Page last updated: 2024-12-06

etofibrate

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

Description

Etofibrate is a lipid-lowering drug that acts as a peroxisome proliferator-activated receptor alpha (PPARα) agonist. It is a fibric acid derivative that was originally developed for the treatment of hyperlipidemia, particularly high levels of triglycerides and cholesterol. Etofibrate's mechanism of action involves binding to and activating PPARα receptors in the liver. This activation leads to increased expression of genes involved in lipid metabolism, such as lipoprotein lipase and apolipoprotein A-I. These effects contribute to a reduction in triglyceride levels and an increase in high-density lipoprotein (HDL) cholesterol. Etofibrate was once widely used for hyperlipidemia, but its use has declined due to concerns about potential liver toxicity and other adverse effects. Research on etofibrate continues, with ongoing studies exploring its potential role in other conditions, such as diabetes and cancer. Etofibrate's mechanism of action and its effects on lipid metabolism make it a subject of ongoing research in various fields.'

etofibrate: analog of clofibrate with nicotinic acid substituted on the 2-carbon of the ethyl ester group; structure; RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID65777
CHEMBL ID358150
CHEBI ID135535
SCHEMBL ID3122
MeSH IDM0054708

Synonyms (48)

Synonym
31637-97-5
etofibrate (inn)
D07187
etofibrate [inn]
lipo-merz
etofibrato [inn-spanish]
einecs 250-743-1
etofibrate
etofibratum [inn-latin]
2-hydroxyethyl nicotinate 2-(p-chlorophenoxy)-2-methylpropionate (ester)
2-(p-chlorophenoxy)-2-methylpropionic acid 2-(nicotinoyloxy)ethyl ester
CHEBI:135535
CHEMBL358150
121GE005
2-[2-(4-chlorophenoxy)-2-methylpropanoyl]oxyethyl pyridine-3-carboxylate
FT-0660287
etofibratum
23tf67g79m ,
etofibrato
unii-23tf67g79m
ethofibrate
2-(2-(4-chlorophenoxy)-2-methylpropanoyloxy)ethyl nicotinate
AKOS025311314
MLS006010106
smr002529563
SCHEMBL3122
etofibrate [mart.]
etofibrate [who-dd]
etofibrate [mi]
2-((2-(4-chlorophenoxy)-2-methylpropanoyl)oxy)ethyl nicotinate
Q-201101
AC-23121
DB08983
etofibrate, analytical standard
DTXSID80185521
HMS3652N04
3-pyridinecarboxylic acid, 2-[2-(4-chlorophenoxy)-2-methyl-1-oxopropoxy]ethyl ester
CS-0017444
HY-A0127
SW219681-1
BCP07572
Q4116990
S4264
mfcd00865727
AS-16847
CCG-268206
T72280
E1359

Research Excerpts

Overview

Etofibrate (Lipo-Merz) is an orally-administered treatment for lipid disorders. It combines fibrate and nicotinic acid in a slow-release formulation.

ExcerptReferenceRelevance
"Etofibrate (Lipo-Merz) is an orally-administered treatment for lipid disorders that combines fibrate and nicotinic acid in a slow-release formulation."( [Efficacy and safety of etofibrate in patients with non-proliferative diabetic retinopathy].
Emmerich, KH; Erbler, H; Goldsteine, J; Görtelmeyer, R; Klindzane, M; Poritis, N; Stelmane, I, 2009
)
1.38
"Etofibrate is a hypolipemic drug belonging to the fibrate class. "( Etofibrate decreases factor VII and fibrinogen levels in patients with polymetabolic syndrome.
Chelstowski, K; Jastrzebska, M; Kopciewicz, J; Naruszewicz, M; Pieczul-Mróz, J; Torbus-Lisiecka, B, 1999
)
3.19
"Etofibrate is a hybrid drug which combines niacin with clofibrate. "( Etofibrate but not controlled-release niacin decreases LDL cholesterol and lipoprotein (a) in type IIb dyslipidemic subjects.
Coelho, OR; Mansur, AP; Maranhão, RC; Ramires, JA; Rodrigues-Sobrinho, CR; Sposito, AC, 2001
)
3.2
"Etofibrate (Lipo-Merz) is a newer antilipaemic agent that contains the nicotinic and clofibric acid moieties joined together through a diester link with ethylene glycol. "( Bioavailability studies of etofibrate in rhesus monkeys.
Chasseaud, LF; Schatton, W; Taylor, T; Waller, AR, 1985
)
2.01

Treatment

Etofibrate treatment decreased plasma cholesterol and triglyceride concentrations and increased the bile flow. Treatment led to a marked decrease in total cholesterol and LDL-cholesterol.

