Page last updated: 2024-11-11

eflucimibe

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

eflucimibe: a powerful and systemic acylcoenzyme A: cholesterol acyltransferase inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9804740
CHEMBL ID1908306
SCHEMBL ID668292
MeSH IDM0376294

Synonyms (18)

Synonym
eflucimibe
202340-45-2
(s)-2',3',5'-trimethyl-4'-hydroxy-alpha-dodecylthioacetanilide
(s)-2-(dodecylthio)-4'-hydroxy-2',3',5'-trimethyl-2-phenylacetanilide
3dk1x2c37m ,
unii-3dk1x2c37m
eflucimibe [inn]
f-12511
CHEMBL1908306
(s)-2',3',5'-trimethyl-4'-hydroxy-.alpha.-dodecylthioacetanilide
SCHEMBL668292
bdbm182848
us9149492, eflucimibe (f12511)
DTXSID70174085
(2s)-2-dodecylsulfanyl-n-(4-hydroxy-2,3,5-trimethylphenyl)-2-phenylacetamide
Q27257077
(s)-2-(dodecylthio)-n-(4-hydroxy-2,3,5-trimethylphenyl)-2-phenylacetamide
AKOS040748308

Research Excerpts

Overview

Eflucimibe is an acyl coenzyme A:cholesterol acyltransferase inhibitor under development by Pierre Fabre SA and Eli Lilly & Co. It is being developed for the potential treatment of hypercholesterolemia and atherosclerosis.

ExcerptReferenceRelevance
"Eflucimibe is an acyl coenzyme A:cholesterol acyltransferase inhibitor under development by Pierre Fabre SA and Eli Lilly & Co for the potential treatment of hypercholesterolemia and atherosclerosis. "( Eflucimibe. Pierre Fabre/Eli Lilly.
Burnett, JR, 2003
)
3.2

Bioavailability

ExcerptReferenceRelevance
"The importance, in therapeutics, of the concept of bioavailability and on-going quality research in the formulation of a drug has prompted us to examine the crystalline polymorphism of eflucimibe as from the research phase."( [Crystalline polymorphism of eflucimibe].
Autin, JM; Autret, JM; Basquin, M; Chauvet, A; Patoiseau, JF; Pena, R; Ribet, JP; Segonds, R, 2002
)
0.8
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sterol O-acyltransferase 2Homo sapiens (human)IC50 (µMol)0.11000.11003.20369.2000AID1342239
Sterol O-acyltransferase 1Homo sapiens (human)IC50 (µMol)0.03900.02501.79758.0000AID1342238
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (9)

Processvia Protein(s)Taxonomy
cholesterol metabolic processSterol O-acyltransferase 2Homo sapiens (human)
macrophage derived foam cell differentiationSterol O-acyltransferase 2Homo sapiens (human)
cholesterol storageSterol O-acyltransferase 2Homo sapiens (human)
intestinal cholesterol absorptionSterol O-acyltransferase 2Homo sapiens (human)
cholesterol effluxSterol O-acyltransferase 2Homo sapiens (human)
very-low-density lipoprotein particle assemblySterol O-acyltransferase 2Homo sapiens (human)
low-density lipoprotein particle clearanceSterol O-acyltransferase 2Homo sapiens (human)
cholesterol homeostasisSterol O-acyltransferase 2Homo sapiens (human)
cholesterol metabolic processSterol O-acyltransferase 1Homo sapiens (human)
cholesterol metabolic processSterol O-acyltransferase 1Homo sapiens (human)
macrophage derived foam cell differentiationSterol O-acyltransferase 1Homo sapiens (human)
cholesterol storageSterol O-acyltransferase 1Homo sapiens (human)
cholesterol effluxSterol O-acyltransferase 1Homo sapiens (human)
very-low-density lipoprotein particle assemblySterol O-acyltransferase 1Homo sapiens (human)
low-density lipoprotein particle clearanceSterol O-acyltransferase 1Homo sapiens (human)
cholesterol homeostasisSterol O-acyltransferase 1Homo sapiens (human)
positive regulation of amyloid precursor protein biosynthetic processSterol O-acyltransferase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
fatty-acyl-CoA bindingSterol O-acyltransferase 2Homo sapiens (human)
sterol O-acyltransferase activitySterol O-acyltransferase 2Homo sapiens (human)
protein bindingSterol O-acyltransferase 2Homo sapiens (human)
cholesterol bindingSterol O-acyltransferase 2Homo sapiens (human)
acyltransferase activitySterol O-acyltransferase 2Homo sapiens (human)
cholesterol O-acyltransferase activitySterol O-acyltransferase 2Homo sapiens (human)
fatty-acyl-CoA bindingSterol O-acyltransferase 1Homo sapiens (human)
sterol O-acyltransferase activitySterol O-acyltransferase 1Homo sapiens (human)
protein bindingSterol O-acyltransferase 1Homo sapiens (human)
cholesterol bindingSterol O-acyltransferase 1Homo sapiens (human)
cholesterol O-acyltransferase activitySterol O-acyltransferase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
endoplasmic reticulumSterol O-acyltransferase 2Homo sapiens (human)
endoplasmic reticulum membraneSterol O-acyltransferase 2Homo sapiens (human)
brush borderSterol O-acyltransferase 2Homo sapiens (human)
endoplasmic reticulum membraneSterol O-acyltransferase 2Homo sapiens (human)
endoplasmic reticulumSterol O-acyltransferase 1Homo sapiens (human)
endoplasmic reticulum membraneSterol O-acyltransferase 1Homo sapiens (human)
membraneSterol O-acyltransferase 1Homo sapiens (human)
endoplasmic reticulum membraneSterol O-acyltransferase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (3)

Assay IDTitleYearJournalArticle
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (18)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's14 (77.78)29.6817
2010's2 (11.11)24.3611
2020's2 (11.11)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (11.11%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other16 (88.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]