Anacetrapib
Anacetrapib is a CETP inhibitor which was being developed to treat elevated cholesterol levels in an effort prevent cardiovascular disease.[1] In 2017 its development was abandoned by Merck.[2]
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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 | |
| Other names
MK-0859 | |
| Identifiers | |
3D model (JSmol) |
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| UNII | |
CompTox Dashboard (EPA) |
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| Properties | |
| C30H25F10NO3 | |
| Molar mass | 637.51 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
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Evidence
In 2017 REVEAL trial anacetrapib was shown to decrease the risk of repeat heart attacks in high-risk patients with previous acute coronary events.[3]
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See also
Other CETP inhibitors:
- Torcetrapib was developed by Pfizer until December 2006 but caused unacceptable increases in blood pressure and had net cardiovascular detriment.
- Dalcetrapib was developed by Hoffmann–La Roche until May 2012. It did not raise blood pressure and did raise HDL, but it showed no clinically meaningful efficacy.
- Evacetrapib was developed by Eli Lilly & Company until October 2015.
References
- Gutstein DE, Krishna R, Johns D, et al. (2012). "Anacetrapib, a Novel CETP Inhibitor: Pursuing a New Approach to Cardiovascular Risk Reduction". Clinical Pharmacology & Therapeutics. 91 (1): 109–122. doi:10.1038/clpt.2011.271. PMID 22130116.
- "Merck says will not seek approval of cholesterol treatment". Reuters. 2017. Retrieved 18 October 2017.
- Filippatos, TD; Kei, A; Elisaf, MS (29 September 2017). "Anacetrapib, a New CETP Inhibitor: The New Tool for the Management of Dyslipidemias?". Diseases. 5 (4): 21. doi:10.3390/diseases5040021. PMC 5750532. PMID 28961179.
Further reading
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