| Anacetrapib | |
|---|---|
 |
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| 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
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| Identifiers | |
| CAS number | 875446-37-0 |
| PubChem | 11556427 |
| Properties | |
| Molecular formula | C30H25F10NO3 |
| Molar mass | 637.51 g·mol−1 |
| Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa) | |
| Infobox references | |
Anacetrapib (USAN,[1] pINN; codenamed MK-0859, Merck) is a CETP inhibitor being developed to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease. It has been in Phase I clinical trials; preliminary results appear encouraging,[2] although long-term safety data are lacking.
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.
See also
- Torcetrapib, another CETP inhibitor unsuccessfully developed by Pfizer
References
- ^ "Statement on a nonproprietary name adopted by the USAN Council: Anacetrapib". American Medical Association. 2007. http://www.ama-assn.org/ama1/pub/upload/mm/365/anacetrapib.pdf. Retrieved 2008-01-19.
- ^ Krishna R, Anderson MS, Bergman AJ, et al. (2007). "Effect of the cholesteryl ester transfer protein inhibitor, anacetrapib, on lipoproteins in patients with dyslipidaemia and on 24-h ambulatory blood pressure in healthy individuals: two double-blind, randomised placebo-controlled phase I studies". Lancet 370 (9603): 1907–14. doi:. PMID 18068514.
Bloomfield D, Carlson GL, Sapre A, et al. Efficacy and safety of the cholesteryl ester transfer protein inhibitor anacetrapib as monotherapy and co-administered with atorvastatin in dyslipidemic patients. Am Heart J 2009; 157:352-360.
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