Presently provided are IDO inhibitors and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase treating indoleamine 2,3-dioxygenase (IDO) mediated inimunosuppression treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent treating tumor-specific immunosuppression associated with cancer and treating immunosuppression associated with an infectious disease.