A Comprehensive Monograph on Ezetimibe (DB00973)

Introduction and Drug Identification

[Ezetimibe is a landmark small-molecule therapeutic agent and the first of its kind, belonging to the novel class of selective cholesterol-absorption inhibitors.][1][ Its development and introduction into clinical practice marked a significant advancement in the management of hyperlipidemia. The drug's therapeutic action is predicated on a unique mechanism that is distinct from the widely used statin class of drugs; rather than inhibiting the endogenous synthesis of cholesterol, ezetimibe targets its absorption in the gastrointestinal tract.][3][ This novel approach provides a complementary strategy for lowering elevated levels of low-density lipoprotein cholesterol (LDL-C).]

[Approved for medical use in the United States in 2002, ezetimibe has become a cornerstone of modern lipid-lowering therapy.][3][ It is frequently prescribed as an adjunctive treatment to statins, a combination that leverages two distinct and synergistic pathways to achieve more potent LDL-C reduction than either agent can accomplish alone. It is also utilized as a monotherapy for patients who are intolerant to statins or for whom statin therapy is otherwise inappropriate.][3][ The clinical importance and widespread adoption of ezetimibe are underscored by its prescription volume; in 2022, it was the 79th most commonly prescribed medication in the United States, accounting for over 8 million prescriptions.][3][ Its role in cardiovascular risk reduction has been solidified through major clinical outcome trials, establishing it as a valuable tool in the armamentarium against atherosclerotic cardiovascular disease.]