Page last updated: 2024-11-13

laquinimod

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 CID54677946
CHEMBL ID66092
CHEBI ID134738
SCHEMBL ID39441
SCHEMBL ID39440
MeSH IDM0452523

Synonyms (58)

Synonym
HY-13010
abr-215062
laquinimod ,
abr215062
abr 215062
CHEBI:134738
abr-215062 free acid
tv-5600 free acid
CHEMBL66092
AKOS005146322
248281-84-7
3-quinolinecarboxamide, 5-chloro-n-ethyl-1,2-dihydro-4-hydroxy-1-methyl-2-oxo-n-phenyl-
908sy76s4g ,
5-chloro-n-ethyl-4-hydroxy-1-methyl-2-oxo-n-phenyl-1,2-dihydroquinoline-3-carboxamide
n-ethyl-n-phenyl-1,2-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide
laquinimod [inn]
unii-908sy76s4g
n-ethyl-n-phenyl-5-chloro-1,2-dihydro-4-hydroxy-1-methyl-2-oxoquinoline-3-carboxamide
BCP9000840
CS-0839
laquinimod,abr-215062
BCP0726000056
laquinimod pound notabr215062
NCGC00346701-01
PB32648
5-chloro-4-hydroxy-1-methyl-2-oxo-n-ethyl-n-phenyl-1,2-dihydroquinoline-3-carboxamide
laquinimod [who-dd]
laquinimod [mi]
S2787
laquinimod,5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydro-quinoline-3-carboxylic acid ethyl-phenyl-amide
gtpl7639
n-ethyl-n-phenyl-5-chloro-1,2-dihydro-4-hydroxy-1-methyl-2-oxo-quinoline-3-carboxamide
GKWPCEFFIHSJOE-UHFFFAOYSA-N
MLS006010210
MLS006010286
smr004701305
SCHEMBL39441
SCHEMBL39440
laquinimod (abr-215062)
5-chloro-n-ethyl-4-hydroxy-1-methyl-2-oxo-n-phenylquinoline-3-carboxamide
FT-0698088
DTXSID30179536
AKOS025395670
J-521632
EX-A079
5-chloro-n-et-4-hydroxy-1-methyl-2-oxo-n-ph-1,2-dihydroquinoline-3-carboxamide
HMS3656N08
civentichem cv-4057
SW220142-1
abr-215062 (laquinimod)
DB06685
BCP04521
Q3487584
mfcd08689859
BS-16743
AMY6804
CCG-268120
NCGC00346701-07

Research Excerpts

Overview

Lquinimod is a quinoline-3-carboxamide and a novel oral immunomodulatory compound in clinical use. The drug is an anti-inflammatory agent with good central nervous system (CNS) bioavailability, and neuroprotective and myelorestorative properties.

