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 Source	ID
PubMed CID	54684617
CHEMBL ID	67776
SCHEMBL ID	1573633
MeSH ID	M0575224

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.

Excerpt	Reference	Relevance
"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.

Excerpt	Reference	Relevance
"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

Excerpt	Reference	Relevance
" 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.

Excerpt	Reference	Relevance
" 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

Excerpt	Relevance	Reference
" 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 ID	Title	Year	Journal	Article
AID115065	Inhibition of acute experimental autoimmune encephalomyelitis (aEAE) induced in SJL/N mice at a dose of 1 mg/kg/day, (po)	2004	Journal 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.
AID115054	Inhibition of acute experimental autoimmune encephalomyelitis in SJL/N mice by 0.2 mg/kg/day p.o.	2004	Journal 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.
AID115204	Inhibition of acute experimental autoimmune encephalomyelitis (aEAE) induced in SJL/N mice at a dose of 5 mg/kg/day, (po) was determined; Not determined	2004	Journal 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)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	1 (7.69)	29.6817
2010's	9 (69.23)	24.3611
2020's	3 (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.

Metric	This Compound (vs All)
Research Demand Index	35.31 (24.57)
Research Supply Index	2.77 (2.92)
Research Growth Index	5.65 (4.65)
Search Engine Demand Index	44.85 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (35.31)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	1 (7.14%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	13 (92.86%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
prednisolone Prednisolone: A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.. prednisolone : A glucocorticoid that is prednisone in which the oxo group at position 11 has been reduced to the corresponding beta-hydroxy group. It is a drug metabolite of prednisone.	3.46	1	1	11beta-hydroxy steroid; 17alpha-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(1),Delta(4)-steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone; tertiary alpha-hydroxy ketone	adrenergic agent; anti-inflammatory drug; antineoplastic agent; drug metabolite; environmental contaminant; immunosuppressive agent; xenobiotic
sucrose Saccharum: A plant genus of the family POACEAE widely cultivated in the tropics for the sweet cane that is processed into sugar.	2.17	1	0	glycosyl glycoside	algal metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; osmolyte; Saccharomyces cerevisiae metabolite; sweetening agent
aluminum sulfate aluminium sulfate (anhydrous) : An aluminium sulfate that contains no water of crystallisation.	2.1	1	0	aluminium sulfate
mycophenolic acid Mycophenolic Acid: Compound derived from Penicillium stoloniferum and related species. It blocks de novo biosynthesis of purine nucleotides by inhibition of the enzyme inosine monophosphate dehydrogenase (IMP DEHYDROGENASE). Mycophenolic acid exerts selective effects on the immune system in which it prevents the proliferation of T-CELLS, LYMPHOCYTES, and the formation of antibodies from B-CELLS. It may also inhibit recruitment of LEUKOCYTES to sites of INFLAMMATION.. mycophenolate : A monocarboxylic acid anion resulting from the removal of a proton from the carboxy group of mycophenolic acid.. mycophenolic acid : A member of the class of 2-benzofurans that is 2-benzofuran-1(3H)-one which is substituted at positions 4, 5, 6, and 7 by methyl, methoxy, (2E)-5-carboxy-3-methylpent-2-en-1-yl, and hydroxy groups, respectively. It is an antibiotic produced by Penicillium brevi-compactum, P. stoloniferum, P. echinulatum and related species. An immunosuppressant, it is widely used (partiularly as its sodium salt and as the 2-(morpholin-4-yl)ethyl ester prodrug, mycophenolate mofetil) to prevent tissue rejection following organ transplants and for the treatment of certain autoimmune diseases.	3.46	1	1	2-benzofurans; gamma-lactone; monocarboxylic acid; phenols	anticoronaviral agent; antimicrobial agent; antineoplastic agent; EC 1.1.1.205 (IMP dehydrogenase) inhibitor; environmental contaminant; immunosuppressive agent; mycotoxin; Penicillium metabolite; xenobiotic
ovalbumin Ovalbumin: An albumin obtained from the white of eggs. It is a member of the serpin superfamily.	7.31	1	0
quinoline-3-carboxamide quinoline-3-carboxamide: structure in first source	3.87	2	1
roquinimex roquinimex: structure in first source	2.02	1	0	aromatic amide
laquinimod [no description available]	2.02	1	0	aromatic amide
transforming growth factor beta Transforming Growth Factor beta: A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins.	2.13	1	0

