Disclosed is an oral pharmaceutical composition, comprising methylglyoxal bis(guanylhydrazone) (MGBG) together with at least one oral pharmaceutically acceptable excipient, which yields a therapeutically effective systemic plasma MGBG level when orally administered to a subject, wherein the oral pharmaceutical composition is formulated to provide a dose of 0.42 mg/kg/day to 4.51 mg/kg/day.