evacetrapib profile

ID Source	ID
PubMed CID	49836058
CHEMBL ID	2017179
SCHEMBL ID	141340
SCHEMBL ID	108602
SCHEMBL ID	108367
CHEBI ID	188637
MeSH ID	M0568701

ID Source

PubMed CID

49836058

CHEMBL ID

2017179

SCHEMBL ID

141340

SCHEMBL ID

108602

SCHEMBL ID

108367

CHEBI ID

188637

MeSH ID

M0568701

Synonyms (59)

Synonym
HY-13327
4-[[(5s)-5-[[3,5-bis(triluoromethyl)phenyl]methyl-(2-methyltetrazol-5-yl)amino]-7,9-dimethyl-2,3,4,5-tetrahydro-1-benzazepin-1-yl]methyl]cyclohexane-1-carboxylic acid
CHEBI:188637
evacetrapib ,
evacetrapib (usan)
D10121
1186486-62-3
bdbm50381415
evacetrapib (ly2484595)
ly 2484595
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
51xwv9k850 ,
unii-51xwv9k850
ly-2484595
ly2484595
cyclohexanecarboxylic acid, 4-(((5s)-5-(((3,5-bis(trifluoromethyl)phenyl)methyl)(2- methyl-2h-tetrazol-5-yl)amino)-2,3,4,5-tetrahydro-7,9-dimethyl-1h-1-benzazepin-1- yl)methyl)-, trans-
evacetrapib [usan:inn]
CHEMBL2017179
(1r,4r)-4-{[(5s)-5-({[3,5-
PB36744
bis(trifluoromethyl)phenyl]methyl}(2-methyl-2h-
tetrahydro-1h-1-benzazepin-1-yl]methyl}cyclohexane-1-
1,2,3,4-tetrazol-5-yl)amino)-7,9-dimethyl-2,3,4,5-
CS-0658
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
cyclohexanecarboxylic acid, 4-(((5s)-5-(((3,5-bis(trifluoromethyl)phenyl)methyl((2-methyl-2h-tetrazol-5-yl)amino)-2,3,4,5-tetrahydro-7,9-dimethyl-1h-1-benzazepin-1-yl)methyl)-, trans-
evacetrapib [mi]
cyclohexanecarboxylic acid, 4-(((5s)-5-(((3,5-bis(trifluoromethyl)phenyl)methyl)(2-methyl-2h-tetrazol-5-yl)amino)-2,3,4,5-tetrahydro-7,9-dimethyl-1h-1-benzazepin-1-yl)methyl)-, trans-
evacetrapib [usan]
evacetrapib [who-dd]
(1r,4r)-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-1-benzazepin-1-yl)methyl)cyclohexane-1-carboxylic acid
evacetrapib [inn]
S2925
SCHEMBL141340
SCHEMBL108602
SCHEMBL108367
trans-4-[[(5s)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2h-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1h-1-b enzazepin-1-yl]methyl]-cyclohexanecarboxylic acid
trans-4-[[(5s)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2h-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1h-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid
AKOS025290246
(1s,4r)-4-(((s)-5-((3,5-bis(trifluoromethyl)benzyl)(2-methyl-2h-tetrazol-5-yl)amino)-7,9-dimethyl-2,3,4,5-tetrahydro-1h-benzo[b]azepin-1-yl)methyl)cyclohexanecarboxylic acid
gtpl8401
4-[[(5s)-5-[[3,5-bis(trifluoromethyl)phenyl]methyl-(2-methyltetrazol-5-yl)amino]-7,9-dimethyl-2,3,4,5-tetrahydro-1-benzazepin-1-yl]methyl]cyclohexane-1-carboxylic acid
trans-(1s,4r)-4-(((s)-5-((3,5-bis(trifluoromethyl)benzyl)(2-methyl-2h-tetrazol-5-yl)amino)-7,9-dimethyl-2,3,4,5-tetrahydro-1h-benzo[b]azepin-1-yl)methyl)cyclohexanecarboxylic acid
AC-30238
J-690053
EX-A621
HMS3651J12
mfcd23105886
(1s,4r)-4-(((s)-5-((3,5-bis(trifluoromethyl)benzyl)(2-methyl-2h-tetrazol-5-yl)amino)-7,9-dimethyl-2,3,4,5-tetrahydro-1h-benzo[b]azepin-1-yl)methyl)cyclohexane-1-carboxylic acid
SW219342-1
DB11655
AKOS032947275
Q553129
4-trans-(((s)-5-((3,5-bis(trifluoromethyl)benzyl)(2-methyl-2h-tetrazol-5-yl)amino)-7,9-dimethyl-2,3,4,5-tetrahydro-1h-benzo[b]azepin-1-yl)methyl)cyclohexanecarboxylic acid
AS-35108
AMY12209
CCG-270310
ihiugivxarlyhp-syjkbglxsa-n
ihiugivxarlyhp-uxnjhfgpsa-n

Synonym

HY-13327

4-[[(5s)-5-[[3,5-bis(triluoromethyl)phenyl]methyl-(2-methyltetrazol-5-yl)amino]-7,9-dimethyl-2,3,4,5-tetrahydro-1-benzazepin-1-yl]methyl]cyclohexane-1-carboxylic acid

CHEBI:188637

evacetrapib ,

evacetrapib (usan)

D10121

1186486-62-3

bdbm50381415

evacetrapib (ly2484595)

ly 2484595

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

51xwv9k850 ,

unii-51xwv9k850

ly-2484595

ly2484595

cyclohexanecarboxylic acid, 4-(((5s)-5-(((3,5-bis(trifluoromethyl)phenyl)methyl)(2- methyl-2h-tetrazol-5-yl)amino)-2,3,4,5-tetrahydro-7,9-dimethyl-1h-1-benzazepin-1- yl)methyl)-, trans-

evacetrapib [usan:inn]

CHEMBL2017179

(1r,4r)-4-{[(5s)-5-({[3,5-

PB36744

bis(trifluoromethyl)phenyl]methyl}(2-methyl-2h-

tetrahydro-1h-1-benzazepin-1-yl]methyl}cyclohexane-1-

1,2,3,4-tetrazol-5-yl)amino)-7,9-dimethyl-2,3,4,5-

CS-0658

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

cyclohexanecarboxylic acid, 4-(((5s)-5-(((3,5-bis(trifluoromethyl)phenyl)methyl((2-methyl-2h-tetrazol-5-yl)amino)-2,3,4,5-tetrahydro-7,9-dimethyl-1h-1-benzazepin-1-yl)methyl)-, trans-

evacetrapib [mi]

cyclohexanecarboxylic acid, 4-(((5s)-5-(((3,5-bis(trifluoromethyl)phenyl)methyl)(2-methyl-2h-tetrazol-5-yl)amino)-2,3,4,5-tetrahydro-7,9-dimethyl-1h-1-benzazepin-1-yl)methyl)-, trans-

evacetrapib [usan]

evacetrapib [who-dd]

