**4. Summary**

Hypercholesterolemia is a complex disorder which presents in different forms, including the familial form, with varying underlying aetiology, and contributes substantially to CAD manifestation. Predisposing variables for the disease include modifiable risk traits, such as diet, overweight and obesity, that are controllable by adopting healthy eating habits and exercise, for example. However, diet alone is often not adequate to achieve the desired lipid lowering effect in individuals harbouring very high cholesterol levels, such as in familial hypercholesterolemia. This necessitates the use of lipid lowering medication to reduce its production or absorption or other forms of therapy including LDL apheresis or surgery. It is now well established that the response to anti‐lipidemic therapy depends on genetic changes in the disease‐causing as well as ADME‐related genes, and the impact of these gene‐drug response relationships will depend on ethnicity. Inter‐ethnical variability in pharmacokinetics of anti‐lipidemic agents may trigger unexpected outcomes such as therapeutic failure, adverse effects and toxicity in individuals of different ethnic origin undergoing therapy. Hence, in‐ depth studies on these relationships have the huge potential of achieving optimal quality use of drugs as well as improving the efficacy and safety of both prospective and currently available anti‐lipidemic therapeutic agents.