ExcerptReferenceRelevance
"Laquinimod is a quinoline-3-carboxamide and a novel oral immunomodulatory compound in clinical use."( Laquinimod Mitigated IL-1β-Induced Impairment of the Cartilage Extracellular Matrix in Human ATDC5 Chondrocytes.
Dan, F; Ruan, W; Xie, P; Yu, G; Yu, H, 2020
)
2.72
"Laquinimod is a drug developed for the treatment of MS known to activate AHR, but the cellular targets of laquinimod are still not completely known."( Aryl Hydrocarbon Receptor Activation in Astrocytes by Laquinimod Ameliorates Autoimmune Inflammation in the CNS.
Alves de Lima, K; Borucki, DM; Chao, CC; Kaye, J; Kenison, JE; Li, Z; Quintana, FJ; Rothhammer, V; Takenaka, MC; Tjon, E, 2021
)
1.59
"Laquinimod is an anti-inflammatory agent with good central nervous system (CNS) bioavailability, and neuroprotective and myelorestorative properties. "( Laquinimod has no effects on brain volume or cellular CNS composition in the F1 3xTg-AD/C3H mouse model of Alzheimer's disease.
Cutter, GR; Fu, M; Hayardeny, L; Hussain, RZ; Jaramillo, TC; Lambracht-Washington, D; Miller-Little, WA; Powell, CM; Rosenberg, RN; Stüve, O; Takahashi, M; Zhang, S, 2017
)
3.34
"Laquinimod is an orally administered immunomodulatory substance currently under development for the treatment of multiple sclerosis (MS) and HD."( Laquinimod treatment in the R6/2 mouse model.
Blusch, A; Brunner, J; Ellrichmann, G; Fatoba, O; Gold, R; Hayardeny, L; Hayden, M; Reick, C; Saft, C; Sehr, D; Winklhofer, KF, 2017
)
2.62
"Laquinimod is an oral immunomodulator in clinical development to treat relapsing-remitting multiple sclerosis (RRMS). "( Safety and in vivo immune assessment of escalating doses of oral laquinimod in patients with RRMS.
Bar-Ilan, O; Hayardeny, L; Mimrod, D; Paul, F; Richter, N; Samara, E; Sehr, T; Sorani, E; Spiegelstein, O; Thomas, K; Tumani, H; Ziemssen, T, 2017
)
2.14
"Laquinimod is an immunomodulatory drug under clinical investigation for the treatment of the progressive form of multiple sclerosis (MS) with both anti-inflammatory and neuroprotective effects. "( Laquinimod ameliorates excitotoxic damage by regulating glutamate re-uptake.
Bullitta, S; Centonze, D; De Vito, F; Fresegna, D; Gentile, A; Mandolesi, G; Musella, A; Rizzo, FR, 2018
)
3.37
"Laquinimod is an orally dosed immuno-modulator currently under development for Huntington's disease (HD). "( The effect of laquinimod, a novel immuno-modulator in development to treat Huntington disease, on the pharmacokinetics of ethinylestradiol and levonorgestrel in healthy young women.
Bar-Ilan, O; Dror, V; Elgart, A; Korver, T; Mimrod, D; Spiegelstein, O; Zur, AA, 2019
)
2.32
"Laquinimod is an orally administered compound that is under investigation in relapsing-remitting multiple sclerosis. "( Modulation of dendritic cell properties by laquinimod as a mechanism for modulating multiple sclerosis.
Furlan, R; Hubo, M; Jolivel, V; Jonuleit, H; Klebow, S; Kraus, SH; Luessi, F; Masri, J; Paterka, M; Poisa-Beiro, L; Siffrin, V; Tumani, H; Waisman, A; Yogev, N; Zipp, F, 2013
)
2.1
"Laquinimod is a novel orally active agent with immunomodulatory properties that was shown to be effective in suppressing disease activity in relapsing-remitting multiple sclerosis patients. "( Assessment of changes in immune measures of multiple sclerosis patients treated with laquinimod.
Barilan, O; Gilmore, W; Hayardeny, L; Kelland, EE; Lund, BT; Weiner, LP, 2013
)
2.06
"Laquinimod is a new orally administered synthetic drug designed as an immunomodulator. "( Review of laquinimod and its therapeutic potential in multiple sclerosis.