(1r,4r)-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-1-benzazepin-1-yl)methyl)cyclohexane-1-carboxylic acid

evacetrapib [inn]

S2925

SCHEMBL141340

SCHEMBL108602

SCHEMBL108367

trans-4-[[(5s)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2h-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1h-1-b enzazepin-1-yl]methyl]-cyclohexanecarboxylic acid

trans-4-[[(5s)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2h-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1h-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid

AKOS025290246

(1s,4r)-4-(((s)-5-((3,5-bis(trifluoromethyl)benzyl)(2-methyl-2h-tetrazol-5-yl)amino)-7,9-dimethyl-2,3,4,5-tetrahydro-1h-benzo[b]azepin-1-yl)methyl)cyclohexanecarboxylic acid

gtpl8401

4-[[(5s)-5-[[3,5-bis(trifluoromethyl)phenyl]methyl-(2-methyltetrazol-5-yl)amino]-7,9-dimethyl-2,3,4,5-tetrahydro-1-benzazepin-1-yl]methyl]cyclohexane-1-carboxylic acid

trans-(1s,4r)-4-(((s)-5-((3,5-bis(trifluoromethyl)benzyl)(2-methyl-2h-tetrazol-5-yl)amino)-7,9-dimethyl-2,3,4,5-tetrahydro-1h-benzo[b]azepin-1-yl)methyl)cyclohexanecarboxylic acid

AC-30238

J-690053

EX-A621

HMS3651J12

mfcd23105886

(1s,4r)-4-(((s)-5-((3,5-bis(trifluoromethyl)benzyl)(2-methyl-2h-tetrazol-5-yl)amino)-7,9-dimethyl-2,3,4,5-tetrahydro-1h-benzo[b]azepin-1-yl)methyl)cyclohexane-1-carboxylic acid

SW219342-1

DB11655

AKOS032947275

Q553129

4-trans-(((s)-5-((3,5-bis(trifluoromethyl)benzyl)(2-methyl-2h-tetrazol-5-yl)amino)-7,9-dimethyl-2,3,4,5-tetrahydro-1h-benzo[b]azepin-1-yl)methyl)cyclohexanecarboxylic acid

AS-35108

AMY12209

CCG-270310

ihiugivxarlyhp-syjkbglxsa-n

ihiugivxarlyhp-uxnjhfgpsa-n

Class	Description
benzazepine	A group of two-ring heterocyclic compounds consisting of a benzene ring fused to an azepine ring.

Class

Description

benzazepine

A group of two-ring heterocyclic compounds consisting of a benzene ring fused to an azepine ring.

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)
Cholesteryl ester transfer protein	Homo sapiens (human)	IC50	0.1100	AID1476688

Protein

Taxonomy

Measurement

Average (mM)

Bioassay(s)

Cholesteryl ester transfer protein

Homo sapiens (human)

IC50

0.1100

AID1476688

Bioassays (12)

Assay ID	Title	Year	Journal	Article
AID1347411	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7 ISSN: 1554-8937	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1783825	Inhibition of recombinant CETP (unknown origin) assessed as maximal inhibition of transfer of [3H]cholesteryl oleate or [3H]triolein between exogenous [3H]LDL in 95% human serum at 10 uM by liquid scintillation analysis	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 ISSN: 1520-4804	Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
AID1166825	Terminal elimination half life in healthy human administered as single oral dose	2014	Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21 ISSN: 1520-4804	Potent cholesteryl ester transfer protein inhibitors of reduced lipophilicity: 1,1'-spiro-substituted hexahydrofuroquinoline derivatives.
AID1783924	Terminal half life in DIO NFR-transgenic mouse liver at 30 mg/kg, po once daily for 14 days	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 ISSN: 1520-4804	Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
AID1783925	Terminal half life in DIO NFR-transgenic mouse adipose tissue at 30 mg/kg, po once daily for 14 days	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 ISSN: 1520-4804	Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
AID657499	Inhibition of CETP in human plasma assessed as reduction in fluorescent intensity by fluorescence analysis	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9 ISSN: 1464-3405	Design, synthesis and structure-activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors.
AID1500886	Octanol-water partition coefficient, log P of the compound at pH 7.4 by HPLC based shake flask method	2017	European journal of medicinal chemistry, Oct-20, Volume: 139ISSN: 1768-3254	Discovery of pentacyclic triterpene 3β-ester derivatives as a new class of cholesterol ester transfer protein inhibitors.
AID1783993	Increase in HDL-cholesterol in transgenic mouse at 100 mg/kg, po treated for 2 weeks relative to control	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 ISSN: 1520-4804	Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
AID1783923	Terminal half life in DIO NFR-transgenic mouse plasma at 30 mg/kg, po once daily for 14 days	2021	Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18 ISSN: 1520-4804	Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
AID1476690	1-Octanol-phosphate buffered saline partition coefficient, log D of compound at pH 7.6 by tandem mass spectrometry method	2017	Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20 ISSN: 1520-4804	Discovery of a Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma.
AID1187829	Ex vivo inhibition of human CETP overexpressed in po dosed double transgenic mouse harboring human apoA1 assessed as elevation of HDL-cholesterol level measured at 8 hrs post dose	2014	European journal of medicinal chemistry, Oct-06, Volume: 85ISSN: 1768-3254	Some molecular targets for antihyperlipidemic drug research.
AID1476688	Inhibition of CETP in human plasma measured every 30 mins for 120 mins by fluorescence method	2017	Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20 ISSN: 1520-4804	Discovery of a Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma.

Assay ID

Title

Year

Journal

Article

AID1347411

qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary

2020

ACS chemical biology, 07-17, Volume: 15, Issue:7
ISSN: 1554-8937

High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.

AID1783825

Inhibition of recombinant CETP (unknown origin) assessed as maximal inhibition of transfer of [3H]cholesteryl oleate or [3H]triolein between exogenous [3H]LDL in 95% human serum at 10 uM by liquid scintillation analysis

2021

Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
ISSN: 1520-4804

Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.

