Anacetrapib
{{chembox
| Verifiedfields = changed
| verifiedrevid = 444391072
| ImageFile = Anacetrapib.svg
| ImageSize = 200px
| PIN = (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
| OtherNames = MK-0859
|Section1={{Chembox Identifiers
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 9731205
| 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/s1
| InChIKey = MZZLGJHLQGUVPN-HAWMADMCBN
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 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/s1
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = MZZLGJHLQGUVPN-HAWMADMCSA-N
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = P7T269PR6S
| CASNo_Ref = {{cascite|correct|??}}
| CASNo = 875446-37-0
| PubChem = 11556427
| ChEMBL_Ref = {{ebicite|changed|EBI}}
| ChEMBL = 1800807
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D08855
| SMILES = O=C2O[C@H](c1cc(cc(c1)C(F)(F)F)C(F)(F)F)[C@@H](N2Cc4c(c3cc(c(F)cc3OC)C(C)C)ccc(c4)C(F)(F)F)C
}}
|Section2={{Chembox Properties
| Formula = C30H25F10NO3
| MolarMass = 637.51 g·mol−1
| Appearance =
| Density =
| MeltingPt =
| BoilingPt =
| Solubility =
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|Section3={{Chembox Hazards
| MainHazards =
| FlashPt =
| AutoignitionPt =
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Anacetrapib is a CETP inhibitor which was being developed to treat elevated cholesterol levels in an effort to prevent cardiovascular disease.
{{cite journal
|vauthors =Gutstein DE, Krishna R, Johns D
|title=Anacetrapib, a Novel CETP Inhibitor: Pursuing a New Approach to Cardiovascular Risk Reduction
|journal=Clinical Pharmacology & Therapeutics
|volume=91 |issue=1 |pages=109–122
|year=2012
|doi=10.1038/clpt.2011.271
|pmid=22130116
|s2cid=36510986
|url=http://www.nature.com/clpt/journal/v91/n1/full/clpt2011271a.html
| display-authors=etal|url-access=subscription
}} In 2017 its development was abandoned by Merck.{{cite news|title=Merck says will not seek approval of cholesterol treatment|url=https://www.reuters.com/article/us-merck-cholesterol/merck-says-will-not-seek-approval-of-cholesterol-treatment-idUSKBN1CG2W1|accessdate=18 October 2017|work=Reuters|date=2017}}
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.{{cite journal|last1=Filippatos|first1=TD|last2=Kei|first2=A|last3=Elisaf|first3=MS|title=Anacetrapib, a New CETP Inhibitor: The New Tool for the Management of Dyslipidemias?|journal= Diseases|date=29 September 2017|volume=5|issue=4|doi=10.3390/diseases5040021|pmid=28961179|pmc=5750532|page=21|doi-access=free}}
See also
Other CETP inhibitors:{{cn|date=March 2023}}
- 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
{{Reflist}}
Further reading
- {{cite patent | country=WO | number=2007005572|title=Process for synthesizing a CETP inhibitor|pubdate=2007-01-11|assign=Merck & Co. Inc.|inventor1-last=Miller|inventor1-first=Ross A.
|inventor2-last=Cote|inventor2-first=Aaron S.}}
{{Lipid modifying agents}}