Gold, R; Thöne, J, 2013
)
2.23
"Laquinimod is a novel oral drug that is currently being evaluated for the treatment of relapsing-remitting multiple sclerosis (RRMS). "( Laquinimod, an up-and-coming immunomodulatory agent for treatment of multiple sclerosis.
Schulze-Topphoff, U; Varrin-Doyer, M; Zamvil, SS, 2014
)
3.29
"Laquinimod is an immunomodulatory drug with neuroprotective potential. "( Laquinimod exerts strong clinical and immunomodulatory effects in Lewis rat experimental autoimmune neuritis.
Ambrosius, B; Gold, R; Hayardeny, L; Hayden, M; Pitarokoili, K; Schrewe, L, 2014
)
3.29
"Laquinimod is a novel oral immunomodulatory drug for the treatment of multiple sclerosis (MS). "( Effects of the anti-multiple sclerosis immunomodulator laquinimod on anxiety and depression in rodent behavioral models.
Amit, BH; Gil-Ad, I; Gueta, RU; Hayardeni, L; Taler, M; Tarasenko, I; Weizman, A, 2015
)
2.11
"Laquinimod is an orally active immunomodulatory small molecule that has shown clear clinical benefit in trials for relapsing-remitting multiple sclerosis and in experimental rodent models that emulate multiple sclerosis (MS). "( In vitro assessment of the direct effect of laquinimod on basic functions of human neural stem cells and oligodendrocyte progenitor cells.
Gilmore, W; Hayardeny, L; Kelland, EE; Lund, BT; Weiner, LP, 2014
)
2.11
"Laquinimod is an oral therapeutic agent under investigation for the treatment of Crohn's disease (CD), Huntington's disease, lupus nephritis and multiple sclerosis. "( A phase II study of laquinimod in Crohn's disease.
Barkay, H; Brown, K; Colombel, JF; D'Haens, G; Feagan, BG; Haviv, A; Rutgeerts, P; Sakov, A; Sandborn, WJ, 2015
)
2.18
"Laquinimod, is a potential oral immunomodulatory drug, for relapsing-remitting multiple sclerosis (RRMS). "( The role of laquinimod in modulation of the immune response in relapsing-remitting multiple sclerosis: Lessons from gene expression signatures.
Achiron, A; Gurevich, M; Hayardeny, L; Zilkha-Falb, R, 2015
)
2.24
"Laquinimod (ABR-215062) is an oral immunomodulatory agent developed for the treatment of relapsing multiple sclerosis (MS). "( Laquinimod (ABR-215062) for the treatment of relapsing multiple sclerosis.
Constantinescu, CS; Constantinescu, SE, 2016
)
3.32
"Laquinimod is an orally active immunomodulator that down-regulates proinflammatory cytokine production in peripheral blood mononuclear cells, and in the brain down-regulates astrocytic and microglial activation by modulating NFκB signalling."( Laquinimod dampens hyperactive cytokine production in Huntington's disease patient myeloid cells.
Dobson, L; Farmer, R; Hayardeny, L; Hayden, MR; Loupe, P; Tabrizi, SJ; Träger, U, 2016
)
2.6
"Laquinimod (ABR-215062) is a new orally available carboxamide derivative, which is currently developed for relapsing remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases. "( Laquinimod in the treatment of multiple sclerosis: a review of the data so far.
Linker, RA; Thöne, J, 2016
)
3.32
"Laquinimod is a new once-daily oral administrable agent, which is under investigation in a phase 3 clinical trial for relapsing remitting multiple sclerosis (RRMS) and in a phase 2 clinical trial for primary progressive MS (PPMS)."( Laquinimod in the treatment of relapsing remitting multiple sclerosis.
Hainke, U; Thomas, K; Ziemssen, T, 2016
)
3.32
"Laquinimod is a first in class oral agent with high potential to reduce disease progression in RRMS and PPMS. "( Laquinimod in the treatment of relapsing remitting multiple sclerosis.
Hainke, U; Thomas, K; Ziemssen, T, 2016
