer.
To predict response to drug treatment or to observe the onset of drug resistance, MSKCC investigators are developing radiotracers that can complement a given therapy and provide more information than currently utilized imaging modalities, including [18F]-FDG. While certain kinases are well known to play a role in cancer, kinase inhibitors bearing PET isotopes have only recently started to emerge as a potential prognostic tool for individually monitoring kinase inhibitor therapy. MSKCC investigators now have demonstrated synthesis and in vivo PET imaging of an [18F]-derivative of the FDA-approved dasatinib (BMS-354825), a potent, multi-targeted kinase inhibitor. This radiotracer may be useful in all cancer types sensitive to dasatinib, including CML and Ph+ALL.
- Radiolabeled molecule retains similar tumor selectivity to non-labeled dasatinib and strong anti-tumor activity
- Using CML xenograft models, no significant uptake in bone was observed, indicating that the compound does not undergo rapid defluorination
Areas of Application
Available for licensing for commercialization as an imaging agent to monitor patient disease progression and responses to dasatinib treatment
Stage of Development
Investigators are finalizing compound formulation for IND submission and are highly motivated and capable of initiating clinical trials.
Steven Larson, MD, Laboratory Head, Molecular Pharmacology and Chemistry Program, Sloan Kettering Institute, Memorial Sloan Kettering
U.S. Patent application pending
Veach DR, et al. (2007) J. Med. Chem. 50:5853-7
Tingting Zhang Kharas, PhD