Evacetrapib: Difference between revisions

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__NOTOC__
__NOTOC__
{{Chembox
{{Chembox
| verifiedrevid = 461280529
| verifiedrevid = 461280529
| ImageFile=Evacetrapib.svg
| ImageFile=Evacetrapib.svg
| ImageSize=150px
| ImageSize=150px
| IUPACName=Trans-4-({(5''S'')-5-[{[3,5-bis(trifluoromethyl)phenyl]methyl}(2-methyl-2''H''-tetrazol-5-yl)amino]-7,9-dimethyl-2,3,4,5-tetrahydro-1''H''-benzazepin-1-yl}methyl) cyclohexanecarboxylic acid
| IUPACName=Trans-4-({(5''S'')-5-[{[3,5-bis(trifluoromethyl)phenyl]methyl}(2-methyl-2''H''-tetrazol-5-yl)amino]-7,9-dimethyl-2,3,4,5-tetrahydro-1''H''-benzazepin-1-yl}methyl) cyclohexanecarboxylic acid
| OtherNames = LY2484595
| OtherNames = LY2484595
| Section1 = {{Chembox Identifiers
| Section1 = {{Chembox Identifiers
| CASNo=1186486-62-3
| CASNo=1186486-62-3
|  CASNo_Ref = {{cascite|correct|??}}
|  CASNo_Ref = {{cascite|correct|??}}
|  PubChem =
|  PubChem =
| KEGG = D10121
| KEGG = D10121
| ChEMBL = 2017179
| ChEMBL = 2017179
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG_Ref = {{keggcite|correct|kegg}}
| SMILES = O=C([C@H]1CC[C@H](CN2CCC[C@H](N(CC3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)C4=NN(C)N=N4)C5=CC(C)=CC(C)=C52)CC1)O
| SMILES = O=C([C@H]1CC[C@H](CN2CCC[C@H](N(CC3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)C4=NN(C)N=N4)C5=CC(C)=CC(C)=C52)CC1)O
|  ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
|  ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 26286916
| ChemSpiderID = 26286916
|  InChI = 1/C31H36F6N6O2/c1-18-11-19(2)27-25(12-18)26(5-4-10-42(27)16-20-6-8-22(9-7-20)28(44)45)43(29-38-40-41(3)39-29)17-21-13-23(30(32,33)34)15-24(14-21)31(35,36)37/h11-15,20,22,26H,4-10,16-17H2,1-3H3,(H,44,45)/t20-,22-,26-/m0/s1
|  InChI = 1/C31H36F6N6O2/c1-18-11-19(2)27-25(12-18)26(5-4-10-42(27)16-20-6-8-22(9-7-20)28(44)45)43(29-38-40-41(3)39-29)17-21-13-23(30(32,33)34)15-24(14-21)31(35,36)37/h11-15,20,22,26H,4-10,16-17H2,1-3H3,(H,44,45)/t20-,22-,26-/m0/s1
|  InChIKey = IHIUGIVXARLYHP-YBXDKENTBY
|  InChIKey = IHIUGIVXARLYHP-YBXDKENTBY
|  StdInChI_Ref = {{stdinchicite|correct|chemspider}}
|  StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 1S/C31H36F6N6O2/c1-18-11-19(2)27-25(12-18)26(5-4-10-42(27)16-20-6-8-22(9-7-20)28(44)45)43(29-38-40-41(3)39-29)17-21-13-23(30(32,33)34)15-24(14-21)31(35,36)37/h11-15,20,22,26H,4-10,16-17H2,1-3H3,(H,44,45)/t20-,22-,26-/m0/s1
| StdInChI = 1S/C31H36F6N6O2/c1-18-11-19(2)27-25(12-18)26(5-4-10-42(27)16-20-6-8-22(9-7-20)28(44)45)43(29-38-40-41(3)39-29)17-21-13-23(30(32,33)34)15-24(14-21)31(35,36)37/h11-15,20,22,26H,4-10,16-17H2,1-3H3,(H,44,45)/t20-,22-,26-/m0/s1
|  StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
|  StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = IHIUGIVXARLYHP-YBXDKENTSA-N
| StdInChIKey = IHIUGIVXARLYHP-YBXDKENTSA-N
}}
}}