)
3.32
"Laquinimod is an immunomodulatory compound that has shown neuroprotective benefits in clinical trials for multiple sclerosis. "( Laquinimod decreases Bax expression and reduces caspase-6 activation in neurons.
Caron, NS; Deng, Y; Ehrnhoefer, DE; Hayden, MR; Qiu, X; Tsang, M, 2016
)
3.32
"Laquinimod is an oral drug currently being evaluated for the treatment of relapsing, remitting, and primary progressive multiple sclerosis and Huntington's disease. "( Laquinimod arrests experimental autoimmune encephalomyelitis by activating the aryl hydrocarbon receptor.
Amit-Romach, E; Ator, MA; Birnberg, T; Caballero, IS; Grossman, I; Hayden, MR; Hingaly, T; Kashi, R; Kaye, J; Knappertz, V; Laifenfeld, D; Laufer, R; Marantz, Y; Orbach, A; Piryatinsky, V; Raymond, E; Rubinstein, E; Shinar, D; Towfic, F, 2016
)
3.32
"Laquinimod is a quinoline carboxamide showing structural similarities with kynurenic acid, which proved to have beneficial effects on reduction of brain atrophy and disability progression."( Kynurenine System and Multiple Sclerosis, Pathomechanism and Drug Targets with An Emphasis on Laquinimod.
Annus, A; Majlath, Z; Vecsei, L, 2018
)
1.42
"Laquinimod is a new quinolonecarboxamide that has demonstrated efficacy in animal models of several autoimmune diseases, including MS. "( Oral laquinimod therapy in relapsing multiple sclerosis.
Preiningerova, J, 2009
)
2.31
"Laquinimod is a novel, orally administered immunomodulator that has advanced to the pre-submission stage and may become an alternative to the current injectable first-line treatments for relapsing MS."( Oral laquinimod therapy in relapsing multiple sclerosis.
Preiningerova, J, 2009
)
2.31
"Laquinimod (LAQ) is a new immunomodulatory drug shown to be effective in the treatment of relapsing-remitting multiple sclerosis (RRMS); however, its molecular target pathways are not well recognized. "( Laquinimod suppress antigen presentation in relapsing-remitting multiple sclerosis: in-vitro high-throughput gene expression study.
Achiron, A; Feldman, A; Gritzman, T; Gurevich, M; Orbach, R; Tuller, T, 2010
)
3.25
"Laquinimod is a new quinolone-carboxamide that has shown efficacy in various animal models of autoimmune disease, including MS. "( Oral laquinimod treatment in multiple sclerosis.
Fernández, O, 2011
)
2.33
"Laquinimod is a novel, orally administered immunomodulator that has advanced to phase III study, a pre-submission stage to the regulatory agencies, and may become an alternative to the current injectable first-line treatments for RRMS."( Oral laquinimod treatment in multiple sclerosis.
Fernández, O, 2011
)
2.33
"Laquinimod is a promising new orally administered substance which has demonstrated beneficial effects in placebo-controlled trials in patients with RRMS and is currently under investigation in two global Phase III trials."( Laquinimod: a promising oral medication for the treatment of relapsing-remitting multiple sclerosis.
Gold, R; Thöne, J, 2011
)
2.53
"Laquinimod is a small, novel, orally active, well-tolerated molecule that significantly reduced gadolinium-enhancing lesions in patients with multiple sclerosis (MS). "( Insight into the mechanism of laquinimod action.
Brück, W; Wegner, C, 2011
)
2.1
"Laquinimod is a novel, orally administered immune-modulatory molecule in advanced phase clinical trials in relapsing-remitting multiple sclerosis. "( Laquinimod in multiple sclerosis.
Bar-Or, A; Giacomini, PS, 2012
)
3.26
