Anti-cancer therapies involving non-cytotoxic dopamine beta-hydroxylase (DBH) inhibitors, such as nepicastat, etamicastat, and their analogs and pharmaceutically acceptable salts, and non-cytotoxic serotonin receptor antagonists, such as amperozide and its analogs and pharmaceutically acceptable salts are provided. The non-cytotoxic DBH inhibitors and serotonin receptor antagonists can be administered alone or in combination with one or more additional anti-cancer agents or anti-cancer therapies. Pharmaceutical compositions and combinations containing the non-cytotoxic DBH inhibitors and serotonin receptor antagonists and one or more additional anti-cancer agents, and methods of treating cancer using the pharmaceutical compositions and combinations are also provided.
