BACKGROUND: The number of patients eligible for cardiovascular therapies in general is forecast to increase substantially in the coming decades. However, the current list of potential future cardiovascular blockbuster drugs is alarmingly short. There is thus a clear need for innovative strategies to increase the efficiency of drug development pipelines by establishing new sensitive biomarkers to monitor drug efficacy and safety in the context of complexity of lipoprotein metabolism targeted by the cardiovascular drugs.

METHODS: Metabolomics is a discipline dedicated to the systematic study of small molecules in cells, tissues and biofluids. Since lipids (including cholesterol), as well as other metabolites, are key constituents of lipoprotein particles and are thus part of the complex lipoprotein metabolism that includes exchange of lipids and metabolites with peripheral tissues, cardiovascular drug safety and efficacy needs to be addressed in the context of systemic lipid metabolism.

RESULTS/CONCLUSION: Metabolomics, lipidomics in particular, is expected to make an important impact on the discovery and development of cardiovascular therapies.