OBJECTIVES The objective of the study was to explore the applicability of pharmacogenomics in ART (Antiretro viral therapy). METHODS Pharmacogenomic studies in HIV patients were identified from the database of WHO, Pubmed, Clinical trials.gov and relevant grey literature from 2000-2008. Two reviewers independently extracted data. RESULTS Pharmacogenomics provides a powerful support to investigate variable responses to antiretroviral therapy. To date, few antiretrovirals appear to have a clear genotype–phenotype correlation. However, such correlations have been demonstrated for CYP2B6 and efavirenz disposition, HLA-B*5701 and abacavir hypersensitivity, and UGT1A1 and atazanavir hyperbilirubinemia. Clinically significant and confirmed pharmacogenomic relationships were identified for three ART drugs. Out of 405 studies, 6/202 studies were identified as relevant to CYP2B6 and efavirenz disposition (2RCTs, 1 nRCT and 3 pharmacokinetic studies). Three (3/118) studies were identified for HLA-B*5701 and abacavir hypersensitivity (2 RCTs and 1 nRCT) and 2/85 studies for UGT1A1 and atazanavir hyperbilirubinemia (1RCT and 1nRCT). Studies (2/6) revealed that genotype and sex were identified as predictive covariates of efavirenz disposition. Studies (2/3) across the world have consistently demonstrated that HLA-B*5701 predicts the likelihood of hypersensitivity reactions to abacavir. As a consequence, pharmacogenetic screening for HLA-B*5701 has entered routine clinical practice and is recommended in most guidelines before starting an abacavir containing regimen. Studies (1/2) show that polymorphisms at MDR1-3435 significantly influence atazanavir plasma concentrations, although ATV plasma concentrations directly correlate with bilirubin levels, the risk of severe hyperbilirubinemia is further increased in the presence of the UGT1A1-TA7 allele. CONCLUSIONS Although the wider applicability of pharmacogenomic relationships is prevalent and its use in clinical practice is still limited. Pharmacogenomics can greatly contribute in taking more adequate therapeutic decisions and to optimise treatment for HIV/AIDS.