Antipsychotic drugs remain the mainstay of pharmacotherapy for schizophrenia. As there are large individual variations in efficacy and side-effects of antipsychotic drugs, there is a strong demand for personalized medication to treat schizophrenia. Pharmacogenetic research into antipsychotic drugs has examined a number of genetic variants and only a few polymorphisms have been found which promise to be associated with the therapeutic efficacy and side-effects of antipsychotic drugs. Brain-derived neurotrophic factor (BDNF) is a neurotrophin that plays a major role in neurogenesis and neuroplasticity, and in the modulation of several neurotransmitter systems including the dopaminergic system involved in the pathophysiology of schizophrenia. This review focused on the association between the BDNF gene Val66Met polymorphism and antipsychotic drugs. The BDNF Val66Met polymorphism has been related to the pathophysiology of schizophrenia, psychotic symptomatology, cognition, efficacy and side-effects of antipsychotic drugs. The BDNF Val66Met variants could be a promising target for antipsychotic medication options or developing next generation antipsychotic drugs. However, some studies showed inconsistent results due to sample size, ethnic differences and different antipsychotic drugs. Further studies will be required in this area to confirm the effect of the BDNF Val66Met polymorphism in the pathophysiology of schizophrenia and patients’ response to antipsychotic drugs, especially in a larger sample size and in different ethnic populations.