ANACETRAPIB

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C30H25F10NO3
Molecular Weight	637.5084
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC1=C(C=C(C(C)C)C(F)=C1)C2=C(CN3[C@@H](C)[C@H](OC3=O)C4=CC(=CC(=C4)C(F)(F)F)C(F)(F)F)C=C(C=C2)C(F)(F)F

InChI

InChIKey=MZZLGJHLQGUVPN-HAWMADMCSA-N

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/s1

HIDE SMILES / InChI

Molecular Formula	C30H25F10NO3
Molecular Weight	637.5084
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	2 / 2
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.cadth.ca/media/pdf/EH0007-000_Anacetrapib_draft_e.pdf
Curator's Comment: Description was created based on several sources, including http://www.selleckchem.com/products/anacetrapib-mk-0859.html

Anacetrapib is a CETP inhibitor being developed by Merck to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease. Anacetrapib is a cholesterol ester transfer protein (CETP) inhibitor that blocks the transfer of cholesterol from highdensity lipoprotein to other lipoproteins. This results in an increase in high-density lipoprotein cholesterol (HDL-C) and a decrease in lowdensity lipoprotein cholesterol (LDL-C), which may reduce the development of atherosclerosis. Anacetrapib has not been approved for sale in Canada or the United States. Clinical evidence to support the use of anacetrapib for dyslipidemia has been reported in two clinical trials. REVEAL is an ongoing, large-scale phase 3 trial evaluating the effectiveness of anacetrapib with a statin for the secondary prevention of major coronary events in patients who have a history of cardiovascular disease. Results are anticipated in January 2017.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Cholesteryl ester transfer protein 15 Target ID: CHEMBL3572 Sources: https://www.cadth.ca/media/pdf/EH0007-000_Anacetrapib_draft_e.pdf https://www.ncbi.nlm.nih.gov/pubmed/20861162	Inhibitor 8504		17.2 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypercholesterolemia 51 Sources: https://clinicaltrials.gov/ct2/show/NCT01252953	Primary		Phase III 665	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
5064 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
3959 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
1498 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	125 mg single, oral dose: 125 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
2421 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
972 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
561 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	125 mg single, oral dose: 125 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: LOW-FAT
788 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
860 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
168 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	125 mg single, oral dose: 125 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
731 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	125 mg single, oral dose: 125 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
414 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
246 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
145 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
56 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
24 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9140 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
889 nM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3.45 μM EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23958252	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
82 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
44 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
23.9 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	125 mg single, oral dose: 125 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
34.2 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
10.7 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
9 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	125 mg single, oral dose: 125 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: LOW-FAT
15.7 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
14 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	125 mg single, oral dose: 125 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9.9 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	125 mg single, oral dose: 125 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.3 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.9 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.68 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.26 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
117.4 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
13.6 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
34.95 μM × h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/23958252	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
61.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
50.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
54.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	125 mg single, oral dose: 125 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
62 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
42.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
50.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	125 mg single, oral dose: 125 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: LOW-FAT
60 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
44.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	250 mg single, oral dose: 250 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
55.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	125 mg single, oral dose: 125 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
46.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	125 mg single, oral dose: 125 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
34.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
28.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
28.88 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
21 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
82.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
61.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19843057	1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered:	ANACETRAPIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

Doses

Dose	Population	Adverse events
1000 mg single, oral Highest studied dose Dose: 1000 mg Route: oral Route: single Dose: 1000 mg Sources: https://pubmed.ncbi.nlm.nih.gov/19843057	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/19843057	Sources: https://pubmed.ncbi.nlm.nih.gov/19843057
300 mg 1 times / day multiple, oral Studied dose Dose: 300 mg, 1 times / day Route: oral Route: multiple Dose: 300 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/23958252	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/23958252	Sources: https://pubmed.ncbi.nlm.nih.gov/23958252

