Page last updated: 2024-12-11

tiacrilast

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

Description

tiacrilast: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6435375
CHEMBL ID337379
SCHEMBL ID635456
SCHEMBL ID635455
MeSH IDM0119957

Synonyms (27)

Synonym
ro-22-3747/000
tiacrilast
ro-22-3747
2-propenoic acid, 3-(6-(methylthio)-4-oxo-3(4h)-quinazolinyl)-, (e)-
tiacrilastum [inn-latin]
brn 5752117
(e)-3-(6-(methylthio)-4-oxo-3(4h)-quinazolinyl)-2-propenoic acid
tiacrilast [usan:inn]
ro 22-3747
(e)-6-(methylthio)-4-oxo-3(4h)-quinazolineacrylic acid
78299-53-3
tiacrilast (usan/inn)
D06123
ro 22-3747/000
CHEMBL337379
(e)-3-(6-methylsulfanyl-4-oxoquinazolin-3-yl)prop-2-enoic acid
74l3dxn051 ,
unii-74l3dxn051
tiacrilastum
SCHEMBL635456
SCHEMBL635455
tiacrilast [usan]
tiacrilast [mart.]
tiacrilast [inn]
Q27266294
DTXSID801167245
(2e)-3-[6-(methylthio)-4-oxo-3(4h)-quinazolinyl]-2-propenoic acid

Research Excerpts

Overview

Tiacrilast (Ro 22-3747) is an allergic mediator release inhibitor. It has demonstrated potent oral activity in two IgE-mediated animal models of immediate hypersensitivity.

ExcerptReferenceRelevance
"Tiacrilast is a potent mast cell degranulation inhibitor in vitro and in animal studies. "( Topical tiacrilast, a potent mast cell degranulation inhibitor, does not improve adult atopic eczema.
Baudin, M; Braun-Falco, O; Brechtel, B; Christophers, E; Czarnetzki, BM; Dupuy, P; Reckers-Czaschka, R; Schöpf, E, 1993
)
2.16
"Tiacrilast (Ro 22-3747) is an allergic mediator release inhibitor which has demonstrated potent oral activity in two IgE-mediated animal models of immediate hypersensitivity: the rat passive cutaneous anaphylaxis test (ID50 of 0.65 mg/kg) and a model in which anaphylactic bronchospasm is induced in passively sensitized rats (ID50 of 0.022 mg/kg). "( The pharmacological profile and initial clinical evaluation of tiacrilast (Ro 22-3747): a new antiallergic agent.
Dunton, AW; McGhee, B; Welton, AF, 1986
)
1.95

Pharmacokinetics

ExcerptReferenceRelevance
" Plasma concentrations and pharmacokinetic parameters were nearly proportional to dose over the 150 to 750 mg dose range studied."( Pharmacokinetics of single and multiple ascending doses of the antiallergic agent tiacrilast in man.
Dunton, A; Keigher, N; Massarella, JW; Pao, J; Silvestri, TM, 1987
)
0.5

Bioavailability

ExcerptReferenceRelevance
" Moreover, there was no evidence of unexpected accumulation of the drug in the plasma during multiple dosing and food did not appear to alter the bioavailability of tiacrilast to any clinically significant extent."( Pharmacokinetics of single and multiple ascending doses of the antiallergic agent tiacrilast in man.
Dunton, A; Keigher, N; Massarella, JW; Pao, J; Silvestri, TM, 1987
)
0.69

Dosage Studied

ExcerptRelevanceReference
" Plasma samples were obtained at specified times after the initial dose, after 4 days of multiple dosing and after the last dose of tiacrilast."( Pharmacokinetics of single and multiple ascending doses of the antiallergic agent tiacrilast in man.
Dunton, A; Keigher, N; Massarella, JW; Pao, J; Silvestri, TM, 1987
)
0.7
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (7)

Assay IDTitleYearJournalArticle
AID592681Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID455986Permeability across human Caco-2 cells2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain.
AID183130Inhibitory dose administered perorally against anaphylactic bronchospasm in passively sensitized rats1983Journal of medicinal chemistry, Mar, Volume: 26, Issue:3
(E)-3-(4-Oxo-4H-quinazolin-3-yl)-2-propenoic acids, a new series of antiallergy agents.
AID1223490Apparent permeability across human differentiated Caco2 cells2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study.
AID186613Tested for antiallergy activity in rat passive cutaneous anaphylaxis (PCA) test at 32 mg/kg administered perorally1983Journal of medicinal chemistry, Mar, Volume: 26, Issue:3
(E)-3-(4-Oxo-4H-quinazolin-3-yl)-2-propenoic acids, a new series of antiallergy agents.
AID12234881-Octanol-water distribution coefficient, log D of the compound at pH 7.42012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study.
AID186612Anti-allergy activity test in rat passive cutaneous anaphylaxis (PCA) test at 16 mg/kg administered intraperitoneally1983Journal of medicinal chemistry, Mar, Volume: 26, Issue:3
(E)-3-(4-Oxo-4H-quinazolin-3-yl)-2-propenoic acids, a new series of antiallergy agents.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (41.67)18.7374
1990's4 (33.33)18.2507
2000's1 (8.33)29.6817
2010's2 (16.67)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: 93.41

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

MetricThis Compound (vs All)
Research Demand Index93.41 (24.57)
Research Supply Index2.77 (2.92)
Research Growth Index4.60 (4.65)
Search Engine Demand Index163.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (93.41)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (25.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other9 (75.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]