Abstract Tuberculosis (TB) is an infectious disease caused by Mycobacterium tuberculosis (Mtb) . With the emergence of multidrug-resistant TB (MDR-TB) and extensively drug-resistant TB (XDR-TB), the treatment of TB has become more severe. In recent years, studies have found that the existence of efflux pumps in Mycobacterium tuberculosis is one of the reasons for its drug resistance. The efflux pumps of major facilitator superfamily (MFS), ATP-Binding Cassette (ABC), resistance-nodulation-division (RND) and small multidrug resistance (SMR) have been found in Mtb. However, the drug resistance mediated by Mtb efflux pumps still remains largely unknown, and there is not much work to develop efflux pump inhibitors from the perspective of new drug discovery. This article reviews the structure and function of the efflux pumps of ABC, MFS, RND and SMR of Mtb, as well as the research progress of efflux pump inhibitors of Mtb.