AID1166825

Terminal elimination half life in healthy human administered as single oral dose

2014

Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
ISSN: 1520-4804

Potent cholesteryl ester transfer protein inhibitors of reduced lipophilicity: 1,1'-spiro-substituted hexahydrofuroquinoline derivatives.

AID1783924

Terminal half life in DIO NFR-transgenic mouse liver at 30 mg/kg, po once daily for 14 days

2021

Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
ISSN: 1520-4804

Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.

AID1783925

Terminal half life in DIO NFR-transgenic mouse adipose tissue at 30 mg/kg, po once daily for 14 days

2021

Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
ISSN: 1520-4804

Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.

AID657499

Inhibition of CETP in human plasma assessed as reduction in fluorescent intensity by fluorescence analysis

2012

Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
ISSN: 1464-3405

Design, synthesis and structure-activity-relationship of 1,5-tetrahydronaphthyridines as CETP inhibitors.

AID1500886

Octanol-water partition coefficient, log P of the compound at pH 7.4 by HPLC based shake flask method

2017

European journal of medicinal chemistry, Oct-20, Volume: 139ISSN: 1768-3254

Discovery of pentacyclic triterpene 3β-ester derivatives as a new class of cholesterol ester transfer protein inhibitors.

AID1783993

Increase in HDL-cholesterol in transgenic mouse at 100 mg/kg, po treated for 2 weeks relative to control

2021

Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
ISSN: 1520-4804

Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.

AID1783923

Terminal half life in DIO NFR-transgenic mouse plasma at 30 mg/kg, po once daily for 14 days

2021

Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
ISSN: 1520-4804

Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.

AID1476690

1-Octanol-phosphate buffered saline partition coefficient, log D of compound at pH 7.6 by tandem mass spectrometry method

2017

Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
ISSN: 1520-4804

Discovery of a Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma.

AID1187829

Ex vivo inhibition of human CETP overexpressed in po dosed double transgenic mouse harboring human apoA1 assessed as elevation of HDL-cholesterol level measured at 8 hrs post dose

2014

European journal of medicinal chemistry, Oct-06, Volume: 85ISSN: 1768-3254

Some molecular targets for antihyperlipidemic drug research.

AID1476688

Inhibition of CETP in human plasma measured every 30 mins for 120 mins by fluorescence method

2017

Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
ISSN: 1520-4804

Discovery of a Novel Piperidine-Based Inhibitor of Cholesteryl Ester Transfer Protein (CETP) That Retains Activity in Hypertriglyceridemic Plasma.

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	63 (87.50)	24.3611
2020's	9 (12.50)	2.80

Timeframe

Studies, This Drug (%)

All Drugs %

pre-1990

0 (0.00)

18.7374

1990's

0 (0.00)

18.2507

2000's

0 (0.00)

29.6817

2010's

63 (87.50)

24.3611

2020's

9 (12.50)

2.80

Publication Type	This drug (%)	All Drugs (%)
Trials	20 (26.67%)	5.53%
Reviews	21 (28.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	34 (45.33%)	84.16%

Publication Type

This drug (%)

All Drugs (%)

Trials

20 (26.67%)

5.53%

Reviews

21 (28.00%)

6.00%

Case Studies

0 (0.00%)

4.05%

Observational

0 (0.00%)

0.25%

Other

34 (45.33%)

84.16%

Substance	Classes	Roles	Relationship Strength
sk&f 81297	benzazepine		low
sk&f 82958	benzazepine		low
sk&f 77434	benzazepine; catechols; tertiary amino compound	dopamine agonist	low
sk&f-38393	benzazepine; catechols; secondary amino compound		low
1h-3-benzazepin-7-ol, 8-bromo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-	benzazepine		low
epinastine	benzazepine; guanidines	anti-allergic agent; H1-receptor antagonist; histamine antagonist; ophthalmology drug	low
fenoldopam	benzazepine	alpha-adrenergic agonist; antihypertensive agent; dopamine agonist; dopaminergic antagonist; vasodilator agent	low
mirtazapine	benzazepine; tetracyclic antidepressant	alpha-adrenergic antagonist; anxiolytic drug; H1-receptor antagonist; histamine antagonist; oneirogen; serotonergic antagonist	low
7-chloro-3-methyl-1-phenyl-1,2,4,5-tetrahydro-3-benzazepin-8-ol	benzazepine; organochlorine compound; tertiary amino compound	dopaminergic antagonist	low
azapetine	benzazepine		low
fluperlapine	benzazepine		low
fenoldopam mesylate	benzazepine		low
zatebradine	benzazepine		low
ecopipam	benzazepine		low
sk&f 104078	benzazepine		low
sk&f 86466	benzazepine		low
nnc 112	benzazepine		low
ivabradine	aromatic ether; benzazepine; carbobicyclic compound; tertiary amino compound	cardiotonic drug	low
sk&f 83959	benzazepine; catechols; organochlorine compound; tertiary amino compound	dopamine agonist	low
conivaptan	benzazepine	aquaretic; vasopressin receptor antagonist	low
tolvaptan	benzazepine; benzenedicarboxamide	aquaretic; vasopressin receptor antagonist	low
sanguinine	benzazepine		low
lycoramine	benzazepine		low
7,8-dimethoxy-1,3-dihydro-3-benzazepin-2-one	benzazepine		low
5-Methyl-8-nitro-3-spirocyclohexyl-2,3,4,5-tetrahydro-1H-2-benzazepine	benzazepine		low
capsazepine	benzazepine; catechols; monochlorobenzenes; thioureas	capsaicin receptor antagonist	low
sch 23390	benzazepine		low
ru 42173	benzazepine		low
benazepril	benzazepine; dicarboxylic acid monoester; ethyl ester; lactam	EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; prodrug	low
benazeprilat	benzazepine; dicarboxylic acid; lactam	EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor	low
(5R)-9-bromo-5-phenyl-3-prop-2-enyl-1,2,4,5-tetrahydro-3-benzazepine-7,8-diol	benzazepine		low
demethylmirtazapine	benzazepine; tetracyclic antidepressant	alpha-adrenergic antagonist; anxiolytic drug; H1-receptor antagonist; histamine antagonist; human xenobiotic metabolite; serotonergic antagonist	low
lorcaserin	benzazepine; organochlorine compound	anti-obesity agent; appetite depressant	low
mln8054	benzazepine		low
mln 8237	benzazepine		low

