It is well known that inter-individual variability exists in the responses to many drugs. Many nongenetic factors, such as age, sex, diet, and organ function, are known to affect the therapeutic effects of drugs. However, recent advances in pharmacogenomics have revealed that genetic polymorphisms also significantly influence both the efficacy and the toxicity of drugs. Mutations in the genes encoding drug-metabolizing enzymes, transporters, and target molecules may alter their expression, activity, or affinity to drugs, thereby influencing the drugs pharmacokinetics and pharmacodynamics. Numerous studies have reported on the correlations between therapeutic outcomes and polymorphisms in drug-metabolizing enzymes, transporters, target molecules, and DNA repair enzymes. These pharmacogenomic discoveries are expected to be useful for the individualization and optimization of cancer chemotherapy.