Voltage-gated ion channels previously found in the brain have been shown to be expressed in human prostate cancer. Studies reveal that the expression of these ion channels may be linked to the invasive and metastatic potential of prostate cancer. We hypothesize that sodium channel blockers engineered to specifically inhibit this ion channel will be effective in preventing or limiting prostate cancer growth and/or metastasis. This seminar will discuss the expression of these ion channel targets in human prostate cancer and integrate topics on engineering potent and selective small molecule ion channel inhibitors with their effects on human prostate cancer cells in vitro and in vivo.