Substance

Studies

Classes

Roles

First Year

Last Year

Average Age

Relationship Strength

Trials

pre-1990

1990's

2000's

2010's

post-2020

low

low

benzazepine;
catechols;
tertiary amino compound

dopamine agonist

low

sk&f-38393

benzazepine;
catechols;
secondary amino compound

low

1h-3-benzazepin-7-ol, 8-bromo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-

benzazepine

low

epinastine

benzazepine;
guanidines

anti-allergic agent;
H1-receptor antagonist;
histamine antagonist;
ophthalmology drug

low

fenoldopam

benzazepine

alpha-adrenergic agonist;
antihypertensive agent;
dopamine agonist;
dopaminergic antagonist;
vasodilator agent

low

mirtazapine

benzazepine;
tetracyclic antidepressant

alpha-adrenergic antagonist;
anxiolytic drug;
H1-receptor antagonist;
histamine antagonist;
oneirogen;
serotonergic antagonist

low

7-chloro-3-methyl-1-phenyl-1,2,4,5-tetrahydro-3-benzazepin-8-ol

benzazepine;
organochlorine compound;
tertiary amino compound

dopaminergic antagonist

low

low

low

low

low

low

low

low

low

aromatic ether;
benzazepine;
carbobicyclic compound;
tertiary amino compound

cardiotonic drug

low

sk&f 83959

benzazepine;
catechols;
organochlorine compound;
tertiary amino compound

dopamine agonist

low

conivaptan

benzazepine

aquaretic;
vasopressin receptor antagonist

low

tolvaptan

benzazepine;
benzenedicarboxamide

aquaretic;
vasopressin receptor antagonist

low

low

low

7,8-dimethoxy-1,3-dihydro-3-benzazepin-2-one

benzazepine

low

5-Methyl-8-nitro-3-spirocyclohexyl-2,3,4,5-tetrahydro-1H-2-benzazepine

benzazepine

low

capsazepine

benzazepine;
catechols;
monochlorobenzenes;
thioureas

capsaicin receptor antagonist

low

low

low

benzazepine;
dicarboxylic acid monoester;
ethyl ester;
lactam

EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
prodrug

low

benazeprilat

benzazepine;
dicarboxylic acid;
lactam

EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor

low

(5R)-9-bromo-5-phenyl-3-prop-2-enyl-1,2,4,5-tetrahydro-3-benzazepine-7,8-diol

benzazepine

low

demethylmirtazapine

benzazepine;
tetracyclic antidepressant

alpha-adrenergic antagonist;
anxiolytic drug;
H1-receptor antagonist;
histamine antagonist;
human xenobiotic metabolite;
serotonergic antagonist

low

lorcaserin

benzazepine;
organochlorine compound

anti-obesity agent;
appetite depressant

low

low

low

Substance	Studies	Classes	Roles	First Year	Last Year	Average Age	Relationship Strength	2010's	post-2020
oleanolic acid	1	hydroxy monocarboxylic acid; pentacyclic triterpenoid	plant metabolite	2017	2017	7.0	low	1	0
ursolic acid	1	hydroxy monocarboxylic acid; pentacyclic triterpenoid	geroprotector; plant metabolite	2017	2017	7.0	low	1	0
betulinic acid	1	hydroxy monocarboxylic acid; pentacyclic triterpenoid	anti-HIV agent; anti-inflammatory agent; antimalarial; antineoplastic agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; plant metabolite	2017	2017	7.0	low	1	0
oleanolic acid 3-acetate	1			2017	2017	7.0	low	1	0
torcetrapib	5	(trifluoromethyl)benzenes; carbamate ester; quinolines	anticholesteremic drug; CETP inhibitor	2012	2021	7.8	low	4	1
dalcetrapib	3	anilide		2012	2017	8.7	low	3	0
anacetrapib	5			2012	2021	7.8	low	4	1

Substance

Studies

Classes

Roles

First Year

Last Year

Average Age

Relationship Strength

Trials

pre-1990

1990's

2000's

2010's

post-2020

oleanolic acid

hydroxy monocarboxylic acid;
pentacyclic triterpenoid

plant metabolite

2017

7.0

low

ursolic acid

hydroxy monocarboxylic acid;
pentacyclic triterpenoid

geroprotector;
plant metabolite

2017

7.0

low

betulinic acid

hydroxy monocarboxylic acid;
pentacyclic triterpenoid

anti-HIV agent;
anti-inflammatory agent;
antimalarial;
antineoplastic agent;
EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor;
plant metabolite

