Page last updated: 2024-12-05

fenspiride

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

Description

Fenspiride is a benzoylpiperidine derivative that was originally developed as an antitussive agent. It is believed to exert its antitussive effect by acting as a centrally acting antitussive, possibly by inhibiting the cough reflex at the level of the medulla oblongata. Fenspiride has also been shown to possess anti-inflammatory properties, likely due to its ability to inhibit the release of histamine and other inflammatory mediators. However, fenspiride has been associated with serious adverse effects, including hepatotoxicity, cardiac arrhythmias, and QT interval prolongation. Due to these safety concerns, fenspiride is no longer marketed in many countries, including the United States. However, it remains available in some parts of Europe and Asia. Recent research has explored the potential of fenspiride in the treatment of other conditions, such as asthma, chronic obstructive pulmonary disease (COPD), and inflammatory bowel disease. However, further studies are needed to determine the safety and efficacy of fenspiride in these settings.'

fenspiride: was heading 1975-94 (see under SPIRO COMPOUNDS 1975-90); use SPIRO COMPOUNDS to search FENSPIRIDE 1975-94; bronchodilator agent used in asthma [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3344
CHEMBL ID576127
CHEBI ID94558
SCHEMBL ID21016
MeSH IDM0225164

Synonyms (83)

Synonym
BRD-K26739552-003-05-5
KBIO1_000526
DIVK1C_000526
fenspiride
8-(2-phenylethyl)-1-oxa-3,8-diazaspiro[4.5]decan-2-one
5053-06-5
respiride
brn 0533332
fenspiride [inn]
fenspiridum [inn-latin]
1-oxa-3,8-diazaspiro(4,5)decan-2-one, 8-(2-phenylethyl)-
einecs 225-751-3
fenspirida [inn-spanish]
viarespan
SPECTRUM_001260
NCGC00015438-01
cas-1151830
lopac-f-6145
NCGC00016988-01
LOPAC0_000496
IDI1_000526
SPECTRUM5_001345
PRESTWICK3_000213
BSPBIO_003170
AB00053591
PRESTWICK2_000213
KBIOSS_001740
KBIOGR_000710
KBIO2_004308
KBIO2_001740
KBIO3_002390
KBIO2_006876
SPBIO_002146
PRESTWICK1_000213
NINDS_000526
SPBIO_001412
SPECTRUM3_001435
SPECTRUM4_000415
SPECTRUM2_001396
PRESTWICK0_000213
BSPBIO_000225
BPBIO1_000249
NCGC00162172-01
NCGC00015438-04
eurespal (tn)
fenspiride (inn)
D07949
CHEMBL576127
eurespal
FT-0650682
s983qc7hkm ,
unii-s983qc7hkm
fenspiridum
fenspirida
CCG-204587
NCGC00015438-03
NCGC00015438-02
AKOS013605285
fenspiride [who-dd]
8-phenethyl-1-oxa-3,8-diazaspiro(4.5)decan-2-one
fenspiride [mi]
SCHEMBL21016
8-phenethyl-1-oxa-3,8-diazaspiro[4.5]decan-2-one
FVNFBBAOMBJTST-UHFFFAOYSA-N
AC-25697
AB00053591_10
AB00053591_11
DTXSID4023048
mfcd00867054
DB08979
8-phenethyl-1-oxa-3,8-diaza-spiro[4.5]decan-2-one
CHEBI:94558
SBI-0050480.P003
BCP07882
Q518027
Z1266873958
SDCCGSBI-0050480.P004
NCGC00015438-13
SB37403
A913266
CS-0013596
EN300-2010427
HY-A0027A

Research Excerpts

Overview

Fenspiride is an anti-inflammatory drug that may have a role in inhibition of histamine receptor H1 and influence a production of archidonic acid metabolites. It is an effective drug for the treatment of moderate chronic obstructive bronchitis.