"Laquinimod is a promising, orally available compound that has been successfully evaluated in placebo-controlled phase II/III studies of relapsing-remitting multiple sclerosis (MS). "( Modulation of autoimmune demyelination by laquinimod via induction of brain-derived neurotrophic factor.
Comi, G; Conrad, R; Ellrichmann, G; Gold, R; Hayardeny, L; Lee, DH; Linker, RA; Peruga, I; Seubert, S; Thöne, J; Wiese, S, 2012
)
2.09
"Laquinimod is a novel oral drug that is currently being evaluated for the treatment of relapsing-remitting (RR) multiple sclerosis (MS). "( Laquinimod, a quinoline-3-carboxamide, induces type II myeloid cells that modulate central nervous system autoimmunity.
Molnarfi, N; Nelson, PA; Sagan, SA; Schulze-Topphoff, U; Shetty, A; Sobel, RA; Varrin-Doyer, M; Zamvil, SS, 2012
)
3.26
"Laquinimod is a novel, small, orally administered medication that has demonstrated efficacy in the treatment of multiple sclerosis, a chronic inflammatory demyelinating disease of the CNS. "( Laquinimod, a once-daily oral drug in development for the treatment of relapsing-remitting multiple sclerosis.
Brück, W; Zamvil, SS, 2012
)
3.26
"Laquinimod is an orally active molecule that showed efficacy in clinical trials in multiple sclerosis. "( Oral treatment with laquinimod augments regulatory T-cells and brain-derived neurotrophic factor expression and reduces injury in the CNS of mice with experimental autoimmune encephalomyelitis.
Aharoni, R; Arnon, R; Eilam, R; Hayardeny, L; Saada, R; Sela, M, 2012
)
2.15
"Laquinimod (LAQ) is a new oral immunomodulatory compound that reduces relapse rate, brain atrophy and disability progression in multiple sclerosis (MS). "( Reduced astrocytic NF-κB activation by laquinimod protects from cuprizone-induced demyelination.
Brakelmann, L; Brück, W; Hagemeier, K; Hanisch, UK; Hayardeny, L; John, GR; Kramann, N; Kuhlmann, T; Pförtner, R; Pham, T; Piryatinsky, V; Regen, T; Stadelmann, C; van Rossum, D; Wegner, C; Zhang, J, 2012
)
2.09
"Laquinimod is an orally administered drug under development for the treatment of Multiple Sclerosis (MS), lacking a fully elucidated mode of action. "( Laquinimod modulates B cells and their regulatory effects on T cells in multiple sclerosis.
Hayardeny, L; Melamed, D; Miller, A; Nussbaum, S; Snir, A; Staun-Ram, E; Toubi, E, 2012
)
3.26
"Laquinimod is an immunomodulator that is currently in clinical trials. "( Determination of laquinimod in plasma by coupled-column liquid chromatography with ultraviolet absorbance detection.
Edman, K; Eriksson, B; Gunnarsson, PO; Svensson, L, 2003
)
2.1
"Laquinimod is a novel immunomodulatory substance developed as an orally available disease modifying treatment in multiple sclerosis (MS). "( Treatment with laquinimod reduces development of active MRI lesions in relapsing MS.
Barkhof, F; Linde, A; Nederman, T; Nordle, O; Polman, C; Sandberg-Wollheim, M, 2005
)
2.12
"Laquinimod is a novel oral immunomodulatory substance, which is currently developed for the treatment of multiple sclerosis (MS). "( Inhibition of the development of chronic experimental autoimmune encephalomyelitis by laquinimod (ABR-215062) in IFN-beta k.o. and wild type mice.
Axelsson, B; Leanderson, T; Ohlsson, L; Runström, A, 2006
)
2
"Laquinimod (ABR-215062) is a synthetic compound currently undergoing clinical development for oral treatment of multiple sclerosis. "( Determination of the immunomodulator laquinimod in human plasma by liquid chromatography/tandem mass spectrometry; development, validation and application of two methods in clinical pharmacokinetic profiling.
Edman, K; Gunnarsson, PO; Hansson, G; Olin, M; Sennbro, CJ; Svensson, LD, 2006
)
2.05

