The class
Patent landscape review tracks CETP inhibitor development from 2000 through the termination of torcetrapib (Expert Opin Ther Pat 2009)
Original title: Cholesteryl ester transfer protein inhibitors as high-density lipoprotein raising agents
This review surveys patenting activity in cholesteryl ester transfer protein (CETP) inhibitors from 2000 to early 2009, a drug class developed to raise HDL cholesterol as a strategy against atherosclerosis-related disease. Phase III trials of torcetrapib, a Pfizer CETP inhibitor, were unexpectedly terminated after it increased cardiovascular events and mortality, effects attributed to compound-specific and off-target actions such as raised blood pressure and aldosterone. The authors report that dalcetrapib (JTT-705) and anacetrapib, neither reported to share the off-target effects of torcetrapib, were in phase III trials at the time of writing and expected to reveal whether CETP inhibition benefits atherosclerosis-related disease.
Original abstract
Background: Not only hypercholesterolemia, but also low levels of high-density lipoprotein cholesterol is a critical risk factor for atherosclerosis-related disease. Therefore, there has been great interest in identifying effective and selective cholesteryl ester transfer protein (CETP) inhibitors that can raise high-density lipoprotein. Recently, Phase III clinical studies of torcetrapib, one of the CETP inhibitors developed by researchers at Pfizer, were unexpectedly terminated because of an increase in cardiovascular events and mortality. Torcetrapib has some compound-specific and off-target effects, such as raising blood pressure and aldosterone, which could affect an increase in cardiovascular events and mortality.
Objective: The aim of this review is to provide an update (from 2000 to early 2009) on the patenting activity in the field of CETP inhibitors and the status of the most advanced compounds.
Conclusion: Dalcetrapib (JTT-705) and anacetrapib, which have not been reported to have the off-target effects of torcetrapib, are currently in Phase III. They are expected to reveal whether CETP inhibition is beneficial for atherosclerosis-related diseases.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 18 August 2026. Methods.