Breast Cancer Resistance Protein (BCRP) is a membrane-associated protein and a member of the the super family of ATP-binding cassette (ABC) transporters known to confer multidrug resistance (MDR) to a number of important anticancer agent and play an important function in governing drug absorption. This book deals about the development of homology model of BCRP and its correspondence with experimentally known topology. This study also helped to understand the protein dynamics of BCRP through coarse-grained normal mode analysis. Structural analysis of substrate specificity bestowed by specific amino acids and its interaction with various synthetic and natural compounds provided clues of developing an efficient inhibitor.