Large differences are observed in chemotherapy response between breast cancer patients, with a substantial part of this variability being explained by genetic factors. Polymorphisms in genes encoding drug-metabolizing enzymes, drug transporters and drug targets influence the pharmacokinetics and pharmacodynamics of these anticancer drugs, leading to differences in therapeutic efficacy. Pharmacogenetic investigations of breast cancer therapeutics focused on these candidate loci have been performed. This article summarizes the status of research to identify polymorphisms in genes that influence response to the chemotherapeutic agents used in breast cancer treatment and suggests future directions for this line of research. Understanding the genetic factors that predispose patients to poor treatment outcomes will help guide individualized therapeutic strategies to obtain maximal benefit.