ID Source | ID |
---|---|
PubMed CID | 54677946 |
CHEMBL ID | 66092 |
CHEBI ID | 134738 |
SCHEMBL ID | 39441 |
SCHEMBL ID | 39440 |
MeSH ID | M0452523 |
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 |
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.
Excerpt | Reference | Relevance |
---|---|---|
"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 |
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.
The most effective and safe dose of laquinimod for patients with multiple sclerosis may be 0.5 mg.
Excerpt | Reference | Relevance |
---|---|---|
" 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 |
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.
Excerpt | Reference | Relevance |
---|---|---|
"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 |
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.
Excerpt | Relevance | Reference |
---|---|---|
" 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 |
Class | Description |
---|---|
aromatic amide | An 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] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID115205 | Inhibition of acute experimental autoimmune encephalomyelitis in SJL/N mice by 5 mg/kg/day p.o./s.c. | 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. |
AID115059 | Inhibition of acute experimental autoimmune encephalomyelitis in SJL/N mice by 0.2 mg/kg/day p.o./s.c. | 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. |
AID1322039 | Immunosuppressive 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 ELISA | 2016 | Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21 | Discovery and structure-activity relationship studies of quinolinone derivatives as potent IL-2 suppressive agents. |
AID115068 | Inhibition of acute experimental autoimmune encephalomyelitis in SJL/N mice by 1 mg/kg/day p.o./s.c. | 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. |
AID1347411 | qHTS 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) Libary | 2020 | ACS 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] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 18 (13.85) | 29.6817 |
2010's | 90 (69.23) | 24.3611 |
2020's | 22 (16.92) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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.
| This Compound (42.42) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 15 (11.54%) | 5.53% |
Reviews | 42 (32.31%) | 6.00% |
Case Studies | 1 (0.77%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 72 (55.38%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |