iguratimod: an immunosuppressive agent
ID Source | ID |
---|---|
PubMed CID | 124246 |
CHEMBL ID | 2107455 |
CHEBI ID | 31689 |
SCHEMBL ID | 26326 |
MeSH ID | M0509070 |
Synonym |
---|
HY-17009 |
careram |
kolbet |
iremod |
t-614 |
colvet |
iguratimod |
NCGC00181783-01 |
D01146 |
123663-49-0 |
iguratimod (jan/inn) |
n-[7-(methanesulfonamido)-4-oxo-6-phenoxychromen-3-yl]formamide |
FT-0654508 |
n-[7-(methanesulfonamido)-4-oxo-6-phenoxy-chromen-3-yl]formamide;iguratimod |
A805134 |
NCGC00181783-02 |
3-formylamino-7-methylsulfonylamino-6-phenoxy-4h-1-benzopyran-4-one |
t 614 |
cas-123663-49-0 |
tox21_113422 |
dtxcid3028897 |
dtxsid0048971 , |
n-(7-(methylsulfonamido)-4-oxo-6-phenoxy-4h-chromen-3-yl)formamide |
c17h14n2o6s |
iguratimod [inn] |
n-(7-((methylsulfonyl)amino)-4-oxo-6-phenoxy-4h-1-benzopyran-3-yl)formamide |
4ihy34y2nv , |
unii-4ihy34y2nv |
CS-0617 |
AKOS015888743 |
CHEMBL2107455 |
S5648 |
iguratimod [who-dd] |
iguratimod [mi] |
iguratimod [jan] |
SCHEMBL26326 |
ANMATWQYLIFGOK-UHFFFAOYSA-N |
I0945 |
n-[7-(methanesulfonamido)-4-oxo-6-phenoxy-4h-chromen-3-yl]formamide |
n-(3-formamido-4-oxo-6-phenoxy-4h-chromen-7-yl)methanesulfonamide |
J-521483 |
mfcd00882374 |
sr-01000945251 |
SR-01000945251-1 |
CHEBI:31689 |
t614 |
gtpl9736 |
n-[7-methanesulfonamido-4-oxo-6-(phenoxy)chromen-3-yl]formamide |
iguratimod, >=98% (hplc) |
DB12233 |
BCP04206 |
AS-12959 |
Q13575264 |
SB16814 |
CCG-268349 |
NCGC00181783-03 |
C71931 |
bdbm50458537 |
EN300-24433520 |
n-(7-methanesulfonamido-4-oxo-6-phenoxy-4h-chromen-3-yl)formamide |
BI164569 |
iguratimod- bio-x |
Z2681891323 |
lguratimod |
Iguratimod (IGU) is a novel disease modified anti-rheumatic drug, which has been found to act directly on B cells for inhibiting the production of antibodies in rheumatoid arthritis (RA) patients. Iguatimod is a conventional synthetic disease-modifying drug that has been approved based on its additive effects with methotrexate.
Iguratimod (T-614) has been confirmed as a highly efficacious and safe novel disease-modifying anti-rheumatic drug (DMARD) for rheumatoid arthritis therapy.
Excerpt | Reference | Relevance |
---|---|---|
"Iguratimod has been shown to promote bone formation and inhibit bone resorption in rheumatoid arthritis patients. " | ( Efficacy of iguratimod on mineral and bone disorders after kidney transplantation: a preliminary study. Chen, H; Fei, S; Gu, M; Han, Z; Huang, Z; Ju, X; Sun, L; Suo, C; Tan, R; Tao, J; Wang, Z, 2023) | 2.73 |
"Iguratimod (T-614) has been confirmed as a highly efficacious and safe novel disease-modifying anti-rheumatic drug (DMARD) for rheumatoid arthritis therapy in China and Japan due to its potent anti-inflammation effect. " | ( Iguratimod (T-614) suppresses RANKL-induced osteoclast differentiation and migration in RAW264.7 cells via NF-κB and MAPK pathways. Feng, X; Gan, K; Tan, W; Wang, F; Xu, L; Yang, L; Zhang, M; Zhang, Q, 2016) | 3.32 |
Iguratimod group showed lower levels of CRP and ESR at W4, W12 and W24. decreased DAS28 score, rheumatoid factor and anti-cyclic citrullinate peptide antibody levels.
