Drug intelligence / Profile preview

statin + ezetimibe

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

This combination therapy involves the co-administration of a statin (specifically rosuvastatin or atorvastatin in the TOLERANT trial) and ezetimibe. Statins inhibit HMG-CoA reductase, the rate-limiting enzyme in hepatic cholesterol synthesis, while ezetimibe inhibits the NPC1L1 protein, reducing the absorption of biliary and dietary cholesterol in the small intestine. This dual mechanism is employed to achieve intensive LDL cholesterol lowering (target < 55 mg/dL) in high-risk patients, such as those with coronary artery disease following drug-eluting stent implantation. The TOLERANT trial (NCT05665582), sponsored by Yonsei University, specifically compares the tolerability and efficacy of high-dose rosuvastatin/ezetimibe (20/10 mg) versus atorvastatin/ezetimibe (40/10 mg) to determine the optimal regimen for maintaining stringent lipid targets in post-stenting patients.

Other names
statin + ezetimibstatin/ezetimibe combinationhigh-dose statin/ezetimibe combination therapy
02

Targets

NPC1L1 (Niemann-pick C1-Like 1 transporter)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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