apoB48R Inhibitors

apoB48R inhibitors predominantly revolve around the central theme of lipid metabolism, reflecting the crucial role of apoB48R in chylomicron remnant uptake. The direct inhibition of apoB48R might not be the primary action for most of these compounds, but their influence on lipid-related pathways can have implications on the protein's function. For instance, Ezetimibe's primary action is the blockage of NPC1L1, curbing intestinal cholesterol absorption. This reduction can, in turn, potentially influence the function of apoB48R. Similarly, the HMG-CoA reductase inhibitor, Atorvastatin, by reducing cholesterol synthesis in the liver, has a cascading effect on various lipid-related pathways, potentially influencing the role of apoB48R.

Compounds like Fenofibrate and Gemfibrozil operate through the activation of PPARα, thereby modulating lipid metabolism at a broader scale. In a somewhat different mechanism, agents like Cholestyramine and Colesevelam function as bile acid sequestrants, interfering with cholesterol's reabsorption in the intestines, which indirectly can influence the functioning of apoB48R.