2017

7.0

low

oleanolic acid 3-acetate

2017

7.0

low

torcetrapib

(trifluoromethyl)benzenes;
carbamate ester;
quinolines

anticholesteremic drug;
CETP inhibitor

2012

2021

7.8

low

dalcetrapib

anilide

2012

2017

8.7

low

anacetrapib

2012

2021

7.8

low

Substance	Studies	Classes	Roles	First Year	Last Year	Average Age	Relationship Strength	Trials	2010's	post-2020
adenine	1	6-aminopurines; purine nucleobase	Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite	2016	2016	8.0	low	0	1	0
niacin	3	pyridine alkaloid; pyridinemonocarboxylic acid; vitamin B3	antidote; antilipemic drug; EC 3.5.1.19 (nicotinamidase) inhibitor; Escherichia coli metabolite; human urinary metabolite; metabolite; mouse metabolite; plant metabolite; vasodilator agent	2011	2014	11.7	low	0	3	0
midazolam	1	imidazobenzodiazepine; monofluorobenzenes; organochlorine compound	anticonvulsant; antineoplastic agent; anxiolytic drug; apoptosis inducer; central nervous system depressant; GABAA receptor agonist; general anaesthetic; muscle relaxant; sedative	2015	2015	9.0	low	1	1	0
probucol	1	dithioketal; polyphenol	anti-inflammatory drug; anticholesteremic drug; antilipemic drug; antioxidant; cardiovascular drug	2018	2018	6.0	low	0	1	0
tolbutamide	1	N-sulfonylurea	human metabolite; hypoglycemic agent; insulin secretagogue; potassium channel blocker	2015	2015	9.0	low	1	1	0
aldosterone	2	11beta-hydroxy steroid; 18-oxo steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid hormone; mineralocorticoid; primary alpha-hydroxy ketone; steroid aldehyde	human metabolite; mouse metabolite	2011	2019	9.0	low	1	2	0
pyrroles	2	pyrrole; secondary amine		2011	2014	11.5	low	2	2	0
fluorobenzenes	1	monofluorobenzenes	NMR chemical shift reference compound	2011	2011	13.0	low	1	1	0
simvastatin	2	delta-lactone; fatty acid ester; hexahydronaphthalenes; statin (semi-synthetic)	EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor; EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor; ferroptosis inducer; geroprotector; prodrug	2011	2015	11.0	low	2	2	0
atorvastatin	6	aromatic amide; dihydroxy monocarboxylic acid; monofluorobenzenes; pyrroles; statin (synthetic)	environmental contaminant; xenobiotic	2011	2022	7.3	low	5	5	1
oxazolidin-2-one	24	carbamate ester; oxazolidinone	metabolite	2011	2021	9.2	medium	0	23	1
ezetimibe	3	azetidines; beta-lactam; organofluorine compound	anticholesteremic drug; antilipemic drug; antimetabolite	2013	2022	6.7	low	2	2	1
moxifloxacin	1	aromatic ether; cyclopropanes; fluoroquinolone antibiotic; pyrrolidinopiperidine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone	antibacterial drug	2014	2014	10.0	low	1	1	0
torcetrapib	15	(trifluoromethyl)benzenes; carbamate ester; quinolines	anticholesteremic drug; CETP inhibitor	2012	2021	8.9	medium	0	14	1
lignans	1			2018	2018	6.0	low	0	1	0
dalcetrapib	17	anilide		2011	2021	9.0	high	0	16	1
bms201038	2	(trifluoromethyl)benzenes; benzamides; fluorenes; piperidines	anticholesteremic drug; MTP inhibitor	2013	2014	10.5	low	0	2	0
etc-1002	1	alpha,omega-dicarboxylic acid	antilipemic drug; EC 2.3.3.8 (ATP citrate synthase) inhibitor; prodrug	2013	2013	11.0	low	0	1	0
ta-8995	2			2016	2017	7.5	high	0	2	0
anacetrapib	24			2011	2021	9.2	high	0	23	1
oligonucleotides	2			2013	2014	10.5	low	0	2	0
pci 32765	1	acrylamides; aromatic amine; aromatic ether; N-acylpiperidine; pyrazolopyrimidine; tertiary carboxamide	antineoplastic agent; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor	2016	2016	8.0	low	0	1	0
piperidines	1			2016	2016	8.0	low	0	1	0
leoligin	1			2018	2018	6.0	medium	0	1	0

Substance

Studies

Classes

Roles

First Year

Last Year

Average Age

Relationship Strength

Trials

pre-1990

1990's

2000's

2010's

post-2020

adenine

6-aminopurines;
purine nucleobase

Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite

2016

8.0

low

niacin

pyridine alkaloid;
pyridinemonocarboxylic acid;
vitamin B3

antidote;
antilipemic drug;
EC 3.5.1.19 (nicotinamidase) inhibitor;
Escherichia coli metabolite;
human urinary metabolite;
metabolite;
mouse metabolite;
plant metabolite;
vasodilator agent

2011

2014

11.7

low

midazolam

imidazobenzodiazepine;
monofluorobenzenes;
organochlorine compound

anticonvulsant;
antineoplastic agent;
anxiolytic drug;
apoptosis inducer;
central nervous system depressant;
GABAA receptor agonist;
general anaesthetic;
muscle relaxant;
sedative

2015

9.0

low

probucol

dithioketal;
polyphenol

anti-inflammatory drug;
anticholesteremic drug;
antilipemic drug;
antioxidant;
cardiovascular drug

2018

6.0

low

tolbutamide

N-sulfonylurea

human metabolite;
hypoglycemic agent;
insulin secretagogue;
potassium channel blocker

2015

9.0

low

aldosterone

11beta-hydroxy steroid;
18-oxo steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(4) steroid;
C21-steroid hormone;
mineralocorticoid;
primary alpha-hydroxy ketone;
steroid aldehyde

human metabolite;
mouse metabolite

2011

2019

9.0

low

pyrroles

pyrrole;
secondary amine

2011

2014

11.5

low

fluorobenzenes

monofluorobenzenes

NMR chemical shift reference compound

2011

13.0

low

simvastatin

delta-lactone;
fatty acid ester;
hexahydronaphthalenes;
statin (semi-synthetic)

EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor;
EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor;
ferroptosis inducer;
geroprotector;
prodrug

2011

2015

11.0

low

atorvastatin

aromatic amide;
dihydroxy monocarboxylic acid;
monofluorobenzenes;
pyrroles;
statin (synthetic)

environmental contaminant;
xenobiotic

2011

2022

7.3

low

oxazolidin-2-one

carbamate ester;
oxazolidinone

metabolite

2011

2021

9.2

medium

ezetimibe

azetidines;
beta-lactam;
organofluorine compound

anticholesteremic drug;
antilipemic drug;
antimetabolite

2013

2022

6.7

low

moxifloxacin

aromatic ether;
cyclopropanes;
fluoroquinolone antibiotic;
pyrrolidinopiperidine;
quinolinemonocarboxylic acid;
quinolone antibiotic;
quinolone

antibacterial drug

2014

10.0

low

torcetrapib

(trifluoromethyl)benzenes;
carbamate ester;
quinolines

anticholesteremic drug;
CETP inhibitor

2012

2021

8.9

medium

lignans

2018

6.0

low

dalcetrapib

anilide

2011

2021

9.0

high

bms201038

(trifluoromethyl)benzenes;
benzamides;
fluorenes;
piperidines

anticholesteremic drug;
MTP inhibitor

2013

2014

10.5

low

etc-1002

alpha,omega-dicarboxylic acid

antilipemic drug;
EC 2.3.3.8 (ATP citrate synthase) inhibitor;
prodrug

2013

11.0

low

ta-8995

2016

2017

7.5

high

anacetrapib

2011

2021

9.2

high

oligonucleotides

2013

2014

10.5

low

pci 32765

acrylamides;
aromatic amine;
aromatic ether;
N-acylpiperidine;
pyrazolopyrimidine;
tertiary carboxamide

antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor

2016

8.0

low

piperidines

2016

8.0

low

leoligin

2018

6.0

medium

Condition	Studies	First Year	Last Year	Average Age	Relationship Strength	Trials	2010's	post-2020
Acute Coronary Syndrome	1	2011	2011	13.0	low	0	1	0
Apolipoprotein B-100, Familial Defective	1	2014	2014	10.0	low	0	1	0
Arteriosclerosis, Coronary	2	2013	2015	10.0	low	1	2	0
Atherogenesis	5	2014	2019	8.0	low	1	5	0
Atherosclerosis	5	2014	2019	8.0	low	1	5	0
Atrioventricular Nodal Re-Entrant Tachycardia	1	2014	2014	10.0	low	1	1	0
Body Weight	2	2017	2017	7.0	low	0	2	0
Brain Vascular Disorders	1	2015	2015	9.0	low	1	1	0
Cardiac Diseases	1	2014	2014	10.0	low	0	1	0
Cardiovascular Diseases	19	2011	2021	7.3	medium	6	17	2
Cerebral Arteriosclerosis	1	2017	2017	7.0	low	1	1	0
Cerebrovascular Disorders	1	2015	2015	9.0	low	1	1	0
Colorectal Cancer	1	2022	2022	2.0	low	0	0	1
Colorectal Neoplasms	1	2022	2022	2.0	low	0	0	1
Complications of Diabetes Mellitus	1	2020	2020	4.0	low	1	1	0
Coronary Artery Disease	2	2013	2015	10.0	low	1	2	0
Coronary Disease	6	2011	2022	6.8	low	1	3	3
Coronary Heart Disease	6	2011	2022	6.8	low	1	3	3
Delayed Effects, Prenatal Exposure	2	2017	2017	7.0	low	0	2	0
Diabetes Mellitus	3	2017	2020	5.3	low	2	3	0
Disease Models, Animal	3	2015	2017	8.3	low	0	3	0
Diseases, Peripheral Vascular	2	2015	2017	8.0	low	2	2	0
Dyslipidemia	11	2011	2017	9.8	low	4	11	0
Dyslipidemias	11	2011	2017	9.8	low	4	11	0
Elevated Cholesterol	4	2011	2021	7.8	low	1	3	1
Genetic Predisposition	1	2017	2017	7.0	low	0	1	0
Heart Disease, Ischemic	1	2017	2017	7.0	low	1	1	0
Heart Diseases	1	2014	2014	10.0	low	0	1	0
Hypercholesterolemia	4	2011	2021	7.8	low	1	3	1
Hyperlipemia	1	2022	2022	2.0	low	1	0	1
Hyperlipidemias	1	2022	2022	2.0	low	1	0	1
Hyperlipoproteinemia	1	2014	2014	10.0	low	0	1	0
Hyperlipoproteinemia Type II	1	2014	2014	10.0	low	0	1	0
Hyperlipoproteinemias	1	2014	2014	10.0	low	0	1	0
Hypertriglyceridemia	1	2017	2017	7.0	low	0	1	0
Intracranial Arteriosclerosis	1	2017	2017	7.0	low	1	1	0
Kidney Diseases	1	2014	2014	10.0	low	0	1	0
Kidney Failure	1	2016	2016	8.0	low	1	1	0
Lipid Metabolism, Inborn Error	3	2014	2015	9.3	low	0	3	0
Liver Diseases	1	2016	2016	8.0	low	1	1	0
Liver Dysfunction	1	2016	2016	8.0	low	1	1	0
Myocardial Ischemia	1	2017	2017	7.0	low	1	1	0
Peripheral Vascular Diseases	2	2015	2017	8.0	low	2	2	0
Pregnancy	2	2017	2017	7.0	low	0	2	0
Renal Insufficiency	1	2016	2016	8.0	low	1	1	0
Tachycardia, Ventricular	1	2014	2014	10.0	low	1	1	0
Vascular Diseases	4	2018	2019	5.8	low	1	4	0

Condition

Indicated

Studies

First Year

Last Year

Average Age

Relationship Strength

Trials

pre-1990

1990's

2000's

2010's

post-2020

Acute Coronary Syndrome

2011

13.0

low

Apolipoprotein B-100, Familial Defective

2014

10.0

low

Arteriosclerosis, Coronary

2013

2015

10.0

low

Atherogenesis

2014

2019

8.0

low

Atherosclerosis

2014

2019

8.0

low

Atrioventricular Nodal Re-Entrant Tachycardia

2014

10.0

low

Body Weight

2017

7.0

low

Brain Vascular Disorders

2015

9.0

low

Cardiac Diseases

2014

10.0

low

Cardiovascular Diseases

2011

2021

7.3

medium

Cerebral Arteriosclerosis

2017

7.0

low

Cerebrovascular Disorders

2015

9.0

low

Colorectal Cancer

2022

2.0

low

Colorectal Neoplasms

2022

2.0

low

Complications of Diabetes Mellitus

2020

4.0

low

Coronary Artery Disease

2013

2015

10.0

low

Coronary Disease

2011

2022

6.8

low

Coronary Heart Disease

2011

2022

6.8

low

Delayed Effects, Prenatal Exposure

2017

7.0

low

Diabetes Mellitus

2017

2020

5.3

low

Disease Models, Animal

2015

2017

8.3

low

Diseases, Peripheral Vascular

2015

2017

8.0

low

Dyslipidemia

2011

2017

9.8

low

Dyslipidemias

2011

2017

9.8

low

Elevated Cholesterol

2011

2021

7.8

low

Genetic Predisposition

2017

7.0

low

Heart Disease, Ischemic

2017

7.0

low

Heart Diseases

2014

10.0

low

Hypercholesterolemia

2011

2021

7.8

low

Hyperlipemia

2022

2.0

low

Hyperlipidemias

2022

2.0

low

Hyperlipoproteinemia

2014

10.0

low

Hyperlipoproteinemia Type II

2014

10.0

low

Hyperlipoproteinemias

2014

10.0

low

Hypertriglyceridemia

2017

7.0

low

Intracranial Arteriosclerosis

2017

7.0

low

Kidney Diseases

2014

10.0

low

Kidney Failure

2016

8.0

low

Lipid Metabolism, Inborn Error

2014

2015

9.3

low

Liver Diseases

2016

8.0

low

Liver Dysfunction

2016

8.0

low

Myocardial Ischemia

2017

7.0

low

Peripheral Vascular Diseases

2015

2017

8.0

low

Pregnancy

2017

7.0

low

Renal Insufficiency

2016

8.0

low

Tachycardia, Ventricular

2014

10.0

low

Vascular Diseases

2018

2019

5.8

low

Safety and Efficacy of Evacetrapib in Patients with Inadequately-controlled Hypercholesterolemia and High Cardiovascular Risk; A meta-analysis of Randomized Placebo-controlled Trials.
Prostaglandins, leukotrienes, and essential fatty acids, , Volume: 168, 2021

Cholesteryl ester transfer protein (CETP) as a drug target for cardiovascular disease.
Nature communications, , 09-24, Volume: 12, Issue:1, 2021

