The ATP-binding cassette (ABC) transporter family is a large class of ATP 
energy-dependent transmembrane proteins, and its primary function is to use the 
energy produced by ATP hydrolysis to transfer the substrate bound to the plasma 
membrane. This family is also closely related to multidrug resistance (MDR) in 
various diseases. Among the ABC transporter proteins, P-glycoprotein (P-gp), 
multidrug resistance-associated protein (MRP) and breast cancer resistance 
protein (BCRP) are the main members associated with MDR. At present, the roles 
of these transporters in therapeutic failures have been extensively studied and 
reviewed in cancer; however, they have rarely been described in autoimmune 
diseases (AIDs). AID is a group of chronic inflammatory diseases of unknown 
aetiology. AID's basic feature is the production of a large number of 
autoantibodies, which leads to extensive damage to multiple systems and multiple 
organs. Disease-modifying anti-rheumatic drugs (DMARDs) are commonly used in the 
treatment of AID, but a considerable number of patients have no response or 
develop resistance to these drugs over time. This phenomenon may be related to 
the abnormal expression of the ABC transporter, which leads to a decrease in the 
amount of drug entering cells that produce MDR. This article reviews the effects 
of DMARDs on the expression and function of P-gp, MRPs, and BCRP and the related 
molecular mechanism in the treatment of AID.