| Section2 = {{Chembox Properties
{{Chembox Properties
 
|  C=31 | H=36 | F=6 | N=6 | O=2
|  C=31 | H=36 | F=6 | N=6 | O=2
|  Appearance =
|  Appearance =
|  Density =
|  Density =
|  MeltingPt =
|  MeltingPt =
|  BoilingPt =
|  BoilingPt =
|  Solubility = }}
|  Solubility = }}
| Section3 = {{Chembox Hazards
| Section3 = {{Chembox Hazards
|  MainHazards =
|  MainHazards =
|  FlashPt =
|  FlashPt =
|  Autoignition = }}
|  Autoignition = }}
}}
}}
{{SI}}
{{SI}}
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==Overview==
==Overview==
'''Evacetrapib''' is a [[medication|drug]] under development by [[Eli Lilly & Company]] (investigational name '''LY2484595''') that inhibits [[cholesterylester transfer protein]], which transfers  and thereby increases [[high-density lipoprotein]] and lowers [[low-density lipoprotein]]. It is thought that modifying lipoprotein levels modifies the risk of [[cardiovascular disease]].<ref name="pmid21957197"/> The first CETP inhibitor, [[torcetrapib]], was unsuccessful because it increased levels of the hormone [[aldosterone]] and increased [[blood pressure]],<ref name="pmid19522058"/> which led to excess cardiac events when it was studied.<ref name="pmid19522058"/> Evacetrapib does not have the same effect.<ref name="pmid21957197">{{cite journal |author=Cao G, Beyer TP, Zhang Y, ''et al.'' |title=Evacetrapib is a novel, potent, and selective inhibitor of cholesteryl ester transfer protein that elevates HDL cholesterol without inducing aldosterone or increasing blood pressure |journal=J. Lipid Res. |volume=52 |issue=12 |pages=2169–76 |year=2011 |month=December |pmid=21957197 |doi=10.1194/jlr.M018069 |url=}}</ref> When studied in a small [[clinical trial]] in people with elevated LDL and low HDL, significant improvements were noted in their lipid profile.<ref name=Nicholls>{{cite journal | author=Nicholls SJ, Brewer HB, Kastelein JJ, Krueger KA, Wang MD, Shao M, Hu B, McErlean E, Nissen SE | title=Effects of the CETP inhibitor evacetrapib administered as monotherapy or in combination with statins on HDL and LDL cholesterol | journal=JAMA | year=2011 | volume=306 | issue=19 | pages=2099–109 | doi=10.1001/jama.2011.1649}}</ref>
Evacetrapib is a [[medication|drug]] under development by [[Eli Lilly & Company]] (investigational name LY2484595) that inhibits [[cholesterylester transfer protein]], which transfers  and thereby increases [[high-density lipoprotein]] and lowers [[low-density lipoprotein]]. It is thought that modifying lipoprotein levels modifies the risk of [[cardiovascular disease]].<ref name="pmid21957197"/> The first CETP inhibitor, [[torcetrapib]], was unsuccessful because it increased levels of the hormone [[aldosterone]] and increased [[blood pressure]],<ref name="pmid19522058"/> which led to excess cardiac events when it was studied.<ref name="pmid19522058"/> Evacetrapib does not have the same effect.<ref name="pmid21957197">{{cite journal |author=Cao G, Beyer TP, Zhang Y, ''et al.'' |title=Evacetrapib is a novel, potent, and selective inhibitor of cholesteryl ester transfer protein that elevates HDL cholesterol without inducing aldosterone or increasing blood pressure |journal=J. Lipid Res. |volume=52 |issue=12 |pages=2169–76 |year=2011 |month=December |pmid=21957197 |doi=10.1194/jlr.M018069 |url=}}</ref> When studied in a small [[clinical trial]] in people with elevated LDL and low HDL, significant improvements were noted in their lipid profile.<ref name=Nicholls>{{cite journal | author=Nicholls SJ, Brewer HB, Kastelein JJ, Krueger KA, Wang MD, Shao M, Hu B, McErlean E, Nissen SE | title=Effects of the CETP inhibitor evacetrapib administered as monotherapy or in combination with statins on HDL and LDL cholesterol | journal=JAMA | year=2011 | volume=306 | issue=19 | pages=2099–109 | doi=10.1001/jama.2011.1649}}</ref>




