Anacetrapib
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Preferred IUPAC name (4S,5R)-5-[3,5-Bis(trifluoromethyl)phenyl]-3-{[4′-fluoro-2′-methoxy-5′-(propan-2-yl)-4-(trifluoromethyl)[1,1′-biphenyl]-2-yl]methyl}-4-methyl-1,3-oxazolidin-2-one | |
Other names MK-0859 | |
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Properties | |
Chemical formula | 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). N verify (what is YN ?) Infobox references |
Chemical compound
Anacetrapib is a CETP inhibitor which was being developed to treat elevated cholesterol levels in an effort to prevent cardiovascular disease.[1] In 2017 its development was abandoned by Merck.[2]
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]
See also
Other CETP inhibitors:[citation needed]
- 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 and 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. S2CID 36510986.
- ^ "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
- WO 2007005572, Miller, Ross A. & Cote, Aaron S., "Process for synthesizing a CETP inhibitor", published 2007-01-11, assigned to Merck & Co. Inc.
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Cholesterol absorption inhibitors, NPC1L1 | |
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Bile acid sequestrants/resins (LDL) |
Statins (HMG-CoA reductase, LDL) | |
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Niacin and derivatives (HDL and LDL) | |
MTTP inhibitors (VLDL) | |
ATP citrate lyase inhibitors (LDL) | |
Thyromimetics (VLDL) |
PPAR agonists (LDL) |
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CETP inhibitors (HDL) |
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PCSK9 inhibitors (LDL) | |||||
ANGPTL3 inhibitors (LDL/HDL) |
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III