Actions

ExcerptReferenceRelevance
"Laquinimod was shown to inhibit both disease development and histopathological changes in the CNS."( Inhibition of the development of chronic experimental autoimmune encephalomyelitis by laquinimod (ABR-215062) in IFN-beta k.o. and wild type mice.
Axelsson, B; Leanderson, T; Ohlsson, L; Runström, A, 2006
)
1.28

Treatment

Laquimod was associated with reduced numbers of monocyte/macrophages, dendritic cells, and lymphocytes. Laquinimod treatment restored BDNF expression to its level in healthy controls. Treatment ameliorated spontaneous colitis in mice.

ExcerptReferenceRelevance
"Laquinimod-treated patients showed more abnormal laboratory levels in liver enzymes, P-amylase, C-reactive protein (CRP), and fibrinogen, but most shifts were clinically non-significant."( Safety and in vivo immune assessment of escalating doses of oral laquinimod in patients with RRMS.
Bar-Ilan, O; Hayardeny, L; Mimrod, D; Paul, F; Richter, N; Samara, E; Sehr, T; Sorani, E; Spiegelstein, O; Thomas, K; Tumani, H; Ziemssen, T, 2017
)
1.41
"In laquinimod-treated patients with multiple sclerosis we consistently found reduced chemokine and cytokine secretion by conventional CD1c+ dendritic cells upon lipopolysaccharide stimulation."( Modulation of dendritic cell properties by laquinimod as a mechanism for modulating multiple sclerosis.
Furlan, R; Hubo, M; Jolivel, V; Jonuleit, H; Klebow, S; Kraus, SH; Luessi, F; Masri, J; Paterka, M; Poisa-Beiro, L; Siffrin, V; Tumani, H; Waisman, A; Yogev, N; Zipp, F, 2013
)
1.17
"Laquinimod treatment was associated with reduced numbers of monocyte/macrophages, dendritic cells, and lymphocytes, as well as with induction of myeloid-derived suppressor cells in spleens and kidneys."( Laquinimod delays and suppresses nephritis in lupus-prone mice and affects both myeloid and lymphoid immune cells.
Hahn, BH; Lourenço, EV; Palma-Diaz, MF; Skaggs, BJ; Wong, M, 2014
)
2.57
"Laquinimod treatment was associated with an excellent safety and tolerability profile."( Laquinimod, an up-and-coming immunomodulatory agent for treatment of multiple sclerosis.
Schulze-Topphoff, U; Varrin-Doyer, M; Zamvil, SS, 2014
)
2.57
"Laquinimod treatment ameliorated spontaneous colitis in Il10(-/-) mice, which was associated with decreased T-cell-associated pro-inflammatory cytokines. "( Laquinimod ameliorates spontaneous colitis in interleukin-10-gene-deficient mice with improved barrier function.
Dong, J; Gong, J; Li, J; Li, Y; Shen, X; Sun, J; Wang, H; Zhao, J; Zhu, W; Zuo, L, 2015
)
3.3
"Oral laquinimod treatment reversed established RR-EAE and was associated with reduced central nervous system (CNS) inflammation, decreased Th1 and Th17 responses, and an increase in regulatory T cells (Treg)."( Laquinimod, a quinoline-3-carboxamide, induces type II myeloid cells that modulate central nervous system autoimmunity.
Molnarfi, N; Nelson, PA; Sagan, SA; Schulze-Topphoff, U; Shetty, A; Sobel, RA; Varrin-Doyer, M; Zamvil, SS, 2012
)
2.28
"Laquinimod treatment restored BDNF expression to its level in healthy controls."( Oral treatment with laquinimod augments regulatory T-cells and brain-derived neurotrophic factor expression and reduces injury in the CNS of mice with experimental autoimmune encephalomyelitis.
Aharoni, R; Arnon, R; Eilam, R; Hayardeny, L; Saada, R; Sela, M, 2012
)
1.42
"Treatment with laquinimod 0.5 mg showed consistent effects on remission (48.3% (CI 31% to 66%) vs 15.9% (CI 9% to 27%)), response 100 (55.2% (CI 37% to 71%) vs 31.7% (CI 22% to 44%)) and response 70 (62.1% (CI 44% to 77%) vs 34.9% (CI 24% to 47%)) versus placebo."( A phase II study of laquinimod in Crohn's disease.
Barkay, H; Brown, K; Colombel, JF; D'Haens, G; Feagan, BG; Haviv, A; Rutgeerts, P; Sakov, A; Sandborn, WJ, 2015
)
1.08
"Treatment with laquinimod for 6 months rescued atrophy in the striatum, in certain cortical regions, and in the corpus callosum of YAC128 HD mice."( Laquinimod rescues striatal, cortical and white matter pathology and results in modest behavioural improvements in the YAC128 model of Huntington disease.
Caron, NS; Chuang, KH; Franciosi, S; Garcia-Miralles, M; Hayardeny, L; Hayden, MR; Hong, X; Huang, Y; Lin, RY; Papapetropoulos, S; Pouladi, MA; Tan, LJ; To, XV, 2016
)
2.22
"Treatment with laquinimod resulted in a significant and persistent increase in BDNF serum levels of MS patients when compared to baseline and placebo-treated patients."( Modulation of autoimmune demyelination by laquinimod via induction of brain-derived neurotrophic factor.
Comi, G; Conrad, R; Ellrichmann, G; Gold, R; Hayardeny, L; Lee, DH; Linker, RA; Peruga, I; Seubert, S; Thöne, J; Wiese, S, 2012
)
0.98
"Treatment with laquinimod as compared with placebo was associated with a modest reduction in the mean (±SE) annualized relapse rate (0.30±0.02 vs. "( Placebo-controlled trial of oral laquinimod for multiple sclerosis.
Boyko, A; Comi, G; Filippi, M; Jeffery, D; Kappos, L; Montalban, X; Rocca, MA, 2012
)
1.01