Effect of C-Reactive Protein on Lipoprotein(a)-Associated Cardiovascular Risk in Optimally Treated Patients With High-Risk Vascular Disease: A Prespecified Secondary Analysis of the ACCELERATE Trial.
JAMA cardiology, , 10-01, Volume: 5, Issue:10, 2020

Genome-Wide Polygenic Score and Cardiovascular Outcomes With Evacetrapib in Patients With High-Risk Vascular Disease: A Nested Case-Control Study.
Circulation. Genomic and precision medicine, , Volume: 13, Issue:1, 2020

Effect of CETP inhibition with evacetrapib in patients with diabetes mellitus enrolled in the ACCELERATE trial.
BMJ open diabetes research & care, , Volume: 8, Issue:1, 2020

Plasma Aldosterone Levels Are Not Associated With Cardiovascular Events Among Patients With High-Risk Vascular Disease: Insights From the ACCELERATE Trial.
Journal of the American Heart Association, , 12-03, Volume: 8, Issue:23, 2019

Evacetrapib reduces preβ-1 HDL in patients with atherosclerotic cardiovascular disease or diabetes.
Atherosclerosis, , Volume: 285, 2019

Cholesteryl ester transfer protein: An enigmatic pharmacology - Antagonists and agonists.
Atherosclerosis, , Volume: 278, 2018

ADCY9 Genetic Variants and Cardiovascular Outcomes With Evacetrapib in Patients With High-Risk Vascular Disease: A Nested Case-Control Study.
JAMA cardiology, , 05-01, Volume: 3, Issue:5, 2018

Evacetrapib and Cardiovascular Outcomes in High-Risk Vascular Disease.
The New England journal of medicine, , 05-18, Volume: 376, Issue:20, 2017

No cardiovascular benefit with evacetrapib - is this the end of the road for the 'cetrapibs'?
Expert opinion on pharmacotherapy, , Volume: 18, Issue:14, 2017

Unending saga of fighting cholesterol: Evacetrapib is another fallen warrior.
Bratislavske lekarske listy, , Volume: 117, Issue:11, 2016

Is Cholesteryl Ester Transfer Protein Inhibition an Effective Strategy to Reduce Cardiovascular Risk? CETP Inhibition as a Strategy to Reduce Cardiovascular Risk: The Pro Case.
Circulation, , Aug-04, Volume: 132, Issue:5, 2015

Is Cholesteryl Ester Transfer Protein Inhibition an Effective Strategy to Reduce Cardiovascular Risk? CETP as a Target to Lower CVD Risk: Suspension of Disbelief?
Circulation, , Aug-04, Volume: 132, Issue:5, 2015

Update on the discovery and development of cholesteryl ester transfer protein inhibitors for reducing residual cardiovascular risk.
Journal of medicinal chemistry, , Jan-09, Volume: 57, Issue:1, 2014

The promise of cholesteryl ester transfer protein (CETP) inhibition in the treatment of cardiovascular disease.
Current pharmaceutical design, , Volume: 19, Issue:17, 2013

Evacetrapib.
Current cardiology reports, , Volume: 14, Issue:3, 2012

New focus on raising HDL "good" cholesterol. But the value of this is not entirely clear.
DukeMedicine healthnews, , Volume: 18, Issue:2, 2012

Effects of the CETP inhibitor evacetrapib administered as monotherapy or in combination with statins on HDL and LDL cholesterol: a randomized controlled trial.
JAMA, , Nov-16, Volume: 306, Issue:19, 2011

Article	Year
Safety and Efficacy of Evacetrapib in Patients with Inadequately-controlled Hypercholesterolemia and High Cardiovascular Risk; A meta-analysis of Randomized Placebo-controlled Trials. Prostaglandins, leukotrienes, and essential fatty acids, , Volume: 168	2021
Efficacy and Safety of the Cholesteryl Ester Transfer Protein Inhibitor Evacetrapib in Combination With Atorvastatin in Japanese Patients With Primary Hypercholesterolemia. Circulation journal : official journal of the Japanese Circulation Society, , 12-25, Volume: 82, Issue:1	2017
Efficacy and Safety of Cholesteryl Ester Transfer Protein Inhibitor Evacetrapib Administered as Monotherapy in Japanese Patients With Primary Hypercholesterolemia. Circulation journal : official journal of the Japanese Circulation Society, , Oct-25, Volume: 81, Issue:11	2017
Efficacy and Safety of Evacetrapib for Modifying Plasma Lipids: A Systematic Review and Meta-Analysis of Randomized Controlled Trials. Current pharmaceutical design, , Volume: 22, Issue:5	2016
Efficacy, safety, tolerability, and pharmacokinetic profile of evacetrapib administered as monotherapy or in combination with atorvastatin in Japanese patients with dyslipidemia. The American journal of cardiology, , Jun-15, Volume: 113, Issue:12	2014
Safety of CETP inhibition. Current opinion in lipidology, , Volume: 23, Issue:6	2012

Article

Year

2021

Efficacy and Safety of the Cholesteryl Ester Transfer Protein Inhibitor Evacetrapib in Combination With Atorvastatin in Japanese Patients With Primary Hypercholesterolemia.
Circulation journal : official journal of the Japanese Circulation Society, , 12-25, Volume: 82, Issue:1

2017

Efficacy and Safety of Cholesteryl Ester Transfer Protein Inhibitor Evacetrapib Administered as Monotherapy in Japanese Patients With Primary Hypercholesterolemia.
Circulation journal : official journal of the Japanese Circulation Society, , Oct-25, Volume: 81, Issue:11

2017

Efficacy and Safety of Evacetrapib for Modifying Plasma Lipids: A Systematic Review and Meta-Analysis of Randomized Controlled Trials.
Current pharmaceutical design, , Volume: 22, Issue:5

2016

Efficacy, safety, tolerability, and pharmacokinetic profile of evacetrapib administered as monotherapy or in combination with atorvastatin in Japanese patients with dyslipidemia.
The American journal of cardiology, , Jun-15, Volume: 113, Issue:12

2014

Safety of CETP inhibition.
Current opinion in lipidology, , Volume: 23, Issue:6

2012

Article	Year
Impact of Increased Gastric pH on the Pharmacokinetics of Evacetrapib in Healthy Subjects. Pharmacotherapy, , Volume: 36, Issue:7	2016
Effect of hepatic or renal impairment on the pharmacokinetics of evacetrapib. European journal of clinical pharmacology, , Volume: 72, Issue:5	2016
Assessment of the persistence of anacetrapib and evacetrapib concentrations using two pharmacokinetic modeling approaches. Journal of clinical pharmacology, , Volume: 55, Issue:7	2015
Efficacy, safety, tolerability, and pharmacokinetic profile of evacetrapib administered as monotherapy or in combination with atorvastatin in Japanese patients with dyslipidemia. The American journal of cardiology, , Jun-15, Volume: 113, Issue:12	2014

