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Small-Molecule
Tumor-Targeting [99mTc] Agents for Breast Cancer Imaging--Anasazi BioMedical Research,
Inc., 101 North Chestnut Street, Suite 206, Winston-Salem, NC 27101; 336-721-9071
Dr. Biao Yang, Principal Investigator
Mrs. Bernita L. Mach, Business Official
DOE Grant No. DE-FG02-00ER82945
Amount:
$100,000
Lack of prognostic tools to access the proliferative
status of breast cancer has been one of the major hurdles in breast cancer
treatment planning patient management. Current approaches (tumor biopsy and fine needle aspirates) in the
measurement of the metastatic potential of breast cancer suffer from a low
predictability (10-35 percent) due to variability of tissue sampling. The goal of the proposed research is to
develop Single Photon Emission Computed Tomography (SPECT) based
radiopharmaceuticals that can provide a non-invasive means of assessing the
proliferative status of breast tumors in vivo and avoid the issues related to
improper tissue sampling. Sigma-2 receptors have emerged as a biomarker for
breast cancer since they are found over expressed in solid breast tumors and
the density of sigma-2 receptors is proportional to the proliferative status of
breast tumor cells both in vitro and in vivo. Therefore, a sigma-2 receptor ligand carrying a radionuclide such
as technetium-99m may provide the means to detect breast cancer and its
proliferative status by applying imaging techniques such as Single Photon
Emission Computed Tomography (SPECT) and Positron Emission Tomography (PET). We have identified a group of small organic
compounds that possess a high binding affinity and high selectivity for sigma-2
receptors. In the Phase I SBIR project
we plan to apply newly improved synthetic routes to incorporate
technetium-99m/rhenium complexes into these highly selective sigma-2 ligands,
which are ideal for Single Photon Emission Computed Tomography. These compounds will be evaluated for binding
to sigma receptors using in vitro binding assays.
Commercial Applications and Other Benefits as
described by the awardee: The product developed in
this Phase I SBIR project is a tumor-targeting non-invasive imaging technique
that will benefit breast cancer patients in treatment strategy planning and
long-term disease control by providing vital information regarding the
proliferative status of the tumor. It can
also be used as a breast cancer screening technique, which will greatly improve
the efficiency and accuracy of the tumor detection. The technique developed in this Phase I SBIR project can also be
translated into other area of cancer diagnosis and patient management such as
lung cancer, glioblastoma, melanoma, head and neck cancers. The product processes a strong commercial
potential because of the widespread availability and low-cost of technetium-99m
generators and scanners throughout the country.