ExcerptReferenceRelevance
"Fenspiride is an antagonist of H1-histamine receptors that is used to treat acute and chronic respiratory tract infections and otitis media in children and adolescents."( Long-term administration of fenspiride has no negative impact on bone mineral density and bone turnover in young growing rats.
Bolanowski, M; Dziewiszek, W; Jędrzejuk, D; Kwiatkowska, J; Landwójtowicz, M; Matuszewska, A; Merwid-Ląd, A; Nowak, B; Szeląg, A; Szeląg, E; Zduniak, K, 2019
)
2.25
"Fenspiride is an anti-inflammatory drug that may have a role in inhibition of histamine receptor H1 and influence a production of archidonic acid metabolites."( [Fenspiride in patients with acute bronchitis].
Ochwat, A; Płusa, T, 2005
)
2.68
"Fenspiride is a nonsteroidal anti-inflammatory agent, which we have previously shown to have an in vivo antibronchoconstrictor action in guinea pigs. "( Antitussive and antibronchoconstriction actions of fenspiride in guinea-pigs.
Bee, D; Crambes, O; Howard, P; Laude, EA, 1995
)
1.99
"Fenspiride is a drug with potential benefits in the treatment of obstructive airways disease. "( Pre- and postjunctional inhibitory effects of fenspiride on guinea-pig bronchi.
Advenier, C; Crambes, O; Girard, V; Lundberg, JM; Malbezin, M; Malmström, RE; Naline, E, 1997
)
2
"Fenspiride is an antiinflammatory drug targeted for the respiratory tract. "( [Efficacy and tolerance of fenspiride in adult patients with acute respiratory tract infections].
Nawacka, D; Płusa, T, 1998
)
2.04
"Fenspiride is a non-steroidal antiinflammatory agent which has a variety of actions, including inhibition of neurogenic bronchoconstriction."( Effect of fenspiride, a non-steroidal antiinflammatory agent, on neurogenic mucus secretion in ferret trachea in vitro.
Khawaja, AM; Liu, YC; Rogers, DF, 1999
)
1.43
"Fenspiride is an effective drug for the treatment of moderate chronic obstructive bronchitis."( [Effectiveness of fenspiride in patients with chronic obstructive bronchitis].
Gracheva, EIu; Iusupova, RS; Lapik, SV; Medvedeva, IV; Shorokhova, TD; Solov'eva, OG, 2001
)
1.37

Effects

ExcerptReferenceRelevance
"Fenspiride has also been reported to produce a subjective improvement in cough in patients."( Antitussive and antibronchoconstriction actions of fenspiride in guinea-pigs.
Bee, D; Crambes, O; Howard, P; Laude, EA, 1995
)
1.26

Treatment

ExcerptReferenceRelevance
"Fenspiride treatment was assessed as relatively effective in terms of influence on exacerbations, and well tolerated during six month therapy."( [The effect of fenspiride on the number of exacerbations and the time of first exacerbation in patients with chronic bronchitis].
Bartmińiski, W; Chyczewska, E; Malinowski, J; Nowak, D; Pachocki, R; Pirozyński, M; Skucha, W; Słomiński, M, 2005
)
2.12

Pharmacokinetics

ExcerptReferenceRelevance
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35

Compound-Compound Interactions

ExcerptReferenceRelevance
"Assess the supplementary therapeutic benefit provided by fenspiride administered in combination with antibiotics in COPD patients presenting an episode of bronchial infection."( [Evaluation and symptomatic treatment of surinfectious exacerbations of COPD: preliminary study of antibiotic treatment combined with fenspiride (Pneumorel 80mg) versus placebo].
Benezet, O; Dansin, E; Lirsac, B; Nouvet, G; Stach, B; Voisin, C, 2000
)
0.76

Bioavailability

ExcerptReferenceRelevance
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
azaspiro compoundAn azaspiro compound is a spiro compound in which at least one of the cyclic components is a nitrogen heterocyle.
[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 (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATAD5 protein, partialHomo sapiens (human)Potency32.62940.004110.890331.5287AID493106
GLS proteinHomo sapiens (human)Potency35.48130.35487.935539.8107AID624146
thyroid stimulating hormone receptorHomo sapiens (human)Potency7.94330.001318.074339.8107AID926; AID938
arylsulfatase AHomo sapiens (human)Potency0.01201.069113.955137.9330AID720538
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency19.95260.035520.977089.1251AID504332
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency26.20000.00207.533739.8107AID891
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency14.00530.00106.000935.4813AID943; AID944
lamin isoform A-delta10Homo sapiens (human)Potency0.00350.891312.067628.1838AID1487
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency37.93300.060110.745337.9330AID485368
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (33)

Assay IDTitleYearJournalArticle
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID468443Inhibition of human FAAH at 1 uM2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): identification of phenmedipham and amperozide as FAAH inhibitors.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (59)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's9 (15.25)18.2507
2000's25 (42.37)29.6817
2010's19 (32.20)24.3611
2020's6 (10.17)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 36.44

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index36.44 (24.57)
Research Supply Index4.34 (2.92)
Research Growth Index4.74 (4.65)
Search Engine Demand Index48.73 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (36.44)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials13 (20.63%)5.53%
Reviews1 (1.59%)6.00%
Case Studies3 (4.76%)4.05%
Observational0 (0.00%)0.25%
Other46 (73.02%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]