Vitamin D Receptor Antagonists for Treating Breast Cancer
Description of Invention:
Vitamin D receptor (VDR) is a nuclear receptor that is activated by calcitriol, the active form of vitamin D. It is best known for regulating dietary calcium uptake necessary for bone growth, but it also affects cell proliferation and differentiation. Therefore, it was thought that treatment with calcitriol or its derivatives could be useful to treat the uncontrolled proliferation typical of cancer cells. However, this approach has been unsuccessful to date because it leads to toxic levels of calcium in the blood.
This invention relates to derivatives of calcitriol that can block cell growth without harmfully raising calcium levels. Specifically, these compounds act as antagonists of VDR blocking its ability to stimulate cell proliferation. This technology can be useful in treating breast cancer or other malignancies.
Applications:
Potential drugs for treating breast cancer and possibly also prostate cancer, colorectal cancer, leukemia, melanoma, or glioma
Prevention of cancer in high-risk population
Research on vitamin D receptor functions and cancer
Market:
About 182,460 American women will be diagnosed with invasive breast cancer in 2008.
Relevant Publication: J Barsony et al. Development of a biologically active fluorescent-labeled calcitriol and its use to study hormone binding to the vitamin D receptor. Anal Biochem. 1995 Jul 20;229(1):68-79. [PubMed abs]
Licensing Status: Available for exclusive or non-exclusive licensing.
Portfolios: Cancer
Cancer -Therapeutics
For Additional Information Please Contact: Whitney Hastings
NIH Office of Technology Transfer
6011 Executive Blvd, Suite 325
Rockville, MD 20852-3804
Phone: 301/451-7337
Email: hastingw@mail.nih.gov
Fax: 301/402-0220