New approaches to atherosclerotic cardiovascular disease. the potentialities of torcetrapib
Related Experiment Video
Updated: Jul 8, 2026

Quantitative Analysis of Cellular Composition in Advanced Atherosclerotic Lesions of Smooth Muscle Cell Lineage-Tracing Mice
Published on: February 20, 2019
Jose Luis Pérez-Castrillon1, Antonio Dueñas-Laita
1Hospital Rio Hortega. University of Valladolid, Valladolid, Spain. castrv@terra.es
Insights
Torcetrapib, a cholesteryl ester-transfer protein (CETP) inhibitor, effectively raises high-density lipoprotein (HDL) cholesterol levels. This drug shows potential for treating atherosclerotic cardiovascular disease by increasing HDL and decreasing LDL cholesterol.
Area of Science:
- Cardiovascular Medicine
- Pharmacology
- Biochemistry
Background:
- Atherosclerosis remains a leading cause of mortality globally, despite existing low-density lipoprotein (LDL) cholesterol-lowering therapies.
- High-density lipoprotein (HDL) cholesterol's role in reverse cholesterol transport offers a potential therapeutic avenue for lipid removal from atheromas.
- Current guidelines recognize elevated HDL cholesterol as a negative risk factor for cardiovascular disease.
Purpose of the Study:
- To evaluate the efficacy of torcetrapib, a cholesteryl ester-transfer protein (CETP) inhibitor, in modulating lipid profiles.
- To assess the impact of torcetrapib on high-density lipoprotein (HDL) cholesterol and other key lipid parameters.
Main Methods:
- Torcetrapib was administered as monotherapy and in combination with statins.
- Changes in high-density lipoprotein (HDL) cholesterol, apolipoprotein A-I, low-density lipoprotein (LDL) cholesterol, apolipoprotein B, triglycerides, and total cholesterol were measured.
Main Results:
- Torcetrapib significantly increased HDL cholesterol and apolipoprotein A-I levels.
- The drug demonstrated a decrease in LDL cholesterol and apolipoprotein B levels.
- Torcetrapib did not substantially alter serum triglyceride or total cholesterol levels.
Conclusions:
- Torcetrapib effectively raises HDL cholesterol and reduces LDL cholesterol, presenting a potential new therapeutic strategy for atherosclerotic cardiovascular disease.
- Further clinical trials focusing on hard clinical endpoints are required to confirm the long-term benefits and safety of torcetrapib.
Abstract:
Atherosclerosis is the leading cause of death and disability in the developed world. Although the low-density lipoprotein (LDL) cholesterol lowering drugs reduce the mortality and morbidity associated with coronary artery disease, considerable mortality and morbidity remains. Reverse cholesterol transport mediated by high-density lipoproteins (HDL) may provide an independent pathway for lipid removal from atheroma. The current NCEP ATPIII include HDL-cholesterol > or =1.6 mmol/l as a negative risk factor. Torcetrapib is an inhibitor of cholesteryl ester-transfer protein (CETP) that increases high-density lipoprotein (HDL) cholesterol levels. The drug increases HDL-cholesterol and apolipoprotein A-I levels and decreases LDL-cholesterol and apolipoprotein B levels. The effect is showed in monotherapy and when administered in combination with statins. In addition, torcetrapib did not significantly change the serum levels of cholesterol and triglycerides. The raising HDL-cholesterol with torcetrapib could be a new approach to atherosclerotic cardiovascular disease although new trials based on hard clinical end points are necessary.
Related Concept Videos
Atherosclerosis III: Management
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
Pharmacogenomics: Identification of New Drug Targets
Lipid-Lowering Drugs: Statins and Miscellaneous Agents
Treatment for Pulmonary Arterial Hypertension: Receptor Tyrosine Kinase Inhibitors and Calcium Channel Blockers
TKIs, such as imatinib (Gleevec), are particularly effective in tackling the growth and mitogenic factors that become upregulated in PAH patients. These factors contribute to the...
Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme (ECE). Of...