Although treatment of different types of sexual dysfunction has improved in the past decade with the introduction of phosphodiesterase type 5 inhibitors and selective serotonin reuptake inhibitors, response rates to these targeted therapies are variable. There are a number of studies in the published literature that provide proof-of-concept that genetic variation contributes to the variable response. Pharmacogenomics will most likely be one part of our therapeutic armamentarium in the future and will provide a stronger scientific basis for optimizing drug therapy on the basis of each patient's genetic constitution. This article will review English language medical literature on the state-of-the-art genetic polymorphisms of drug targets, transporters and signaling molecules as well as pharmacogenetic studies of sexual dysfunction and suggested possible applications. Collectively, the data demonstrate that pharmacogenomics in the field of sexual medicine is still in its infancy. More research will provide further intriguing new discoveries in years to come.