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Anacetrapib

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Anacetrapib
Names
Preferred IUPAC name (4S,5R)-5--3-{-2-yl]methyl}-4-methyl-1,3-oxazolidin-2-one
Other names MK-0859
Identifiers
CAS Number
3D model (JSmol)
ChEMBL
ChemSpider
KEGG
PubChem CID
UNII
CompTox Dashboard (EPA)
InChI
  • InChI=1S/C30H25F10NO3/c1-14(2)22-11-23(25(43-4)12-24(22)31)21-6-5-18(28(32,33)34)9-17(21)13-41-15(3)26(44-27(41)42)16-7-19(29(35,36)37)10-20(8-16)30(38,39)40/h5-12,14-15,26H,13H2,1-4H3/t15-,26-/m0/s1Key: MZZLGJHLQGUVPN-HAWMADMCSA-N
  • InChI=1/C30H25F10NO3/c1-14(2)22-11-23(25(43-4)12-24(22)31)21-6-5-18(28(32,33)34)9-17(21)13-41-15(3)26(44-27(41)42)16-7-19(29(35,36)37)10-20(8-16)30(38,39)40/h5-12,14-15,26H,13H2,1-4H3/t15-,26-/m0/s1Key: MZZLGJHLQGUVPN-HAWMADMCBN
SMILES
  • O=C2O(c1cc(cc(c1)C(F)(F)F)C(F)(F)F)(N2Cc4c(c3cc(c(F)cc3OC)C(C)C)ccc(c4)C(F)(F)F)C
Properties
Chemical formula C30H25F10NO3
Molar mass 637.51 g·mol
Except where otherwise noted, data are given for materials in their standard state (at 25 °C , 100 kPa). ☒verify (what is  ?) 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. In 2017 its development was abandoned by Merck.

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.

See also

Other CETP inhibitors:

References

  1. 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.
  2. "Merck says will not seek approval of cholesterol treatment". Reuters. 2017. Retrieved 18 October 2017.
  3. 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. 
Lipid-lowering agents (C10)
GI tract
Cholesterol absorption inhibitors, NPC1L1
Bile acid sequestrants/resins (LDL)
Liver
Statins (HMG-CoA reductase, LDL)
Niacin and derivatives (HDL and LDL)
MTTP inhibitors (VLDL)
ATP citrate lyase inhibitors (LDL)
Thyromimetics (VLDL)
Blood vessels
PPAR agonists (LDL)
Fibrates
Others
CETP inhibitors (HDL)
PCSK9 inhibitors (LDL)
ANGPTL3 inhibitors (LDL/HDL)
Combinations
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