Page last updated: 2024-11-13

paquinimod

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

Cross-References

ID SourceID
PubMed CID54684617
CHEMBL ID67776
SCHEMBL ID1573633
MeSH IDM0575224

Synonyms (31)

Synonym
CHEMBL67776
abr-215757
paquinimod ,
hb76glg27v ,
248282-01-1
unii-hb76glg27v
paquinimod [inn]
n-ethyl-n-phenyl-5-ethyl-1,2-dihydro-4-hydroxy-1-methyl-2-oxo-3-quinolinecarboxamide
n-ethyl-n-phenyl- 5-ethyl- 1,2-dihydro- 4-hydroxy- 1-methyl- 2-oxo- 3-quinolinecarboxamide
DIKSYHCCYVYKRO-UHFFFAOYSA-N
n,5-diethyl-4-hydroxy-1-methyl-2-oxo-n-phenyl-1,2-dihydroquinoline-3-carboxamide ,
SCHEMBL1573633
DTXSID90179537
CS-0019027
HY-100442
DB13118
abr25757
abr 25757
abr-25757
BS-16767
EX-A2923
paquinimod; abr 25757
abr?215757; abr 215757; abr21575
BCP29381
SB17375
Q27279838
C74280
AKOS037649156
n,5-diethyl-4-hydroxy-1-methyl-2-oxo-n-phenylquinoline-3-carboxamide
BP164809
abr?215757

Research Excerpts

Overview

Paquinimod is an immunomodulatory compound preventing S100A9 binding to TLR-4.

ExcerptReferenceRelevance
"Paquinimod is an immunomodulatory compound preventing S100A9 binding to TLR-4."( Prophylactic treatment with S100A9 inhibitor paquinimod reduces pathology in experimental collagenase-induced osteoarthritis.
Blom, AB; Eriksson, H; Geven, EJ; Koenders, MI; Leanderson, T; Roth, J; Schelbergen, RF; van de Loo, FA; van den Berg, WB; van den Bosch, MH; van der Kraan, PM; van Lent, PL; Vogl, T, 2015
)
1.4

Treatment

Paquinimod treatment of collagenase-induced OA (CIOA) resulted in significantly reduced synovial thickening. Treatment also resulted in a reduced TGFβ-response in the skin and an abrogation of the increased auto-antibody production.

ExcerptReferenceRelevance
"Paquinimod treatment of collagenase-induced OA (CIOA) resulted in significantly reduced synovial thickening (57%), osteophyte size at the medial femur (66%) and cruciate ligaments (67%) and cartilage damage at the medial tibia (47%) and femur (75%; n=7, untreated n=6). "( Prophylactic treatment with S100A9 inhibitor paquinimod reduces pathology in experimental collagenase-induced osteoarthritis.
Blom, AB; Eriksson, H; Geven, EJ; Koenders, MI; Leanderson, T; Roth, J; Schelbergen, RF; van de Loo, FA; van den Berg, WB; van den Bosch, MH; van der Kraan, PM; van Lent, PL; Vogl, T, 2015
)
2.12
"Paquinimod treatment also resulted in a reduced TGFβ-response in the skin and an abrogation of the increased auto-antibody production in this SSc model."( Paquinimod reduces skin fibrosis in tight skin 1 mice, an experimental model of systemic sclerosis.
Eriksson, H; Leanderson, T; Liberg, D; Nyhlén, HC; Sparre, B; Stenström, M; Törngren, M; Tuvesson, H, 2016
)
2.6
"Paquinimod treatment resulted in disease inhibition in MRL-lpr/lpr mice, comparable to that obtained with prednisolone and mycophenolate mofetil; prominent effects on disease manifestations and serologic markers and a steroid-sparing effect were observed. "( Pharmacokinetics, tolerability, and preliminary efficacy of paquinimod (ABR-215757), a new quinoline-3-carboxamide derivative: studies in lupus-prone mice and a multicenter, randomized, double-blind, placebo-controlled, repeat-dose, dose-ranging study in
Axelsson, B; Bengtsson, AA; Leanderson, T; Lood, C; Ohman, MW; Rönnblom, L; Sparre, B; Sturfelt, G; Tuvesson, H; van Vollenhoven, RF, 2012
)
2.06

