Drug intelligence / Profile preview

anacetrapib + simvastatin

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

Overview

Anacetrapib + simvastatin (often transliterated in Chinese contexts as ansetropi + simvastatin) is a combination pharmacological therapy designed to manage dyslipidemia and reduce cardiovascular risk. The combination consists of **anacetrapib**, a cholesteryl ester transfer protein (CETP) inhibitor, and **simvastatin**, an HMG-CoA reductase inhibitor (statin). Anacetrapib works by inhibiting the CETP-mediated transfer of cholesteryl esters from high-density lipoprotein (HDL) to low-density lipoprotein (LDL) and very-low-density lipoprotein (VLDL), which leads to a marked increase in HDL-C and a decrease in LDL-C. Simvastatin provides a complementary mechanism by inhibiting the rate-limiting enzyme in the cholesterol biosynthesis pathway in the liver. While the original developer of anacetrapib, Merck, discontinued its global development in 2017 due to modest clinical benefits and drug accumulation in adipose tissue, the combination has seen continued interest in specific markets. For instance, Hainan Helpson Medical and Biotechnology acquired patent rights for a specific composition of these two agents in China.

Other names
ansetropi + simvastatinanacetrapib/simvastatinansetropi simvastatin
02

Targets

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

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