Article

Year

Impact of Increased Gastric pH on the Pharmacokinetics of Evacetrapib in Healthy Subjects.
Pharmacotherapy, , Volume: 36, Issue:7

2016

Effect of hepatic or renal impairment on the pharmacokinetics of evacetrapib.
European journal of clinical pharmacology, , Volume: 72, Issue:5

2016

Assessment of the persistence of anacetrapib and evacetrapib concentrations using two pharmacokinetic modeling approaches.
Journal of clinical pharmacology, , Volume: 55, Issue:7

2015

2014

Article	Year
Absolute bioavailability of evacetrapib in healthy subjects determined by simultaneous administration of oral evacetrapib and intravenous [(13) C8 ]-evacetrapib as a tracer. Journal of labelled compounds & radiopharmaceuticals, , 05-30, Volume: 59, Issue:6	2016

Article

Year

Absolute bioavailability of evacetrapib in healthy subjects determined by simultaneous administration of oral evacetrapib and intravenous [(13) C8 ]-evacetrapib as a tracer.
Journal of labelled compounds & radiopharmaceuticals, , 05-30, Volume: 59, Issue:6

2016

Article	Year
Calibration-Free Second Harmonic Generation (SHG) Image Analysis for Quantification of Trace Crystallinity Within Final Dosage Forms of Amorphous Solid Dispersions. Applied spectroscopy, , Volume: 72, Issue:11	2018
Fertility and Embryo-Fetal Development Assessment in Rats and Rabbits with Evacetrapib: A Cholesteryl Ester Transfer Protein Inhibitor. Birth defects research, , 04-17, Volume: 109, Issue:7	2017
CYP-mediated drug-drug interactions with evacetrapib, an investigational CETP inhibitor: in vitro prediction and clinical outcome. British journal of clinical pharmacology, , Volume: 80, Issue:6	2015
A Multidose Study to Examine the Effect of Food on Evacetrapib Exposure at Steady State. Journal of cardiovascular pharmacology and therapeutics, , Volume: 20, Issue:5	2015
Evacetrapib at a supratherapeutic steady state concentration does not prolong QT in a thorough QT/QTc study in healthy participants. Journal of cardiovascular pharmacology and therapeutics, , Volume: 19, Issue:3	2014
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 of lipid research, , Volume: 52, Issue:12	2011

Article

Year

Calibration-Free Second Harmonic Generation (SHG) Image Analysis for Quantification of Trace Crystallinity Within Final Dosage Forms of Amorphous Solid Dispersions.
Applied spectroscopy, , Volume: 72, Issue:11

2018

Fertility and Embryo-Fetal Development Assessment in Rats and Rabbits with Evacetrapib: A Cholesteryl Ester Transfer Protein Inhibitor.
Birth defects research, , 04-17, Volume: 109, Issue:7

2017

CYP-mediated drug-drug interactions with evacetrapib, an investigational CETP inhibitor: in vitro prediction and clinical outcome.
British journal of clinical pharmacology, , Volume: 80, Issue:6

2015

A Multidose Study to Examine the Effect of Food on Evacetrapib Exposure at Steady State.
Journal of cardiovascular pharmacology and therapeutics, , Volume: 20, Issue:5

2015

Evacetrapib at a supratherapeutic steady state concentration does not prolong QT in a thorough QT/QTc study in healthy participants.
Journal of cardiovascular pharmacology and therapeutics, , Volume: 19, Issue:3

2014

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 of lipid research, , Volume: 52, Issue:12

2011

Article	Year
Efficacy and Safety of the Cholesteryl Ester Transfer Protein Inhibitor Evacetrapib in Combination With Atorvastatin in Japanese Patients With Primary Hypercholesterolemia. Circulation journal : official journal of the Japanese Circulation Society, , 12-25, Volume: 82, Issue:1	2017
Evacetrapib alone or in combination with statins lowers lipoprotein(a) and total and small LDL particle concentrations in mildly hypercholesterolemic patients. Journal of clinical lipidology, , Volume: 10, Issue:3
CYP-mediated drug-drug interactions with evacetrapib, an investigational CETP inhibitor: in vitro prediction and clinical outcome. British journal of clinical pharmacology, , Volume: 80, Issue:6	2015
Efficacy, safety, tolerability, and pharmacokinetic profile of evacetrapib administered as monotherapy or in combination with atorvastatin in Japanese patients with dyslipidemia. The American journal of cardiology, , Jun-15, Volume: 113, Issue:12	2014
Effects of the CETP inhibitor evacetrapib administered as monotherapy or in combination with statins on HDL and LDL cholesterol: a randomized controlled trial. JAMA, , Nov-16, Volume: 306, Issue:19	2011

Article

Year

2017

Evacetrapib alone or in combination with statins lowers lipoprotein(a) and total and small LDL particle concentrations in mildly hypercholesterolemic patients.
Journal of clinical lipidology, , Volume: 10, Issue:3

CYP-mediated drug-drug interactions with evacetrapib, an investigational CETP inhibitor: in vitro prediction and clinical outcome.
British journal of clinical pharmacology, , Volume: 80, Issue:6

2015

2014

Effects of the CETP inhibitor evacetrapib administered as monotherapy or in combination with statins on HDL and LDL cholesterol: a randomized controlled trial.
JAMA, , Nov-16, Volume: 306, Issue:19

2011

evacetrapib

Description

Cross-References

Synonyms (59)

Drug Classes (1)

Protein Targets (1)

Inhibition Measurements

Bioassays (12)

Research

Studies (72)

Study Types

Safety/Toxicity (6)

Pharmacokinetics (4)

Bioavailability (1)

Dosage (6)

Interactions (5)

evacetrapib

Description

Cross-References

Synonyms (59)

Drug Classes (1)

Protein Targets (1)

Inhibition Measurements

Bioassays (12)

Research

Studies (72)

Study Types

Related Drugs (63)

Drugs in this Class (35)

Drugs Involved in Assays Together (7)

Drugs Researched Together (24)

Related Conditions (47)

Safety/Toxicity (6)

Pharmacokinetics (4)

Bioavailability (1)

Dosage (6)

Interactions (5)