Drug intelligence / Profile preview

atorvastatin + torcetrapib

Development stage
Discontinued
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Atorvastatin + torcetrapib was a fixed-dose combination therapy developed by Pfizer for the treatment of hypercholesterolemia and the prevention of cardiovascular disease. The combination paired atorvastatin, a standard-of-care HMG-CoA reductase inhibitor (statin) used to lower LDL cholesterol, with torcetrapib, a first-in-class cholesteryl ester transfer protein (CETP) inhibitor designed to raise HDL cholesterol levels. By inhibiting CETP, the drug aimed to prevent the transfer of cholesterol from HDL to LDL and VLDL particles. Although the combination successfully raised HDL by 55-60% and lowered LDL by 50-60%, Pfizer abruptly terminated the Phase III ILLUMINATE trial in December 2006. The decision followed the discovery of an increased risk of mortality and cardiovascular events in the combination arm, later attributed to off-target effects of torcetrapib such as increased blood pressure and elevated aldosterone levels.

Brand names
None found
Other names
torcetrapib + atorvastatintorcetrapib/atorvastatin
02

Targets

CETPHMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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