Flourine-18 Dasatinib Derivative For PET Imaging Of Tumors

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.

Advantages

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.

Lead Inventor

Steven Larson, MD

Patent Information

U.S. Patent application pending

References

Veach DR, et al. (2007) J. Med. Chem. 50:5853-7

Contact Information

Peter Fong, PhD
Manager, New Ventures and Business Development
fongp@mskcc.org
Tel: 646-227-7196; Fax: 212-557-8349

Stage of Development

Animal studies

cancer (KAN-ser)

A term for diseases in which abnormal cells divide without control and can invade nearby tissues. Cancer cells can also spread to other parts of the body through the blood and lymph systems. There are several main types of cancer. Carcinoma is a cancer that begins in the skin or in tissues that line or cover internal organs. Sarcoma is a cancer that begins in bone, cartilage, fat, muscle, blood vessels, or other connective or supportive tissue. Leukemia is a cancer that starts in blood-forming tissue such as the bone marrow, and causes large numbers of abnormal blood cells to be produced and enter the blood. Lymphoma and multiple myeloma are cancers that begin in the cells of the immune system. Central nervous system cancers are cancers that begin in the tissues of the brain and spinal cord. Also called malignancy.