Revision as of 12:46, 26 April 2013

Template:Chembox E number
Evacetrapib
Error creating thumbnail: File missing
Names
IUPAC name
Trans-4-({(5S)-5-[{[3,5-bis(trifluoromethyl)phenyl]methyl}(2-methyl-2H-tetrazol-5-yl)amino]-7,9-dimethyl-2,3,4,5-tetrahydro-1H-benzazepin-1-yl}methyl) cyclohexanecarboxylic acid
Other names
LY2484595
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
ECHA InfoCard Lua error in Module:Wikidata at line 879: attempt to index field 'wikibase' (a nil value). Lua error in Module:Wikidata at line 879: attempt to index field 'wikibase' (a nil value).
KEGG
Properties
C31H36F6N6O2
Molar mass 638.66 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
☑Y verify (what is ☑Y☒N ?)
Infobox references

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Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Raviteja Guddeti, M.B.B.S. [2]

Overview

Evacetrapib is a drug under development by Eli Lilly & Company (investigational name LY2484595) that inhibits cholesterylester transfer protein, which transfers and thereby increases high-density lipoprotein and lowers low-density lipoprotein. It is thought that modifying lipoprotein levels modifies the risk of cardiovascular disease.[1] The first CETP inhibitor, torcetrapib, was unsuccessful because it increased levels of the hormone aldosterone and increased blood pressure,[2] which led to excess cardiac events when it was studied.[2] Evacetrapib does not have the same effect.[1] When studied in a small clinical trial in people with elevated LDL and low HDL, significant improvements were noted in their lipid profile.[3]


Evacetrapib is one of two CETP inhibitors currently being evaluated (the other being anacetrapib).[1] Two other CETP inhibitors (torcetrapib and dalcetrapib) were discontinued during trials due to increased deaths and little identifiable cardiovascular benefit (despite substantial increases in HDL). Some hypothesize that CETP inhibitors may still be useful in the treatment of dyslipidemia, though significant caution is warranted.[2]


References

  1. ↑ 1.0 1.1 1.2 Cao G, Beyer TP, Zhang Y; et al. (2011). "Evacetrapib is a novel, potent, and selective inhibitor of cholesteryl ester transfer protein that elevates HDL cholesterol without inducing aldosterone or increasing blood pressure". J. Lipid Res. 52 (12): 2169–76. doi:10.1194/jlr.M018069. PMID 21957197. Unknown parameter |month= ignored (help)
  2. ↑ 2.0 2.1 2.2 Joy T, Hegele RA (2009). "The end of the road for CETP inhibitors after torcetrapib?". Curr. Opin. Cardiol. 24 (4): 364–71. doi:10.1097/HCO.0b013e32832ac166. PMID 19522058. Unknown parameter |month= ignored (help)
  3. ↑ Nicholls SJ, Brewer HB, Kastelein JJ, Krueger KA, Wang MD, Shao M, Hu B, McErlean E, Nissen SE (2011). "Effects of the CETP inhibitor evacetrapib administered as monotherapy or in combination with statins on HDL and LDL cholesterol". JAMA. 306 (19): 2099–109. doi:10.1001/jama.2011.1649.


Template:Lipid modifying agents

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