The present invention provides a combination of a Type I protein arginine methyltransferase (Type I PRMT) inhibitor and a Type II protein arginine methyltransferase (Type II PRMT) inhibitor. The present invention also provides methods for treating cancer in a human in need thereof, the methods comprising administering to the human a combination of a Type I PRMT inhibitor and a Type II PRMT inhibitor, together with at least one of: a pharmaceutically acceptable carrier and a pharmaceutically acceptable diluent, thereby treating the cancer in the human. The present invention further provide a pharmaceutical composition comprising a therapeutically effective amount of a Type I PRMT inhibitor and a second pharmaceutical composition comprising a therapeutically effective amount of a Type II PRMT inhibitor.