Toxicity

ExcerptReferenceRelevance
" Reported adverse events (AEs) were mild to moderate and expected with the most common being arthralgia (n = 3) and headache (n = 3), and C-reactive protein (CRP) increase."( An open-label study to evaluate biomarkers and safety in systemic sclerosis patients treated with paquinimod.
Andersson, F; Distler, JHW; Distler, O; Eriksson, H; Hesselstrand, R; Nyhlén, HC; Riemekasten, G; Sparre, B; Törngren, M; Tuvesson, H; Wuttge, DM, 2021
)
0.84

Pharmacokinetics

The pharmacokinetic properties of paquinimod were linear and well suitable for once-daily oral treatment.

ExcerptReferenceRelevance
" Dose-response data and pharmacokinetic data were used to calculate effective and safe clinical doses of paquinimod."( Pharmacokinetics, tolerability, and preliminary efficacy of paquinimod (ABR-215757), a new quinoline-3-carboxamide derivative: studies in lupus-prone mice and a multicenter, randomized, double-blind, placebo-controlled, repeat-dose, dose-ranging study in
Axelsson, B; Bengtsson, AA; Leanderson, T; Lood, C; Ohman, MW; Rönnblom, L; Sparre, B; Sturfelt, G; Tuvesson, H; van Vollenhoven, RF, 2012
)
0.84
" In patients with SLE, the pharmacokinetic properties of paquinimod were linear and well suitable for once-daily oral treatment."( Pharmacokinetics, tolerability, and preliminary efficacy of paquinimod (ABR-215757), a new quinoline-3-carboxamide derivative: studies in lupus-prone mice and a multicenter, randomized, double-blind, placebo-controlled, repeat-dose, dose-ranging study in
Axelsson, B; Bengtsson, AA; Leanderson, T; Lood, C; Ohman, MW; Rönnblom, L; Sparre, B; Sturfelt, G; Tuvesson, H; van Vollenhoven, RF, 2012
)
0.87

Dosage Studied

ExcerptRelevanceReference
" Dose-response data and pharmacokinetic data were used to calculate effective and safe clinical doses of paquinimod."( Pharmacokinetics, tolerability, and preliminary efficacy of paquinimod (ABR-215757), a new quinoline-3-carboxamide derivative: studies in lupus-prone mice and a multicenter, randomized, double-blind, placebo-controlled, repeat-dose, dose-ranging study in
Axelsson, B; Bengtsson, AA; Leanderson, T; Lood, C; Ohman, MW; Rönnblom, L; Sparre, B; Sturfelt, G; Tuvesson, H; van Vollenhoven, RF, 2012
)
0.84
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (3)

Assay IDTitleYearJournalArticle
AID115065Inhibition of acute experimental autoimmune encephalomyelitis (aEAE) induced in SJL/N mice at a dose of 1 mg/kg/day, (po)2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
Synthesis and biological evaluation of new 1,2-dihydro-4-hydroxy-2-oxo-3-quinolinecarboxamides for treatment of autoimmune disorders: structure-activity relationship.
AID115054Inhibition of acute experimental autoimmune encephalomyelitis in SJL/N mice by 0.2 mg/kg/day p.o.2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
Synthesis and biological evaluation of new 1,2-dihydro-4-hydroxy-2-oxo-3-quinolinecarboxamides for treatment of autoimmune disorders: structure-activity relationship.
AID115204Inhibition of acute experimental autoimmune encephalomyelitis (aEAE) induced in SJL/N mice at a dose of 5 mg/kg/day, (po) was determined; Not determined2004Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
Synthesis and biological evaluation of new 1,2-dihydro-4-hydroxy-2-oxo-3-quinolinecarboxamides for treatment of autoimmune disorders: structure-activity relationship.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (13)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (7.69)29.6817
2010's9 (69.23)24.3611
2020's3 (23.08)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 35.31

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 Index35.31 (24.57)
Research Supply Index2.77 (2.92)
Research Growth Index5.65 (4.65)
Search Engine Demand Index44.85 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (35.31)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (7.14%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other13 (92.86%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]