The present invention relates to copper chelator compounds and their use for treating vasculopathies, for example, pulmonary hypertension (e.g., pulmonary arterial hypertension or portopulmonary hypertension). The methods include administering a composition comprising an effective amount of a copper chelator compound to a patient in need thereof. Administration can be via oral, intraperitoneal, transdermal, intravenous and inhalation routes. In another aspect of the invention, compositions are provided comprising a copper chelator compound complexed to or encapsulated by a lipid component, for example, a copper chelator encapsulated by a liposome and methods of treatment employing the same.