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY10537	https://www.001chemical.com/chem/search?q=DY10537
1PlusChem LLC	1P0039O1	https://www.1pchem.com/search?query=1P0039O1
A2B Chem	AB51697	http://a2bchem.com/prod/AB51697
AA Blocks	AA00394L	http://aablocks.com/goods/Goods/detail?id=AA00394L
AChemBlock	C-3348	http://www.achemblock.com/catalogsearch/result/?q=C-3348
AK Scientific	Y0279	https://aksci.com/item_detail.php?cat=Y0279
Alfa Chemistry	33894	http://www.alfa-chemistry.com/search.aspx?q=33894
Alfa Chemistry	ACM1061715909	http://www.alfa-chemistry.com/search.aspx?q=ACM1061715909
Ambeed	A293882	http://www.ambeed.com/search/Search.html?keyword=A293882
Angene	AGN-PC-0VENDU	http://www.angenechemical.com/productshow/AGN-PC-0VENDU.html
AOBIOUS INC	AOB87304	http://aobious.com/aobious/search?search_query=AOB87304
ApexBio Technology	A4375	https://www.apexbt.com/catalogsearch/result/?q=A4375
AstaTech	41214	http://astatechinc.com/CPSResult.php?CRNO=41214
BioSynth	J-501484	https://www.biosynth.com/en/products/life-science/other-biochemicals/products/J-501484
BOC Sciences	875446-37-0	http://www.bocsci.com/description.asp?cas=875446-37-0
BoronPharm	BP22252	https://www.boronpharm.com/boron/search.do?q=BP22252
Capot Chemical	29380	https://www.capotchem.com/search.do?q=29380
Cayman Chemical	21558	http://www.caymanchem.com/app/template/Product.vm/catalog/21558
ChemShuttle	104914	https://www.chemshuttle.com/catalogsearch/result/?q=104914
Combi-Blocks	QE-9719	http://www.combi-blocks.com/cgi-bin/find.cgi?QE-9719
Coresyn	CM14263	http://www.coresyn.com/search.do?q=CM14263
eMolecules	108761774	https://orderbb.emolecules.com/search/#?query=108761774
eMolecules	300515794	https://orderbb.emolecules.com/search/#?query=300515794
eMolecules	36096531	https://orderbb.emolecules.com/search/#?query=36096531
eNovation Chemicals	D496738	https://www.enovationchem.com/Products.asp?SEARCHTEXT=D496738&searchbtn.x=0&searchbtn.y=0
Excenen	EX-A420	http://www.excenen.com/searchresultlist.php?id=EX-A420
Hairui	ANSA064	http://www.hairuichem.com/en/product/search.do?q=ANSA064
KeyOrganics	AS-19552	http://www.keyorganicsinc.com/bionet/catalogsearch/result?q=AS-19552
Lab Seeker	SC-50566	http://www.labseeker.com/search.php?keywords=SC-50566&category=0
LabSeeker	SC-50566	http://www.labseeker.com/search.php?keywords=SC-50566&category=0
Matrix Scientific	112674	http://www.matrixscientific.com/112674.html
mcule	MCULE-4574141932	https://mcule.com/MCULE-4574141932/
mcule	MCULE-7871861095	https://mcule.com/MCULE-7871861095/
MedChem Express	HY-12090	https://www.medchemexpress.com/search.html?q=HY-12090&ft=&fa=&fp=
Molcore	MC10537	http://www.molcore.com/CatMC10537.html
Molnova	M16362	https://www.molnova.com/en/serch-list.html?keywords=M16362
MolPort	MolPort-021-804-915	https://www.molport.com/shop/molecule-link/MolPort-021-804-915
MuseChem	R052759	https://www.musechem.com/product/R052759.html
Ryan Scientific	Pseudolaric_Acid_B	https://ryansci.com/products?q=Pseudolaric_Acid_B&list_q=&search_type=exact
ShangHai Biochempartner	BCP000329	http://www.biochempartner.com/search_BCP000329
ShangHai Biochempartner	BCP02374	http://www.biochempartner.com/search_BCP02374
Synovel	SN-0280	http://www.synovellab.com/?s=SN-0280&submit=Search
TargetMol	T1928	https://www.targetmol.com/search?keyword=T1928
Tetrahedron	TS87152	http://www.thsci.com/search.do?q=TS87152
Toronto Research Chemicals	A637200	https://www.trc-canada.com/product-detail/?CatNum=A637200

