Background: Ezetimibe is an inhibitor of the intestinal absorption of cholesterol. There are different cholesterol transporters in small intestine and one of the most important is Niemann-Pick C1L1 protein (NPC1L1), who is the therapeutic target of ezetimibe. When we talk about cholesterol gallstones disease, we deal with a public health problem, whose pharmacological treatment is limited. Ursodeoxycholic acid is used to dissolve cholesterol stones, and statins are other drugs with possible applications in the treatment of this disease.
Objective: Our main purpose is to discuss how is that the authors have reported on the effects of ezetimibe in cholesterol gallstones disease and to make a proposal on different mechanisms of action that can contribute to the future treatment of this disease.
Results: When gallstones generate symptoms, medical treatment indicates gallbladder removal. In different scientific studies, ezetimibe has been studied as a drug for preventing and treating cholesterol gallstones; however, is not the same dissolve cholesterol gallstones (treatment) than inhibit their formation (prevention). In the twenty-first century, there seems to be a broad interest in studying the intestinal absorption of cholesterol and associate it with the treatment of gallstones. It is an interesting research pathway in the research of treatment and prevention of gallstones.
Conclusion: Ezetimibe is a drug that needs more clinical studies to be considered as an agent for the treatment and prevention of cholesterol gallstones.
Keywords: Ezetimibe, cholesterol gallstones, prevention, NPC1L1 protein, gallbladder, mice.