ExcerptReferenceRelevance
"Etofibrate treatment also produced significant improvements in total cholesterol, LDL-cholesterol and HDL-cholesterol in comparison to the placebo treatment group."( [Efficacy and safety of etofibrate in patients with non-proliferative diabetic retinopathy].
Emmerich, KH; Erbler, H; Goldsteine, J; Görtelmeyer, R; Klindzane, M; Poritis, N; Stelmane, I, 2009
)
1.38
"3. Etofibrate treatment decreased plasma cholesterol and triglyceride concentrations and increased the bile flow."( Effect of etofibrate on bile production in the normolipidemic rat.
Bocos, C; Castro, M; Herrera, E; Orozco, E; Quack, G, 1995
)
1.21
"Treatment with etofibrate led to a marked decrease in total cholesterol and LDL-cholesterol."( Etofibrate treatment alters low density lipoprotein susceptibility to lipid peroxidation.
Burkard, M; Huth, K; Quack, G; Richter, CM; Wülfroth, P, 1992
)
2.07

Toxicity

Etofibrate provides a safe and effective treatment for ocular pathology resulting from type 2 diabetes mellitus. Safety evaluations (adverse events, laboratory parameters) did not reveal any clinically significant adverse effects in comparison to placebo.

ExcerptReferenceRelevance
" Safety evaluations (adverse events, laboratory parameters) did not reveal any clinically significant adverse effects of etofibrate in comparison to placebo."( [Efficacy and safety of etofibrate in patients with non-proliferative diabetic retinopathy].
Emmerich, KH; Erbler, H; Goldsteine, J; Görtelmeyer, R; Klindzane, M; Poritis, N; Stelmane, I, 2009
)
0.87
"Etofibrate provides a safe and effective treatment for ocular pathology resulting from type 2 diabetes mellitus."( [Efficacy and safety of etofibrate in patients with non-proliferative diabetic retinopathy].
Emmerich, KH; Erbler, H; Goldsteine, J; Görtelmeyer, R; Klindzane, M; Poritis, N; Stelmane, I, 2009
)
2.1

Bioavailability

The relative bioavailability of 2-(p-chlorophenoxy)-2-methylpropionic acid [2-(nicotinyloxy)-ethyl]-ester (etofibrate) with respect to Lipo-Merz (600 mg) has been determined in 10 health volunteers.

ExcerptReferenceRelevance
" The bioavailability of these moieties in etofibrate was compared to that from equimolar amounts of these drugs administered alone to rhesus monkeys (clofibric acid 354 mg, nicotinic acid 203 mg)."( Bioavailability studies of etofibrate in rhesus monkeys.
Chasseaud, LF; Schatton, W; Taylor, T; Waller, AR, 1985
)
0.83
"The relative bioavailability of 2-(p-chlorophenoxy)-2-methylpropionic acid [2-(nicotinyloxy)-ethyl]-ester (etofibrate) from Lipo-Merz retard (500 mg) with respect to Lipo-Merz (600 mg) has been determined in 10 health volunteers in a crossover study."( Relative bioavailability of etofibrate. A comparison of an acute and a new sustained release formulation.
Hoppe, HJ; Johnson, KI; Schatton, W, 1984
)
0.77

Dosage Studied

ExcerptRelevanceReference
" Lipo-Merz retard was administered in a dosage of one capsule/day, the combination product in a dosage of one capsule three times daily."( [Therapy of lipoproteinemia. Comparison between Lipo-Merz retard and a commercial combination drug].
Steger, W, 1980
)
0.26
"In a randomised blind study with 404 patients 1 capsule Etofibrate per day (500 mg) in sustained release dosage form was tested in comparison to other lipid-lowering drugs."( [An alternative in the therapy of primary hyperlipemias: etofibrate in depot preparations].
Füsgen, I; Summa, JD, 1980
)
0.75
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
monocarboxylic acidAn oxoacid containing a single carboxy group.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Bioassays (39)

Assay IDTitleYearJournalArticle
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1774079Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 10 uM incubated for 1 week by absorbance method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1774076Inhibition of 8-anilinonaphthalene-l-sulfonic acid binding to TTR V3OM mutant (unknown origin) expressed in Escherichia coli at 400 uM incubated for 1 hr in presence of 75 uM ANS by fluorescence method (Rvb = 91 +/- 0.92%)2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1774078Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 4 uM incubated for 1 week by absorbance method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1774075Inhibition of 8-anilinonaphthalene-l-sulfonic acid binding to TTR V3OM mutant (unknown origin) expressed in Escherichia coli assessed as ANS saturation ratio at 400 uM incubated for 1 hr in presence of 7.5 uM ANS by fluorescence method (Rvb = 56 +/- 2.3%)2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (73)

TimeframeStudies, This Drug (%)All Drugs %
pre-199043 (58.90)18.7374
1990's20 (27.40)18.2507
2000's7 (9.59)29.6817
2010's2 (2.74)24.3611
2020's1 (1.37)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.43

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index21.43 (24.57)
Research Supply Index4.64 (2.92)
Research Growth Index4.43 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.43)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials22 (27.16%)5.53%
Reviews5 (6.17%)6.00%
Case Studies1 (1.23%)4.05%
Observational0 (0.00%)0.25%
Other53 (65.43%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]