Dietary fats and cholesterol

Dietary fats and cholesterol represent a broad category of exogenous macronutrients, primarily triglycerides and sterols, that are essential for human physiology but are not themselves specific molecular therapeutic targets. They serve as critical energy sources, structural components of cellular membranes, and precursors for the synthesis of steroid hormones and bile acids (NIH, 2023). In a pharmacological context, the term is considered 'incorrect' as a target because drugs actually interact with the proteins responsible for their processing, such as pancreatic lipase (inhibited by orlistat) or the Niemann-Pick C1-Like 1 (NPC1L1) transporter (inhibited by ezetimibe) (StatPearls, 2023). Excessive intake or impaired metabolism of these lipids is a primary driver of hyperlipidemia and atherosclerosis, leading to significant cardiovascular morbidity (PubMed, 2022). Consequently, therapeutic strategies focus on limiting the absorption or enhancing the clearance of these substances to manage metabolic and heart diseases (PubChem, 2024).

Other names

Dietary lipidsExogenous cholesterolTriglyceridesDietary sterolsAlimentary lipids

Inhibition of intestinal absorption through the targeting of specific enzymes (e.g., pancreatic lipase) or transporters (e.g., NPC1L1), or the sequestration of bile acids to promote hepatic cholesterol consumption.