Iguratimod treatment increased miR-146a while decreased cell proliferation, IRAK1 and TRAF6/JNK1 pathway in RA-FLS in a dose-dependent manner.
Excerpt | Reference | Relevance |
---|---|---|
"Iguratimod treatment significantly reduced the proliferation, migration, and invasive capacities of RA-FLSs in a dose-dependent manner " | ( Iguratimod Inhibits the Aggressiveness of Rheumatoid Fibroblast-Like Synoviocytes. Cao, H; Chen, W; Ke, Y; Lin, J; Olsen, N; Sun, C; Wang, X; Xu, B; Xu, D; Xu, G; Xu, L; Yu, Y; Yue, L, 2019) | 3.4 |
"Iguratimod treatment increased miR-146a while decreased cell proliferation, IRAK1 and TRAF6/JNK1 pathway in RA-FLS in a dose-dependent manner. " | ( Iguratimod ameliorates rheumatoid arthritis progression through regulating miR-146a mediated IRAK1 expression and TRAF6/JNK1 pathway: an in vivo and in vitro study. Gao, J; Ji, L; Kong, R; Peng, Y; Zhang, J; Zhao, D, ) | 3.02 |
Iguratimod may have similar treatment response, functional ability, disease state, and adverse event profile at 24 weeks compared with those on methotrexate. Frequent adverse events for 52 weeks were nasopharyngitis, upper respiratory tract inflammation, stomatitis, lymphocyte decrease, AST increase, ALT increase and blood iron decrease.
Excerpt | Reference | Relevance |
---|---|---|
" On the other hand, the pharmacokinetic parameters of WF including maximum plasma concentration (Cmax) and area under the plasma concentration-time curve from 0 to 24 h (AUC0-24 h) were not affected by the combination with IGU." | ( Pharmacokinetic and Pharmacodynamic Analyses of Drug-Drug Interactions between Iguratimod and Warfarin. Hasegawa, K; Onoda, M; Tanaka, K; Yamamoto, T, 2016) | 0.66 |
This study was designed to explore the clinical efficacy of methotrexate combined with iguratimod on patients with rheumatoid arthritis (RA) and its influence on the expression levels of HOTAIR in serum. A total of 268 RA patients were selected as research objects.
Excerpt | Reference | Relevance |
---|---|---|
" Iguratimod (alone or in combination with MTX) is an emerging option for the treatment of DMARD-experienced adult patients with active RA who have had an inadequate response to or are intolerant of other DMARDs." | ( Iguratimod in combination with methotrexate in active rheumatoid arthritis : Therapeutic effects. Hou, N; Li, X; Liu, H; Lyu, J; Song, L; Xia, Z, 2016) | 2.79 |
"The current systematic review and meta-analysis aims to evaluate the efficacy and safety of iguratimod (IGU) combined with methotrexate (MTX) versus MTX alone in rheumatoid arthritis (RA)." | ( Efficacy and safety of iguratimod combined with methotrexate vs. methotrexate alone in rheumatoid arthritis : A systematic review and meta-analysis of randomized controlled trials. Chen, LJ; Li, JY; Tian, F; Wen, ZH; Zhou, YJ, 2021) | 1.15 |
"In this study, we aimed to explore the effects of iguratimod (IGU) combined with methotrexate (MTX) and hydroxychloroquine (HCQ) on bone mineral density (BMD) in patients with rheumatoid arthritis (RA)." | ( The effects of iguratimod combined with methotrexate and hydroxychloroquine on bone mineral density in patients with rheumatoid arthritis. Ma, RR; Wu, F; Wu, TJ; Ying, ZH; Yu, JJ; Zhang, Y, 2021) | 1.23 |
"This study was designed to explore the clinical efficacy of methotrexate combined with iguratimod on patients with rheumatoid arthritis (RA) and its influence on the expression levels of HOTAIR in serum." | ( Clinical Efficacy of Methotrexate Combined with Iguratimod on Patients with Rheumatoid Arthritis and Its Influence on the Expression Levels of HOTAIR in Serum. Dan, J; Liu, Y; Tan, J, 2021) | 1.1 |
"A total of 268 RA patients were selected as research objects, 145 patients received methotrexate alone were used as a control group (CG), 123 patients received methotrexate combined with iguratimod were taken as a research group (RG), and serum of 60 healthy people undergoing physical examination was selected as a healthy control group (HCG)." | ( Clinical Efficacy of Methotrexate Combined with Iguratimod on Patients with Rheumatoid Arthritis and Its Influence on the Expression Levels of HOTAIR in Serum. Dan, J; Liu, Y; Tan, J, 2021) | 1.07 |
