Анацетрапиб

An orally active and potent cholesterol ester transfer protein (CETP) inhibitor for the treatment of atherosclerosis, in particular dyslipidemia.

This cholesteryl ester transfer protein (or CETP) inhibitor (FW = 637.51 g/mol; CAS 875446-37-0), also known by the code name MK-0859, reduces plasma cholesterol concentrations, thereby increasing serum highdensity lipoprotein levels and preventing cardiovascular disease associated with hypercholesteremia. X-ray crystal studies suggest that CETP is a crescent-shaped protein with a 6-nm hydrophobic tunnel traversing its core Both of the tunnel’s two entrances face the protein’s concave surface, which most likely is the interaction platform for binding HDL particles and engaging its lipoprotein constituents. CETP mediates the reciprocal transfer of neutral lipids (e.g., cholesteryl esters and triglycerides) and phospholipids between different lipoprotein fractions in blood plasma. Anacetrapib is unlike many CETP inhibitors, which increase systolic blood pressure. Anacetrapib also exhibits a low-to-moderate degree of absorption after oral dosing and majority of the absorbed dose is eliminated via oxidation to a series of hydroxylated metabolites that undergo conjugation with glucuronate before excretion into bile. Unlike torcetrapib, another CETP inhibitor, anacetrapib does not elevate blood pressure, alter electrolytes, or cause any significant side effects.