Abstract: Auranofin, a gold(I) compound, is a thioredoxin reductase inhibitor previously approved by the U.S. FDA for the treatment of rheumatoid arthritis. Auranofin has been found to have anti-tumor activity in some solid tumors. Auranofin exerts anti-tumor activity of inhibiting proliferation, migration and invasion of tumor cells via inducing apoptosis by inhibiting thioredoxin reductase. Auranofin is currently approved in clinical trials for the treatment of ovarian and lung cancers. Although auranofin has shown good anti-tumor effect in many studies, the effect of single auranofin treatment is still not desirable. This leads to further research of auranofin combination therapy. Recently progress has shown that auranofin in combination with several drugs achieve has desirable outcomes. In this review, the studies of auranofin combination therapy was summarized, and some ideas and strategies was provided for the combination of auranofin and other drugs in cancer treatment.