Anacetrapib 875446-37-0

Anacetrapib

Anacetrapib (USAN, pINN; codenamed MK-0859, Merck) is a CETP inhibitor being developed to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease. It is currently in a Phase III trial designed to assess its effects on LDL, HDL, and clinically measurable cardiovascular events, and safety; results are anticipated in 2010. At the 16th International Symposium on Drugs Affecting Lipid Metabolism (New York, Oct 4-7, 2007), Merck reported on a Phase IIb study. The eight week study reported dosage correlated reduction in LDL-C and increases in HDL-C levels with no corresponding increases in blood pressure in any cohort. The increase in HDL was particularly significant, averaging 44 percent, 86 percent, 139 percent and 133 percent at doses of 10 mg, 40 mg, 150 mg and 300 mg.

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Systematic (IUPAC) name: (4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-({2-[4-fluoro-2-methoxy-5-(propan-2-yl)phenyl]-5-(trifluoromethyl)phenyl}methyl)-4-methyl-1,3-oxazolidin-2-one
Anacetrapib CAS number: 875446-37-0
ATC code: L01XX01
PubChem: 11556427
DrugBank:
Formula: C30H25F10NO3
Molecular mass: 637.51 g·mol−1 g/mol
Anacetrapib Assay/Purity: Typically NLT 98%
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