Voltage Gated Sodium Channel Blockers as Treatment for Prostate Cancer

Categories: "Cancer Therapeutics"

Reference #: 2008-018, 2009-002

OTC Contact: Ruchika Nijhara, Ph.D., MBA, CLP (Directory Information | Send a Message)

Description

Voltage Gated Sodium Channels (VGSC or Nav) with known expression in central nervous and cardiac tissue are present in human prostate cancer. This invention encompasses novel sodium channel blockers that inhibit both androgen dependent and independent human prostate cancer. These blockers down-regulate the expression of certain Nav isoform(s) relevant to prostate cancer. Structure Analysis Relationship (SAR) has demonstrated a significant correlation with Nav isoform selectivity. In tumors from prostate cancer patients, a correlation between Gleason Score and isoform specificity has been elucidated, which has led to identification of specific Nav isoforms as biomarkers for prostate cancer. The results of this research demonstrate the potential of Nav targeted therapies for the treatment and diagnosis of human prostate cancer.

Applications

Small molecule agents for the treatment and diagnosis of prostate cancer.

Advantages

  • Sodium channel blockers represent a novel approach to the treatment of prostate cancer.
  • Fluorescent moieties allow for these compounds to be traced in assays for the diagnosis of prostate cancer.
  • Fluorescent moieties enable the visualization of compounds reaching the treatment target.
  • Isoform specific Nav can be used as biomarkers to identify the stage of prostate cancer.

Stage of Development

  • A lead compound was evaluated against a human tumor xenograft model and a 70% reduction in tumor volume was observed.
  • Compound stability studies, including metabolic studies using human liver microsomes by LCMS detection, are currently in progress.

Relevant Publications

No references or resources available.

Patent Status

U.S. Patent No. 7,439,382; Issued October 21, 2008; Additional Applications Filed