| Message: | Product Description:
Anacetrapib, also known as MK-0859, is a potent and selective inhibitor of cholesteryl ester transfer protein (CETP) that exhibits strong inhibition against CETP-mediated transfer of cholesteryl esters and triglycerides with values of inhibition constant IC50 of 16 nM and 29 nM respectively. Anacetrapib is mainly metabolized by CYP3A4 through O-demethylation, hydroxylation on the biphenyl moiety and hydroxylation on the isopropyl side chain resulting in three oxidative metabolites M1, M2 and M3 respectively. Anacetrapib is being investigated for the treatment of primary hypercholesterolemia and mixed hyperlipidemia due to its impressive effects to lower low-density lipoprotein (LDL) cholesterol levels and increase high-density lipoprotein (HDL) cholesterol levels without any associated major adverse events.
Application:
1.Anacetrapib is a cholesteryl ester transfer protein (CETP) inhibitor currently in Phase III of development as a treatment for those with dyslipidemia and the risk of cardiovascular disease. The agent acts by inhibiting the CETP, which mediates the transfer of cholesterol esters from high-density lipoprotein cholesterol (HDL-C) to other lipoproteins. HDL-C has been inversely linked to cardiac risk and is thus a potential target for decreasing residual cardiovascular risk, which remains despite aggressive low-density lipoprotein cholesterol therapy with statin drugs.
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