Target intelligence / Profile preview

Low-density lipoprotein and High-density lipoprotein cholesterol (LDL-C/HDL-C)

Target
LDL-C/HDL-C
Molecular classification
Lipoprotein, Lipid-protein complex, Other
01

Overview

Low-density lipoprotein (LDL) and High-density lipoprotein (HDL) cholesterol are clinical biomarkers representing the cholesterol content within specific lipoprotein particles (NIH, 2023). LDL particles transport cholesterol to peripheral tissues and are strongly associated with the development of atherosclerosis and coronary heart disease when present in excess (StatPearls, 2023). HDL particles facilitate reverse cholesterol transport, carrying cholesterol from the vasculature back to the liver for biliary excretion, which is generally considered cardioprotective (Wikipedia, 2024). While LDL and HDL are the focus of therapeutic intervention, they are not individual molecular targets; instead, pharmacological agents modulate their levels by interacting with specific proteins such as HMG-CoA reductase, PCSK9, or the LDL receptor (PubMed, 2021). Managing these lipoprotein levels is a primary strategy for reducing cardiovascular morbidity and mortality.

Other names
Low-density lipoprotein cholesterolHigh-density lipoprotein cholesterolLDL-CHDL-CBad cholesterolGood cholesterolLipoprotein cholesterol
02

Mechanism of action

Pharmacological agents modulate these levels by targeting specific proteins: statins inhibit HMG-CoA reductase to reduce hepatic cholesterol synthesis; PCSK9 inhibitors prevent LDL receptor degradation to increase clearance; ezetimibe inhibits the NPC1L1 transporter to reduce intestinal absorption; and fibrates activate PPAR-alpha to increase HDL synthesis and fatty acid oxidation.

03

Biological functions

Lipid transportCholesterol homeostasisReverse cholesterol transportOther
04

Disease associations

Cardiovascular diseaseAtherosclerosisDyslipidemiaHypercholesterolemiaOther
05

Safety considerations

MyopathyRhabdomyolysisHepatotoxicityIncreased risk of new-onset diabetes mellitusGastrointestinal distress
06

Interacting drugs

Atorvastatin

8 more in the full profile.

07

Biomarkers

Low-density lipoprotein cholesterol (LDL-C)High-density lipoprotein cholesterol (HDL-C)Apolipoprotein BApolipoprotein A-INon-HDL cholesterolLipoprotein(a)

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