Toxicity

The most effective and safe dose of laquinimod for patients with multiple sclerosis may be 0.5 mg.

ExcerptReferenceRelevance
" One serious adverse event (SAE) of perichondritis was reported, which was unrelated to laquinimod (0."( Safety and in vivo immune assessment of escalating doses of oral laquinimod in patients with RRMS.
Bar-Ilan, O; Hayardeny, L; Mimrod, D; Paul, F; Richter, N; Samara, E; Sehr, T; Sorani, E; Spiegelstein, O; Thomas, K; Tumani, H; Ziemssen, T, 2017
)
0.92
" Risk of adverse events: The risk of diarrhea, nausea, abdominal pain, and all adverse events did not significantly increase (p > 0."( The effects and side effects of laquinimod for the treatment of multiple sclerosis patients: a systematic review and meta-analysis of clinical trials.
Abbastabar, H; Bitarafan, S; Harirchian, MH; Mohammadpour, Z; Noureini, SK; Rouhi, F, 2020
)
0.84

Pharmacokinetics

The combination of COC and laquinimod treatment was found to be safe, tolerable, and devoid of any noticeable pharmacokinetic interaction. These results indicate that coadministration of laquimod with moderate to strong inhibitors of CYP3A or strong inducers of CYC3A may give rise to significant drug interactions.

ExcerptReferenceRelevance
" In conclusion, our developed methods were found to be selective, sensitive, robust and suitable for applications in clinical pharmacokinetic profiling."( Determination of the immunomodulator laquinimod in human plasma by liquid chromatography/tandem mass spectrometry; development, validation and application of two methods in clinical pharmacokinetic profiling.
Edman, K; Gunnarsson, PO; Hansson, G; Olin, M; Sennbro, CJ; Svensson, LD, 2006
)
0.61
" Blood samples for pharmacokinetic profiling of laquinimod, EE and LNG were collected on day 21 and day 22 of Cycles 1 and 3 pre-dose and multiple times post-dose."( The effect of laquinimod, a novel immuno-modulator in development to treat Huntington disease, on the pharmacokinetics of ethinylestradiol and levonorgestrel in healthy young women.
Bar-Ilan, O; Dror, V; Elgart, A; Korver, T; Mimrod, D; Spiegelstein, O; Zur, AA, 2019
)
1.13
"The combination of COC and laquinimod treatment was found to be safe, tolerable, and devoid of any noticeable pharmacokinetic interaction."( The effect of laquinimod, a novel immuno-modulator in development to treat Huntington disease, on the pharmacokinetics of ethinylestradiol and levonorgestrel in healthy young women.
Bar-Ilan, O; Dror, V; Elgart, A; Korver, T; Mimrod, D; Spiegelstein, O; Zur, AA, 2019
)
1.17
" These results indicate that coadministration of laquinimod with moderate to strong inhibitors of CYP3A or strong inducers of CYP3A may give rise to significant pharmacokinetic drug interactions."( The Effect of CYP3A Induction and Inhibition on the Pharmacokinetics of Laquinimod, a Novel Neuroimmunomodulator.
Elgart, A; Greenblatt, DJ; Loupe, PS; Mimrod, D; Spiegelstein, O; Weiss, S; Zur, AA, 2020
)
1.04

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

Laquinimod is an orally dosed immuno-modulator currently under development for Huntington's disease (HD) To determine the drug-drug interaction potential, interaction assessments were conducted in healthy volunteers.

