Erianin is the major bisbenzyl compound extracted from the traditional Chinese medicine Lindl. Erianin possesses many biological properties relevant to cancer prevention and therapy. The previous studies confirmed that antitumor effects of erianin are regulated with multiple signaling pathways. The mechanisms of erianin are numerous, and most of them induce cancer cell apoptosis that may be intrinsic or extrinsic and modulate the ROS/JNK signaling pathways. Invasion, migration, and angiogenesis represent emerging targets of erianin and support its anticancer properties. This review aimed to summarize the recent advances in the antitumor activity of erianin and to provide a rationale for further exploring the potential application of erianin in overcoming cancer in the future.