Intravenous Water Soluble Formulation of MJC13 – A Novel Lead Compound for the Treatment of Castrate-resistant Prostate Cancer
Normal prostate growth and maintenance is dependent on androgens acting through the androgen receptor (AR). AR expression is maintained and plays an important role throughout prostate cancer progression. A lead molecule, MJC13, has been identified and has higher potency and better selectivity for AR than any other compound tested. It has been shown to effectively block AR-dependent gene expression in cellular models of prostate cancer at micromolar concentrations.
MJC13, although an attractive drug candidate, has low aqueous solubility. This has hindered the clinical development of MJC13. Scientists at NIH, University of Texas-El-Paso and Texas Southern University have developed a water soluble and stable MJC13 liquid dosage formulation that is suitable for intravenous administration. The solubility of this formulation has increased over 25,000 times compared to MJC13 itself. Additionally, a sensitive LC/MS/MS method to analyze MJC13 has also been developed, which can detect as little as 1 ng/mL of MJC13 in solution or plasma. These studies are of great importance for future pre-clinical and clinical studies of MJC13.
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Leonard Neckers (NCI)
US Application No. 61/788,716
PCT Application No. PCT/US2014/025678
The National Cancer Institute is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate or commercialize this technology with an initial goal of preclinical evaluation and an ultimate goal of clinical testing. For collaboration opportunities, please contact John D. Hewes, Ph.D. at email@example.com. To view the NCI collaborative opportunity announcement, click here.
Eggerton Campbell , Ph.D.
NIH Office of Technology Transfer
OTT Reference No: E-065-2013/0