"Clinical studies of IGU combined with MP for pSS were searched through eight databases." | ( Efficacy and safety of iguratimod combined with methylprednisolone for primary Sjögren's syndrome: a meta-analysis and trial sequential analysis. Hu, G; Xu, Q; Yang, XY; Yin, S; You, H; Yu, YF, 2023) | 1.22 |
"IGU combined with MP effectively attenuates autoimmune responses (IgG, IgM, IgA), reduces clinical symptoms and disease activity (ESR, PLT, ESSPRI, ESSDAI), and improves the exocrine gland functional status (SIT) in patients with pSS." | ( Efficacy and safety of iguratimod combined with methylprednisolone for primary Sjögren's syndrome: a meta-analysis and trial sequential analysis. Hu, G; Xu, Q; Yang, XY; Yin, S; You, H; Yu, YF, 2023) | 1.22 |
NanoIGUR-loaded hydrogel composites for sustained release of therapeutics. The pharmacokinetic parameters showed better bioavailability and longer half-life time with NanoIGur-loaded Hydrogel by subcutaneous administration.
Class | Description |
---|---|
organic molecular entity | Any molecular entity that contains carbon. |
[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] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
AR protein | Homo sapiens (human) | Potency | 17.1834 | 0.0002 | 21.2231 | 8,912.5098 | AID743036; AID743042; AID743054; AID743063 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 10.1014 | 0.0002 | 29.3054 | 16,493.5996 | AID743069; AID743075 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 35.4813 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Macrophage migration inhibitory factor | Homo sapiens (human) | IC50 (µMol) | 6.8100 | 0.0380 | 3.0910 | 9.8000 | AID1384609 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Process | via Protein(s) | Taxonomy |
---|---|---|
protease binding | Macrophage migration inhibitory factor | Homo sapiens (human) |
dopachrome isomerase activity | Macrophage migration inhibitory factor | Homo sapiens (human) |
cytokine activity | Macrophage migration inhibitory factor | Homo sapiens (human) |
cytokine receptor binding | Macrophage migration inhibitory factor | Homo sapiens (human) |
protein binding | Macrophage migration inhibitory factor | Homo sapiens (human) |
chemoattractant activity | Macrophage migration inhibitory factor | Homo sapiens (human) |
identical protein binding | Macrophage migration inhibitory factor | Homo sapiens (human) |
phenylpyruvate tautomerase activity | Macrophage migration inhibitory factor | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
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. |
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. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
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. |
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. |
AID1384609 | Inhibition of recombinant human MIF tautomerase activity using L-dopachrome methyl ester as substrate measured for 20 secs | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Advances and Insights for Small Molecule Inhibition of Macrophage Migration Inhibitory Factor. |
[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 | 7 (5.26) | 18.2507 |
2000's | 16 (12.03) | 29.6817 |
2010's | 52 (39.10) | 24.3611 |
2020's | 58 (43.61) | 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 very strong demand-to-supply ratio for research on this compound.
| This Compound (67.66) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 19 (14.18%) | 5.53% |
Reviews | 18 (13.43%) | 6.00% |
Case Studies | 7 (5.22%) | 4.05% |
Observational | 5 (3.73%) | 0.25% |
Other | 85 (63.43%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |