Page last updated: 2024-12-07

iguratimod

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Description

iguratimod: an immunosuppressive agent [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID124246
CHEMBL ID2107455
CHEBI ID31689
SCHEMBL ID26326
MeSH IDM0509070

Synonyms (64)

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

Research Excerpts

Overview

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.

ExcerptReferenceRelevance
"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. "( Iguratimod Restrains Circulating Follicular Helper T Cell Function by Inhibiting Glucose Metabolism
Bai, Z; Jin, M; Li, X; Liu, R; Lu, Z; Tang, Y; Wang, G; Ye, X, 2022
)
3.61
"Iguratimod (IGU) is a new drug that is used for controlling CTD."( Iguratimod ameliorates bleomycin-induced pulmonary fibrosis by inhibiting the EMT process and NLRP3 inflammasome activation.
Han, X; Li, Q; Liu, W; Sun, L; Wang, J, 2022
)
2.89
"Iguratimod is a synthesized anti-rheumatic disease-modifying drug, which shows drastic inhibition to EGR1 expression in B cells."( Iguratimod attenuated fibrosis in systemic sclerosis via targeting early growth response 1 expression.
Bao, C; Cao, S; Chen, X; Fan, C; Fu, Q; Jin, Y; Lu, L; Shen, L; Sun, L; Xu, X; Yan, Q; Yin, H; Zhan, Y; Zhang, Z, 2023
)
3.07
"Iguratimod (IGUR) is a novel disease-modifying antirheumatic drug used for treating rheumatoid arthritis (RA). "( In Situ Forming Injectable Hydrogel For Encapsulation Of Nanoiguratimod And Sustained Release Of Therapeutics.
Le, Y; Li, C; Liu, X; Ma, Z; Qi, S; Sun, L; Tao, C; Wang, J; Zhang, J; Zhao, J, 2019
)
2.2
"Iguratimod (IGU) is a novel small-molecule anti-rheumatic drug with remarkable effectiveness and good safety for the treatment of active rheumatoid arthritis. "( Molecular mechanisms and clinical application of Iguratimod: A review.
Gao, H; Jiang, H; Wang, M; Wang, Q; Wu, B, 2020
)
2.26
"Iguratimod (IGU) is a conventional synthetic disease-modifying drug that has been approved based on its additive effects with methotrexate (MTX) for the treatment of rheumatoid arthritis (RA). "( Clinical effectiveness of iguratimod based on real-world data of patients with rheumatoid arthritis.
Kodera, H; Mizutani, S; Nanki, T; Sato, Y; Yasuoka, H; Yoshida, S, 2021
)
2.36
"Iguratimod (IGU) is a novel small molecule anti-rheumatic drug with the effect of non-steroidal anti-inflammatory drug and disease-modifying anti-rheumatic drug. "( Molecular mechanisms and clinical studies of iguratimod for the treatment of ankylosing spondylitis.
Cui, Y; Liu, S; Zhang, X, 2021
)
2.32
"Iguratimod (IGU) is a novel anti-rheumatic drug that suppresses the secretion of inflammatory factors, but is also able to modulate the differentiation of multiple cells."( Anti-fibrotic effect of iguratimod on pulmonary fibrosis by inhibiting the fibroblast-to-myofibroblast transition.
Cui, Y; Dong, G; Lin, H; Wu, C; Xie, Y; Zhang, G; Zhang, X; Zhu, F, 2020
)
1.59
"Iguratimod (IGU) is a novel conventional synthetic disease-modifying anti-rheumatic drug developed in Japan."( Effects of iguratimod on glucocorticoid-induced disorder of bone metabolism in vitro.
Ebina, K; Etani, Y; Goshima, A; Hirao, M; Kanamoto, T; Miura, T; Miyama, A; Nakata, K; Okamura, G; Oyama, S; Takami, K; Yoshikawa, H, 2021
)
1.73
"Iguratimod is a new kind of synthetic small molecule disease modified anti-rheumatic drug with good efficacy for rheumatoid arthritis (RA) treatment; meanwhile, it exhibits potency to alleviate alveolar inflammation and pulmonary fibrosis. "( Iguratimod attenuates general disease activity and improves lung function in rheumatoid arthritis-associated interstitial lung disease patients.
Cai, XN; Lu, L; Ma, H; Shao, SQ; Shu, P; Yin, HQ; Yin, SL; Zhou, DM, 2021
)
3.51
"Iguratimod (IGU) is a new small molecular, anti-rheumatic drug and has shown the potential for drug repurposing from rheumatoid arthritis (RA) to LN treatment."( Comparison of iguratimod and conventional cyclophosphamide with sequential azathioprine as treatment of active lupus nephritis: study protocol for a multi-center, randomized, controlled clinical trial (iGeLU study).
Bao, C; Dai, M; Du, F; Huang, X; Jiang, G; Kang, Y; Li, Z; Tang, J; Wang, N; Wang, X; Xu, J; Xue, Q; Yan, Q; Ye, P; Zhang, X; Zhou, Y, 2021
)
1.7
"Iguratimod (IGU) is a novel disease-modifying anti-rheumatic drug (DMARD) in rheumatoid arthritis (RA). Like other DMARDs, IGU exhibited significant differences in effectiveness and safety."( Genetic predictors of efficacy and toxicity of iguratimod in patients with rheumatoid arthritis.
Cai, X; Dai, L; Guo, JP; Li, C; Li, X; Li, Y; Li, Z; Liu, D; Luo, L; Mu, R; Sun, E; Tao, Y; Wang, Y; Wei, W; Wu, L; Wu, M; Xiao, W; Ye, H; Zhang, M; Zhao, J; Zou, Y, 2018
)
2.18
"Iguratimod is a novel anti-rheumatic drug with the capability of anti-cytokines as report goes. "( Suspected drug-induced liver injury associated with iguratimod: a case report and review of the literature.
Hong, RT; Li, XL; Liu, XC; Shi, H; Song, YL, 2018
)
2.17
"Iguratimod (IGU) is a new synthetic disease-modifying antirheumatic drug intended to treat patients with rheumatoid arthritis (RA). "( Efficacy of the clinical use of iguratimod therapy in patients with rheumatoid arthritis.
Kobayashi, T; Okamura, K; Okura, C; Takagishi, K; Yonemoto, Y, 2015
)
2.14
"Iguratimod is a novel disease-modifying antirheumatic drug. "( In vitro inhibition of CYP2C9-mediated warfarin 7-hydroxylation by iguratimod: possible mechanism of iguratimod-warfarin interaction.
Matsuzawa, N; Ohmori, S; Sakuyama, K; Shiozawa, A; Takami, K; Yamaori, S, 2015
)
2.1
"Iguratimod is a novel anti-rheumatic drug which is reported to have the capability of anti-cytokines."( Anti-rheumatic drug iguratimod (T-614) alleviates cancer-induced bone destruction via down-regulating interleukin-6 production in a nuclear factor-κB-dependent manner.
Peng, G; Sun, Y; Wang, BY; Wu, YX; Ye, DW; Yu, SY; Zhang, P, 2016
)
1.48
"Iguratimod (T-614) is an anti-inflammatory agent which has been reported to show the inhibitory effect of bone destruction in RA."( T-614 Promotes Osteoblastic Cell Differentiation by Increasing Dlx5 Expression and Regulating the Activation of p38 and NF-
Chen, G; Cheng, W; He, D; Liu, H; Miao, Y; Niu, X; Song, J; Wang, F; Xi, Y; Yang, F; Zhu, Q, 2018
)
1.2

Effects

Iguratimod (T-614) has been confirmed as a highly efficacious and safe novel disease-modifying anti-rheumatic drug (DMARD) for rheumatoid arthritis therapy.

ExcerptReferenceRelevance
"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

Actions

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.

ExcerptReferenceRelevance
"Iguratimod may have lower C-reactive protein and erythrocyte sedimentation rate values."( Relative efficacy and safety of iguratimod monotherapy for the treatment of patients with rheumatoid arthritis: a systematic review and meta-analysis.
Shrestha, S; Yang, C; Zhang, J; Zhao, J, 2020
)
1.56
"Iguratimod group showed lower levels of CRP and ESR at W4, W12 and W24; as well as decreased DAS28 score, rheumatoid factor and anti-cyclic citrullinate peptide antibody levels at W12 and W24 compared to Control group."( Iguratimod attenuates general disease activity and improves lung function in rheumatoid arthritis-associated interstitial lung disease patients.
Cai, XN; Lu, L; Ma, H; Shao, SQ; Shu, P; Yin, HQ; Yin, SL; Zhou, DM, 2021
)
2.79
"Iguratimod may inhibit hepatocellular carcinogensis by inhibition of interleukin-8 production in a rat model."( Inhibitory Effect of Anti-rheumatic Drug Iguratimod for Hepatocellular Carcinogenesis by Inhibition of Serum Interleukin-8 Production.
Fujiwara, Y; Furukawa, K; Haruki, K; Ishii, Y; Iwase, R; Sakamoto, T; Shiba, H; Shirai, Y; Yanaga, K, 2016
)
2.14

Treatment

Iguratimod treatment increased miR-146a while decreased cell proliferation, IRAK1 and TRAF6/JNK1 pathway in RA-FLS in a dose-dependent manner.

ExcerptReferenceRelevance
"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

Toxicity

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.

