Target intelligence / Profile preview

Very-low-density lipoprotein production (VLDL)

Target
VLDL
Molecular classification
Other, Metabolic process
01

Overview

Very-low-density lipoprotein is a lipoprotein complex produced primarily in the liver that is responsible for transporting endogenously synthesized triglycerides and cholesterol to peripheral tissues via the bloodstream. VLDL particles are assembled in hepatocytes from triglycerides, cholesterol, and apolipoproteins—most notably Apo B-100—with the assistance of microsomal triglyceride transfer protein. Once secreted, VLDL undergoes lipolysis and conversion into intermediate-density lipoproteins and then low-density lipoproteins, a process central for lipid homeostasis. Abnormalities in VLDL production, composition, and clearance are major contributors to atherosclerosis, metabolic syndrome, and other cardiometabolic diseases.

Other names
VLDL (for the lipoprotein particle)Very-low-density lipoprotein particleEndogenous triglyceride–rich lipoproteinHepatic VLDL
02

Mechanism of action

Inhibition of microsomal triglyceride transfer protein (blocks VLDL particle assembly and secretion); Reduction of hepatic triglyceride synthesis (lowers substrate for VLDL assembly); Enhancement of lipoprotein lipase activity (increases VLDL catabolism).

03

Biological functions

Lipid transportCholesterol homeostasisTriglyceride delivery to peripheral tissuesRegulation of blood pressure (via downstream signaling)
04

Disease associations

Cardiovascular disease (atherosclerosis, coronary heart disease)Diabetes/metabolic syndromeNon-alcoholic fatty liver diseaseHyperlipidemia
05

Safety considerations

Hepatic steatosis (fatty liver) with MTP inhibitionIncreased risk of fat-soluble vitamin deficiency (due to reduced VLDL export)Dyslipidemia and hypertriglyceridemiaDrug interactions leading to muscle toxicity (statins/fibrates)
06

Interacting drugs

Lomitapide (inhibits MTP)

3 more in the full profile.

07

Biomarkers

Plasma VLDL concentrationApo B-100 (quantifying apoB-containing lipoproteins)Triglyceride levelsVLDL particle size (NMR lipoprotein profiling)

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