The mechanism of ezetimibe is quite different from a currently available class of drugs known as "bile acid sequestrants," which lower cholesterol by physically binding to bile acids in the small intestine.  Ezetimibe lowers cholesterol through a unique mechanism of action by inhibiting cholesterol absorption in the intestine. This mechanism of action makes the agent complementary to statins, which work in the liver. Patients who take ezetimibe with a statin can achieve additional reductions in LDL and total cholesterol. 

In clinical trials, ezetimibe was generally well tolerated with an overall side effect profile similar to placebo. The agent is administered as a once-daily tablet in a single 10-mg strength. It can be taken with or without food.