Page last updated: 2024-12-10

femoxetine

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

Description

femoxetine: serotonin uptake inhibitor; RN given refers to (3R-trans)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3012003
CHEMBL ID94739
CHEBI ID135330
SCHEMBL ID49869
MeSH IDM0056311

Synonyms (28)

Synonym
CHEMBL94739 ,
fg-4963
nnc-20-4963
femoxetine
(3r,4s)-3-[(4-methoxyphenoxy)methyl]-1-methyl-4-phenyl-piperidine
(3r,4s)-3-(4-methoxy-phenoxymethyl)-1-methyl-4-phenyl-piperidine
femoxetinum [inn-latin]
femoxetina [inn-spanish]
femoxetine [inn]
piperidine, 3-((4-methoxyphenoxy)methyl)-1-methyl-4-phenyl-, (3r-trans)-
(+)-trans-3-((p-methoxyphenoxy)methyl)-1-methyl-4-phenylpiperidine
CHEBI:135330
(3r,4s)-3-[(4-methoxyphenoxy)methyl]-1-methyl-4-phenylpiperidine
bdbm50014247
3-(4-methoxy-phenoxymethyl)-1-methyl-4-phenyl-piperidine(femoxetine)
unii-8y719zlx8c
(+)-femoxetine
femoxetinum
59859-58-4
8y719zlx8c ,
femoxetina
femoxetine [who-dd]
femoxetine [mi]
femoxetine [mart.]
SCHEMBL49869
DTXSID70208576
fg4963
Q5442938

Research Excerpts

Actions

ExcerptReferenceRelevance
"Femoxetine tended to increase pupil diameter and amitriptyline to increase accommodation near point, but no visual disturbances were reported on any treatment."( Cardiovascular (ECG and systolic time intervals) and anticholinergic effects of repeated doses of femoxetine--a comparison with amitriptyline and placebo in healthy men.
Skrumsager, BK; Turner, P; Warrington, SJ, 1989
)
1.22

Pharmacokinetics

ExcerptReferenceRelevance
" The elimination half-life of femoxetine was within the normal limits in most of the patients."( Femoxetine clearance in patients with liver cirrhosis.
Hansen, BA; Keiding, S; Lund, J; Mengel, H, 1984
)
2

Bioavailability

ExcerptReferenceRelevance
" The tablet gave a longer lag time and a slower absorption rate than the solution."( Biovailability and pharmacokinetics of femoxetine.
Lange, J; Lund, J; Mengel, H, 1983
)
0.54

Dosage Studied

ExcerptRelevanceReference
" After 6 weeks of treatment with a daily dosage of 600 mg femoxetine or 150 mg amitriptyline, no statistically significant differences between the 2 treatment groups were observed, either when using the HDS or the clinical global assessment scale."( Femoxetine and amitriptyline in general practice: a randomized double-blind group comparison.
Jeppesen, K; Skrumsager, BK, 1986
)
1.96
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
piperidines
[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]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sodium-dependent noradrenaline transporterMus musculus (house mouse)Ki0.12000.01200.09050.2900AID134216
Sodium-dependent serotonin transporterMus musculus (house mouse)Ki0.00910.00040.59574.1000AID134217
Sodium-dependent dopamine transporterMus musculus (house mouse)Ki1.03500.40400.68731.0350AID134215
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (31)

Assay IDTitleYearJournalArticle
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]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID179747In vitro inhibition of serotonin (5-HT) uptake in crude rat brain synaptosomes1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Molecular structure of fluoxetine hydrochloride, a highly selective serotonin-uptake inhibitor.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
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]
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
AID179990Tested in vivo for serotonin syndrome antagonizing activity in rat1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Pyrroloisoquinoline antidepressants. 3. A focus on serotonin.
AID132107In vivo effect on Tetrabenazine motor activity in mice following i.p. administration.1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Pyrroloisoquinoline antidepressants. 3. A focus on serotonin.
AID134217Tested in vitro for serotonin(5-HT) neuronal uptake inhibition1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Pyrroloisoquinoline antidepressants. 3. A focus on serotonin.
AID206023Percent inhibition of EtBr efflux against Staphylococcus aureus 1199B at 50 concentration2004Bioorganic & medicinal chemistry letters, Jun-21, Volume: 14, Issue:12
Structural differences between paroxetine and femoxetine responsible for differential inhibition of Staphylococcus aureus efflux pumps.
AID132108In vivo effect on Tetrabenazine ptosis activity in mice following i.p. administration.1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Pyrroloisoquinoline antidepressants. 3. A focus on serotonin.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID229635Selectivity ratio measured as the ratio of IC50 of NE/IC50 of 5-HT1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Molecular structure of fluoxetine hydrochloride, a highly selective serotonin-uptake inhibitor.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID134215Tested in vitro for dopamine(DA) neuronal uptake inhibition1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Pyrroloisoquinoline antidepressants. 3. A focus on serotonin.
AID179744In vitro inhibition of norepinephrine (NE) uptake in crude rat brain synaptosomes1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Molecular structure of fluoxetine hydrochloride, a highly selective serotonin-uptake inhibitor.
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]
AID554098Inhibition of NorA in Staphylococcus aureus 1199B assessed as reduction in ethidium bromide efflux at 50 uM by fluorimetry after 5 mins2011Journal of medicinal chemistry, Jan-13, Volume: 54, Issue:1
Discovery of novel inhibitors of the NorA multidrug transporter of Staphylococcus aureus.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' 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]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID134216Tested in vitro for norepinephrine (NE) neuronal uptake inhibition1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Pyrroloisoquinoline antidepressants. 3. A focus on serotonin.
AID132117Tested in vivo for head twitches antagonizing activity in mice1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
Pyrroloisoquinoline antidepressants. 3. A focus on serotonin.
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]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (54)

TimeframeStudies, This Drug (%)All Drugs %
pre-199042 (77.78)18.7374
1990's5 (9.26)18.2507
2000's6 (11.11)29.6817
2010's1 (1.85)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 23.12

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 Index23.12 (24.57)
Research Supply Index4.25 (2.92)
Research Growth Index4.03 (4.65)
Search Engine Demand Index26.67 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.12)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials13 (23.21%)5.53%
Reviews1 (1.79%)6.00%
Case Studies1 (1.79%)4.05%
Observational0 (0.00%)0.25%
Other41 (73.21%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]