The discovery and characterization of P-glycoprotein (P-gp) as a mechanism of multidrug resistance (MDR) is widely recognized as a seminal contribution to the ongoing effort to reduce the morbidity and mortality associated with resistance to anticancer drugs. More recently, some of the ABC drug transporters have been shown to confer resistance to antibody–drug conjugates and proteolysis-targeting chimeras (PROTACs). High-resolution structural studies, biophysical approaches, and in silico analyses, together with compelling evidence that ABC transporters limit drug penetration into and effectiveness within the central nervous system, have greatly advanced our understanding of the mechanisms underlying drug transport by ABC drug transporters, including ABCB1 and ABCG2. These advances have, in turn, contributed to the development of promising strategies to overcome cancer chemoresistance, including radiation-based immunotherapies, thermal therapies, and nanomedicine. This meeting will bring together national and international experts in the field of multidrug resistance to discuss recent advances and emerging opportunities in this rapidly evolving area.