Related Experiment Video
Updated: Aug 10, 2026

Differential Effects of Lipid-lowering Drugs in Modulating Morphology of Cholesterol Particles
Published on: November 10, 2017
Torcetrapib and atorvastatin: a novel combination therapy for dyslipidemia
1Department of Environmental Medicine, University of Rochester, School of Medicine and Dentistry, Rochester, New York 14642, USA. grazyna_zareba@urmc.rochester.edu
Insights
New cholesterol ester transfer protein (CETP) inhibitors, like torcetrapib, significantly raise high-density lipoprotein (HDL) and lower low-density lipoprotein (LDL) cholesterol. Combination therapy with statins shows promise for cardiovascular disease risk reduction.
Area of Science:
- Cardiovascular Medicine
- Pharmacology
- Biochemistry
Background:
- Low-density lipoproteins (LDL) and high-density lipoproteins (HDL) are key modulators of cardiovascular disease risk.
- Statins are widely used to lower LDL and triglycerides in hypercholesterolemia.
- Cholesterol ester transfer protein (CETP) inhibitors represent a novel drug class for lipid management.
Purpose of the Study:
- To evaluate the efficacy and safety of torcetrapib, a CETP inhibitor, in combination with atorvastatin.
- To assess the impact of torcetrapib on HDL and LDL cholesterol levels.
- To determine the potential of CETP inhibition in reducing atherosclerosis risk.
Main Methods:
- Administration of torcetrapib alone and in combination with atorvastatin.
- Monitoring of changes in high-density lipoprotein (HDL) and low-density lipoprotein (LDL) cholesterol levels.
- Assessment of safety and tolerability of the combination therapy.
Main Results:
- Torcetrapib significantly increased HDL cholesterol by 46% alone and 61% with atorvastatin.
- Combination therapy with torcetrapib and atorvastatin further reduced LDL cholesterol compared to atorvastatin alone.
- Doubling torcetrapib dosage led to over 100% increase in HDL; combination therapy was safe and well-tolerated.
Conclusions:
- Torcetrapib, a CETP inhibitor, effectively raises HDL and lowers LDL cholesterol.
- Combination therapy with torcetrapib and statins demonstrates favorable lipid-modifying effects and appears safe.
- Ongoing large trials will establish the clinical efficacy of this combination in reducing cardiovascular risk.
Abstract:
Epidemiological studies have identified both low-density lipoproteins (LDL) and high-density lipoproteins (HDL) as independent factors that modulate the risk of cardiovascular disease. Statins (HMG-CoA reductase inhibitors) that lower LDL and triglyceride levels are widely used for the treatment of hypercholesterolemia. Recently, a new class of drugs, cholesterol ester transfer protein (CETP) inhibitors, which significantly raise HDL and lower LDL, has been developed. Torcetrapib, a CETP inhibitor, has been shown to be effective, safe and well tolerated when used in combination with atorvastatin therapy. Torcetrapib has been shown to increase HDL cholesterol levels by 46% when given alone and by 61% when given in combination with atorvastatin, as well as to decrease LDL cholesterol levels by more than that achieved by atorvastatin alone. When the dosage of torcetrapib was doubled (at maximum tolerated dose), HDL increased by over 100%. Combination therapy appeared safe and well tolerated. Large trials evaluating the efficacy and safety of torcetrapib in combination therapy with atorvastatin are now in progress in order to establish whether CETP inhibition in combined therapy with statins will reduce the risk for atherosclerosis.
Related Concept Videos
Lipid-Lowering Drugs: Statins and Miscellaneous Agents
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...
Atherosclerosis III: Management
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...
Pharmacogenomics: Identification of New Drug Targets
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...