Vitamin D Receptor Antagonists for Treating Breast Cancer

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.

Potential Commercial Applications: Competitive Advantages:
  • 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

Development Stage:
Pre-clinical data available


Julianna Barsony (NIDDK)  ➽ more inventions...

Intellectual Property:
US Pat: 7,361,664 issued 2008-04-22
PCT Application No. PCT/US02/19774 filed on 2002-06-20

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 Contact:
Admin. Licensing Specialist (ALS),

OTT Reference No: E-213-2001-2
Updated: Sep 1, 2008