Abstract: Disclosed is a pharmaceutical composition, comprising a first component and a second component, wherein the first component is selected from at least one of a farnesoid X receptor agonist and a precursor, an active metabolite, a stereoisomer, a pharmaceutically acceptable salt, an ester and a solvate thereof; and the second component is selected from at least one of a NPC1L1 receptor inhibitor and a precursor, an active metabolite, a stereoisomer, a pharmaceutically acceptable salt, an ester and a solvate thereof. The composition can be used in preventing and/or treating non-alcoholic fatty liver disease, diabetes or cardiovascular disease.