Ezetimibe phenoxy glucuronide is the primary active metabolite of ezetimibe, a medication used in the treatment of hypercholesterolemia, a condition characterized by high levels of cholesterol in the blood. As the glucuronide conjugate, it is responsible for the pharmacological activity of ezetimibe by inhibiting the absorption of cholesterol in the small intestine via blockade of the Niemann-Pick C1-Like 1 (NPC1L1) protein, thereby reducing the amount of cholesterol that enters the bloodstream. This makes it particularly effective in lowering low-density lipoprotein (LDL) cholesterol, often referred to as "bad" cholesterol.

The metabolite contributes to the efficacy when ezetimibe is used in combination with statins, another class of cholesterol-lowering drugs, to enhance overall treatment outcomes. By combining these two mechanisms—reducing cholesterol absorption and decreasing cholesterol production in the liver—patients can achieve better control over their cholesterol levels.

Additionally, it is beneficial for patients who cannot tolerate high doses of statins or those requiring additional cholesterol-lowering effects. It also plays a role in the management of familial hypercholesterolemia, a genetic disorder causing extremely high cholesterol levels from a young age.

Overall, its activity is crucial in reducing the risk of cardiovascular diseases, such as heart attacks and strokes, by maintaining healthier cholesterol levels. As a high-purity reagent (≥98%), it is commonly used in pharmaceutical research, analytical standards, and metabolic studies.