ExcerptRelevanceReference
" Phase II studies in relapsing MS demonstrate a dose-response effect on disease activity, measured by number of active lesions on brain magnetic resonance imaging, and show favorable tolerability and safety based on clinical and laboratory indicators."( Oral laquinimod therapy in relapsing multiple sclerosis.
Preiningerova, J, 2009
)
0.87
" Phase II studies in RRMS demonstrate a dose-response effect on disease activity, measured by the number of active lesions on brain magnetic resonance imaging, and show favourable tolerability and safety based on clinical and laboratory indicators."( Oral laquinimod treatment in multiple sclerosis.
Fernández, O, 2011
)
0.88
" Further studies are necessary to evaluate both neuroprotective efficacy and optimal dosage of laquinimod in more detail."( Review of laquinimod and its therapeutic potential in multiple sclerosis.
Gold, R; Thöne, J, 2013
)
1.01
" New information about cardiovascular events is prompting the discontinuation of higher dosing regimens in both ongoing trials."( Laquinimod in the treatment of relapsing remitting multiple sclerosis.
Hainke, U; Thomas, K; Ziemssen, T, 2016
)
1.88
"Laquinimod is an orally dosed immuno-modulator currently under development for Huntington's disease (HD)."( The effect of laquinimod, a novel immuno-modulator in development to treat Huntington disease, on the pharmacokinetics of ethinylestradiol and levonorgestrel in healthy young women.
Bar-Ilan, O; Dror, V; Elgart, A; Korver, T; Mimrod, D; Spiegelstein, O; Zur, AA, 2019
)
2.32
" Due to its extremely low solubility in water, it was difficult to develop an injectable liquid dosage form."( Injected laquinimod D-α-tocopheryl polyethylene glycol-1000 succinate polymeric micelles for the treatment of inflammatory bowel disease.
Chen, R; Tong, M; Wang, L; Xu, H; Xue, P; Yang, W; Yao, Q; Yuan, J; Zhao, Y; ZhuGe, D, 2020
)
0.98
" To determine the drug-drug interaction potential of laquinimod with CYP3A inhibitors and inducers, interaction assessments were conducted in healthy volunteers using single-dose administration of laquinimod before and after multiple dosing of CYP3A inhibitors (ketoconazole, fluconazole, and cimetidine) or a CYP3A4 inducer (rifampin)."( The Effect of CYP3A Induction and Inhibition on the Pharmacokinetics of Laquinimod, a Novel Neuroimmunomodulator.
Elgart, A; Greenblatt, DJ; Loupe, PS; Mimrod, D; Spiegelstein, O; Weiss, S; Zur, AA, 2020
)
1.04
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic amideAn amide in which the amide linkage is bonded directly to an aromatic system.
[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]

Bioassays (34)

Assay IDTitleYearJournalArticle
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
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.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID115205Inhibition of acute experimental autoimmune encephalomyelitis in SJL/N mice by 5 mg/kg/day p.o./s.c.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.
AID115059Inhibition of acute experimental autoimmune encephalomyelitis in SJL/N mice by 0.2 mg/kg/day p.o./s.c.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.
AID1322039Immunosuppressive activity in human PMA/ionomycin stimulated Jurkat T cells assessed as suppression of IL2 production at 10 uM pretreated with cells followed by PMA/ionomycin stimulation measured after 13 hrs by ELISA2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Discovery and structure-activity relationship studies of quinolinone derivatives as potent IL-2 suppressive agents.
AID115068Inhibition of acute experimental autoimmune encephalomyelitis in SJL/N mice by 1 mg/kg/day p.o./s.c.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.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (130)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's18 (13.85)29.6817
2010's90 (69.23)24.3611
2020's22 (16.92)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 42.42

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 Index42.42 (24.57)
Research Supply Index4.98 (2.92)
Research Growth Index5.10 (4.65)
Search Engine Demand Index62.48 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (42.42)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials15 (11.54%)5.53%
Reviews42 (32.31%)6.00%
Case Studies1 (0.77%)4.05%
Observational0 (0.00%)0.25%
Other72 (55.38%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]