PubMed

Title	Date	PubMed
Anacetrapib lowers LDL by increasing ApoB clearance in mildly hypercholesterolemic subjects.	2015-06	25961461
Anacetrapib as lipid-modifying therapy in patients with heterozygous familial hypercholesterolaemia (REALIZE): a randomised, double-blind, placebo-controlled, phase 3 study.	2015-05-30	25743173
Cholesteryl ester transfer protein inhibition in cardiovascular risk management: ongoing trials will end the confusion.	2011-12	20645987
Biphenyl-substituted oxazolidinones as cholesteryl ester transfer protein inhibitors: modifications of the oxazolidinone ring leading to the discovery of anacetrapib.	2011-07-14	21682257
Treatment of dyslipidemia in patients with type 2 diabetes.	2010-12-20	21172030
Safety of anacetrapib in patients with or at high risk for coronary heart disease.	2010-12-16	21082868
Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport.	2010-12	20861162
Good news for 'good' cholesterol.	2010-11-18	21085143
Effects of fenofibrate on lipid profiles, cholesterol ester transfer activity, and in-stent intimal hyperplasia in patients after elective coronary stenting.	2010-10-25	20973966
Drug off-target effects predicted using structural analysis in the context of a metabolic network model.	2010-09-23	20957118
Biochemical characterization of cholesteryl ester transfer protein inhibitors.	2010-09	20458119
Emerging drugs for hyperlipidemia.	2010-09	20423271
Raising HDL cholesterol in women.	2010-08-09	21072287
Update on CETP inhibition.	2010-08-02	21122682
Dissociating HDL cholesterol from cardiovascular risk.	2010-07-31	20655104
High density lipoproteins-based therapies for cardiovascular disease.	2010-07	21187875
Cholesterol efflux potential and antiinflammatory properties of high-density lipoprotein after treatment with niacin or anacetrapib.	2010-07	20448206
[Recent advances in the research on HDL subfraction].	2010-06	20662273
Dalcetrapib: a review of Phase II data.	2010-06	20465364
High-density lipoprotein-mediated anti-atherosclerotic and endothelial-protective effects: a potential novel therapeutic target in cardiovascular disease.	2010-05	20196740
Gateways to clinical trials.	2010-04-13	20383346
Current status and future directions in lipid management: emphasizing low-density lipoproteins, high-density lipoproteins, and triglycerides as targets for therapy.	2010-03-03	20234782
Metabolism and excretion of anacetrapib, a novel inhibitor of the cholesteryl ester transfer protein, in humans.	2010-03	20016053
Pharmacokinetics, metabolism, and excretion of anacetrapib, a novel inhibitor of the cholesteryl ester transfer protein, in rats and rhesus monkeys.	2010-03	20016052
[HDL and CETP in atherogenesis].	2010-02	20082258
Cholesteryl ester transfer protein: at the heart of the action of lipid-modulating therapy with statins, fibrates, niacin, and cholesteryl ester transfer protein inhibitors.	2010-01	19825813
Anacetrapib.	2010	20653333
The pharmacology and off-target effects of some cholesterol ester transfer protein inhibitors.	2009-11-16	19895942
Triglycerides and HDL cholesterol: stars or second leads in diabetes?	2009-11	19875584
Single-dose pharmacokinetics and pharmacodynamics of anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects.	2009-10	19843057
Design of the DEFINE trial: determining the EFficacy and tolerability of CETP INhibition with AnacEtrapib.	2009-10	19781408
Anacetrapib, a cholesterol ester transfer protein (CETP) inhibitor for the treatment of atherosclerosis.	2009-09	19705341
Cholesteryl ester transfer protein inhibitors as high-density lipoprotein raising agents.	2009-09	19663630
Effect of cholesteryl ester transfer protein inhibitor on vitamin E transport should be studied.	2009-07	19540377
The end of the road for CETP inhibitors after torcetrapib?	2009-07	19522058
Assessment of a pharmacokinetic and pharmacodynamic interaction between simvastatin and anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects.	2009-05	19552746
Drug discovery using chemical systems biology: identification of the protein-ligand binding network to explain the side effects of CETP inhibitors.	2009-05	19436720
Gateways to clinical trials.	2009-04	19536362
High-density lipoprotein cholesterol: current perspective for clinicians.	2009-02-26	19240106
Efficacy and safety of the cholesteryl ester transfer protein inhibitor anacetrapib as monotherapy and coadministered with atorvastatin in dyslipidemic patients.	2009-02	19185645
Assessment of the CYP3A-mediated drug interaction potential of anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy volunteers.	2009-01	19004846
Multiple-dose pharmacodynamics and pharmacokinetics of anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects.	2008-12	18580870
JTT-705: is there still future for a CETP inhibitor after torcetrapib?	2008-10	18808319
Torcetrapib-induced blood pressure elevation is independent of CETP inhibition and is accompanied by increased circulating levels of aldosterone.	2008-08	18536749
The failure of torcetrapib: what have we learned?	2008-08	18536741
Treating high-density lipoprotein cholesterol: a return to inhibition of cholesteryl ester transfer protein?	2008-06	18489843
Anacetrapib: new hope for cholesteryl ester transfer protein inhibitors in the treatment of dyslipidemia.	2008-06	18431368
HDL metabolism and CETP inhibition.	2008-04-17	18414186
Cholesteryl ester transfer protein inhibition and HDL increase: has the dream ended?	2008-04	18363511
Gateways to clinical trials.	2008-03	18560631

Patents

Sample Use Guides

In Vivo Use Guide

tablet, 100mg daily

Route of Administration: Oral

In Vitro Use Guide

Anacetrapib (0.1 to 10 uM) dose-dependently inhibited pre-β-HDL formation in vitro in human plasma

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:26:16 GMT 2025` Edited by `admin` on `Mon Mar 31 18:26:16 GMT 2025`
Record UNII	P7T269PR6S
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

MK-0859

Preferred Name

English

ANACETRAPIB

Official Name

English

MK0859

Code

English

anacetrapib [INN]

Common Name

English

2-OXAZOLIDINONE, 5-(3,5-BIS(TRIFLUOROMETHYL)PHENYL)-3-((4'-FLUORO-2'-METHOXY-5'-(1-METHYLETHYL)-4-(TRIFLUOROMETHYL)(1,1'-BIPHENYL)-2-YL)METHYL)-4-METHYL-, (4S,5R)-

Common Name

English

ANACETRAPIB [USAN]

Common Name

English

(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

Common Name

English

ANACETRAPIB [MART.]

Common Name

English

Anacetrapib [WHO-DD]

Common Name

English

ANACETRAPIB [JAN]

Common Name

English

ANACETRAPIB [MI]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C471