2-[18F]-Labeled Compounds and PET Imaging of Tumors for Enhanced Diagnostic and Therapeutic Monitoring Purposes

SK1365

Summary of Invention

Leading Memorial Sloan Kettering Cancer Center scientists have developed alternative molecules that address the unmet need for enhanced PET imaging. This available technology is a series of small molecules, including a lead compound, which demonstrates desirable characteristics for clinical use. These characteristics include pre-clinical demonstration of high-yield, easily synthesized molecules with increased tumor uptake and biodistribution, allowing for clinically useful PET imaging.

Background

Medical radionuclide imaging is a key component in modern medical practice. Recent advances in imaging, particularly positron emission tomography (PET), provide images which are useful in clinical diagnosis and treatment of disease. The current “universal” PET imaging agent, 18F-FDG, has been generally unsatisfactory, however, for imaging with PET in several tumor types.

In prostate cancer, for example, the 60-70% sensitivity of 18F-FDG PET is not high enough to justify its routine clinical use for staging or restaging of the disease, a problem compounded by imaging difficulties that arise from significant excretion of the agent into the adjacent urinary bladder. As prostate cancer currently affects one in six men during the course of their lifetimes, there is a compelling need for improved PET imaging capabilities.

Market Need

These molecules may serve as a specialized application for types of cancer that 18F-FDG does not satisfactorily address, including prostate, breast, and brain cancer (with 192,280, 194,280, and 22,070 new cases diagnosed, respectively, in the U.S. during 2009 alone). These molecules also may demonstrate utility as broad-spectrum imaging agents, supplementing or replacing 18F-FDG use in PET.

As a point of reference, sales of 18F-FDG were approximately $400 million in 2007, estimated to grow to exceed over $1 billion by 2014. Reflecting trends such as greater use of PET technology in oncology and other areas, the overall market for diagnostic radiopharmaceuticals is expected to grow by 11% or more yearly.

Advantages

  • There are well-established procedures that can be used to generate this easily synthesized suite of three- and four-carbon compounds in development.
  • A lead compound, 2-[18F]-Fluoropropionic acid (FPA), has demonstrated utility in mouse models of multiple cancer types including prostate cancer, breast cancer, and brain cancer. This new technology offers potential for development as a pan-tumor imaging compound for both primary and metastatic tumor detection.
  • Other currently used PET tracers require fasting of the patient, however, preliminary studies indicate that fasting will not be necessary with these compounds.
  • The tumor-to-background ratios for all organs measured is greater than 1, which allows for better delineation of tumors when compared to other imaging molecules, including 18F-FDG and another alternative, 11C-acetate.

Areas of Application

  • For staging tumors based on relative uptake of compound
  • For non-invasive measurement of patient response to therapeutic intervention using PET scanning to measure pre- and post-treatment tumor uptake
  • For use alone or in combination with other imaging techniques for aid in biopsy, surgical resection or the planning of specific radiotherapy

Stage of Development

Pre-clinical proof of concept demonstrated.The researchers are highly motivated and capable of initiation of clinical development.

Lead Inventors

Patent Information

References

Pillarsetty N, et al. (2009) J Nucl Med. Oct;50(10):1709-14

Contact

Peter Fong, PhD
Senior Manager, New Ventures and Business Development
fongp@mskcc.org
Tel: 646-888-1067; Fax: 646-888-1120

Stage of Development
Animal studies
Technology Types
Indications