Abstract

Enzalutamide resistance is a major obstacle in the treatment of metastatic, castration-resistant prostate cancer (mCRPC). Recently we developed a small-molecule lead compound BKM1644 and demonstrated its potent activity against bone metastatic prostate cancer cells. In this Phase I STTR application, we hypothesize that BKM1644 is a novel targeted therapy to overcome enzalutamide resistance and effectively target bone metastasis.
Two Aims are proposed:
Aim 1 will evaluate the in vivo pharmacokinetics, distribution and efficacy of BKM1644 in targeting enzalutamide-resistant, bone metastatic prostate cancer in animal models.
Aim 2 will determine the mechanism of action of BKM1644 in mCRPC cells. The project has immediate therapeutic potential in treating a lethal disease.

Public Health Relevance

In this Phase I STTR application, we will develop a small-molecule drug BKM1644 to overcome enzalutamide resistance and treat bone metastatic prostate cancer, a major cause of cancer death in American men. This project has immediate potential in treating a lethal disease, reducing cancer morbidity and improving healthcare in the United States and globally.

  Funding Agency

Agency
National Institute of Health (NIH)
Institute
National Cancer Institute (NCI)
Type
Small Business Technology Transfer (STTR) Grants - Phase I (R41)
Project #
1R41CA206725-01A1
Application #
9253209
Study Section
Special Emphasis Panel (ZRG1-OTC-T (10)B)
Program Officer
Weber, Patricia A
Project Start
2016-09-15
Project End
2017-08-31
Budget Start
2016-09-15
Budget End
2017-08-31
Support Year
1
Fiscal Year
2016
Total Cost
$224,999
Indirect Cost

  Institution

Name
Metcure Therapeutics, LLC
Department
Type
DUNS #
078866511
City
Atlanta
State
GA
Country
United States
Zip Code
30341