Condition	Indicated	Relationship Strength	Studies	Trials
Autoimmune Disease [description not available]	0	2.46	2	0
Allergic Encephalomyelitis [description not available]	0	2.45	2	0
Autoimmune Diseases Disorders that are characterized by the production of antibodies that react with host tissues or immune effector cells that are autoreactive to endogenous peptides.	0	2.46	2	0
Colitis Inflammation of the COLON section of the large intestine (INTESTINE, LARGE), usually with symptoms such as DIARRHEA (often with blood and mucus), ABDOMINAL PAIN, and FEVER.	0	2.31	1	0
Asthma, Bronchial [description not available]	0	2.31	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	4.76	6	1
Asthma A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).	0	7.31	1	0
Sclerosis, Systemic [description not available]	0	3.51	2	0
Scleroderma, Systemic A chronic multi-system disorder of CONNECTIVE TISSUE. It is characterized by SCLEROSIS in the SKIN, the LUNGS, the HEART, the GASTROINTESTINAL TRACT, the KIDNEYS, and the MUSCULOSKELETAL SYSTEM. Other important features include diseased small BLOOD VESSELS and AUTOANTIBODIES. The disorder is named for its most prominent feature (hard skin), and classified into subsets by the extent of skin thickening: LIMITED SCLERODERMA and DIFFUSE SCLERODERMA.	1	5.51	2	0
Uveitis Inflammation of part or all of the uvea, the middle (vascular) tunic of the eye, and commonly involving the other tunics (sclera and cornea, and the retina). (Dorland, 27th ed)	0	2.17	1	0
Autoimmune Diabetes [description not available]	0	2.17	1	0
Glycosuria The appearance of an abnormally large amount of GLUCOSE in the urine, such as more than 500 mg/day in adults. It can be due to HYPERGLYCEMIA or genetic defects in renal reabsorption (RENAL GLYCOSURIA).	0	2.17	1	0
Diabetes Mellitus, Type 1 A subtype of DIABETES MELLITUS that is characterized by INSULIN deficiency. It is manifested by the sudden onset of severe HYPERGLYCEMIA, rapid progression to DIABETIC KETOACIDOSIS, and DEATH unless treated with insulin. The disease may occur at any age, but is most common in childhood or adolescence.	0	2.17	1	0
Depression Depressive states usually of moderate intensity in contrast with MAJOR DEPRESSIVE DISORDER present in neurotic and psychotic disorders.	0	2.17	1	0
Atherogenesis [description not available]	0	2.08	1	0
Atheroma [description not available]	0	2.08	1	0
Angiitis [description not available]	0	2.08	1	0
Vasculitis Inflammation of any one of the blood vessels, including the ARTERIES; VEINS; and rest of the vasculature system in the body.	0	2.08	1	0
Atherosclerosis A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA.	0	2.08	1	0
Innate Inflammatory Response [description not available]	0	2.08	1	0
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	0	2.08	1	0
Primary Peritonitis [description not available]	0	2.1	1	0
Peritonitis INFLAMMATION of the PERITONEUM lining the ABDOMINAL CAVITY as the result of infectious, autoimmune, or chemical processes. Primary peritonitis is due to infection of the PERITONEAL CAVITY via hematogenous or lymphatic spread and without intra-abdominal source. Secondary peritonitis arises from the ABDOMINAL CAVITY itself through RUPTURE or ABSCESS of intra-abdominal organs.	0	2.1	1	0
Adjuvant Arthritis [description not available]	0	2.11	1	0
Cirrhosis [description not available]	0	2.13	1	0
Fibrosis Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury.	0	7.13	1	0
Libman-Sacks Disease [description not available]	0	3.46	1	1
Lupus Erythematosus, Systemic A chronic, relapsing, inflammatory, and often febrile multisystemic disorder of connective tissue, characterized principally by involvement of the skin, joints, kidneys, and serosal membranes. It is of unknown etiology, but is thought to represent a failure of the regulatory mechanisms of the autoimmune system. The disease is marked by a wide range of system dysfunctions, an elevated erythrocyte sedimentation rate, and the formation of LE cells in the blood or bone marrow.	1	5.46	1	1

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