ExcerptReferenceRelevance
" No statistically significant difference was noted in the incidence of adverse reactions between iguratimod and salazosulfapyridine."( Efficacy and safety of iguratimod compared with placebo and salazosulfapyridine in active rheumatoid arthritis: a controlled, multicenter, double-blind, parallel-group study.
Abe, T; Hara, M; Hashimoto, H; Hoshi, K; Irimajiri, S; Matsui, N; Mizushima, Y; Nakano, S; Nobunaga, M; Sugawara, S; Yoshino, S, 2007
)
0.87
" The cumulative incidence of adverse events for 100 weeks was 97."( Long-term safety study of iguratimod in patients with rheumatoid arthritis.
Abe, T; Hara, M; Hashimoto, H; Hoshi, K; Irimajiri, S; Matsui, N; Mizushima, Y; Nobunaga, M; Sugawara, S; Yoshino, S, 2007
)
0.64
" The incidence of adverse events (AEs) was not significantly higher with T-614 than with placebo, but upper abdominal discomfort, leucopenia, elevated serum alanine aminotransferase (sALT), skin rash and/or pruritus were more common in the 50 mg and 25 mg dosage groups."( Safety and efficacy of T-614 in the treatment of patients with active rheumatoid arthritis: a double blind, randomized, placebo-controlled and multicenter trial.
Bao, CD; Han, XH; Li, XF; Lü, LJ; Sun, LY; Teng, JL; Wu, HX; Xu, JH, 2008
)
0.35
" Frequent adverse events for 52 weeks in the iguratimod + MTX group were nasopharyngitis, upper respiratory tract inflammation, stomatitis, lymphocyte decrease, AST increase, ALT increase and blood iron decrease."( Safety and efficacy of combination therapy of iguratimod with methotrexate for patients with active rheumatoid arthritis with an inadequate response to methotrexate: an open-label extension of a randomized, double-blind, placebo-controlled trial.
Hara, M; Ishiguro, N; Katayama, K; Kondo, M; Mimori, T; Nagai, K; Soen, S; Sumida, T; Yamaguchi, T; Yamamoto, K, 2014
)
0.92
" Iguratimod for RA had few adverse events, and its efficacy and safety were the same as those of MTX and SASP for RA."( Efficacy and safety of iguratimod for the treatment of rheumatoid arthritis.
Chen, S; Li, J; Liang, Y; Lu, Y; Mao, H; Shi, G; Yang, N, 2013
)
1.61
" Clinical features at baseline and efficacy endpoints of the ACR 20 % response (ACR20), ACR50, ACR70, and adverse events at 24 weeks were evaluated, respectively."( Efficacy and safety evaluation of a combination of iguratimod and methotrexate therapy for active rheumatoid arthritis patients: a randomized controlled trial.
Duan, XW; Mao, SY; Shang, JJ; Shi, XD; Zhang, XL, 2015
)
0.67
" All adverse events (AEs) and adverse drug reactions (ADRs) were collected."( Safety and effectiveness of 24-week treatment with iguratimod, a new oral disease-modifying antirheumatic drug, for patients with rheumatoid arthritis: interim analysis of a post-marketing surveillance study of 2679 patients in Japan.
Atsumi, T; Fujii, T; Harigai, M; Ikeuchi, S; Koike, T; Kushimoto, S; Kuwana, M; Matsuno, H; Mimori, T; Momohara, S; Takasaki, Y; Takei, S; Tamura, N, 2017
)
0.71
" We evaluated adverse events (AEs); adverse drug reactions (ADRs); ADRs of special interest, including liver and renal dysfunctions, interstitial lung disease, gastrointestinal and blood disorders, and infection; and change in Disease Activity Score 28-C-reactive protein (DAS28-CRP) at week 52."( Safety and effectiveness of iguratimod in patients with rheumatoid arthritis: Final report of a 52-week, multicenter postmarketing surveillance study.
Atsumi, T; Fujii, T; Harigai, M; Ikeuchi, S; Koike, T; Kushimoto, S; Kuwana, M; Matsuno, H; Mimori, T; Momohara, S; Takasaki, Y; Takei, S; Tamura, N; Yamamoto, K, 2019
)
0.81
" Follow-up indexes included IgG4-RD responder index (IgG4-RD RI), serology and imaging, plasma cytokines and adverse drug effect."( Efficacy and safety of iguratimod plus corticosteroid as bridge therapy in treating mild IgG4-related diseases: A prospective clinical trial.
Chen, H; Fei, Y; Gong, Y; Li, J; Li, Y; Lin, W; Liu, X; Liu, Y; Liu, Z; Peng, L; Shen, M; Shi, Q; Wang, M; Zeng, X; Zhang, F; Zhang, P; Zhang, W; Zhang, X; Zhao, Y; Zhou, J, 2019
)
0.82
" Clinical manifestation, IgG4-RD responder index (IgG-RD RI), serological indexes, gland ultrasound findings, and adverse drug effect were recorded."( Efficacy and safety of iguratimod on patients with relapsed or refractory IgG4-related disease.
Bian, W; Chen, D; Chen, J; Fu, J; Li, Y; Li, Z; Liu, Y; Sun, X; Zhang, W; Zhang, Y; Zhao, X, 2020
)
0.87
" Although iguratimod had superior efficacy than placebo, the incidence of adverse events was also higher."( Relative efficacy and safety of iguratimod monotherapy for the treatment of patients with rheumatoid arthritis: a systematic review and meta-analysis.
Shrestha, S; Yang, C; Zhang, J; Zhao, J, 2020
)
1.24
"• Patients on iguratimod may have similar treatment response, functional ability, disease state, and adverse event profile at 24 weeks compared with those on methotrexate."( Relative efficacy and safety of iguratimod monotherapy for the treatment of patients with rheumatoid arthritis: a systematic review and meta-analysis.
Shrestha, S; Yang, C; Zhang, J; Zhao, J, 2020
)
1.2
" The results of the meta-analysis demonstrated that there was no statistical significance in adverse events (1."( 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
)
0.93
" We investigated the frequency of adverse drug reactions before and after implementation of each safety measure to examine the preventive effect of these measures."( Effectiveness of drug safety measures for reducing the incidence of adverse drug reactions: Post-hoc analysis of data from all-case surveillance of iguratimod using generalized estimating equations.
Ikeuchi, S; Ishii, M; Shibata, K; Yoshimura, A, 2021
)
0.82
"IGU may be an effective and safe intervention for AS."( Efficacy and safety of Iguratimod in the treatment of Ankylosing Spondylitis: A systematic review and meta-analysis of randomized controlled trials.
Chen, H; Deng, Y; Fan, J; Hao, W; He, Q; Long, Z; Yang, K; Zeng, L, 2023
)
1.22
"IGU (IGU), a novel immunomodulatory agent for rheumatoid arthritis, has been shown to be effective and safe as monotherapy in a small population with refractory lupus nephritis (LN)."( Efficacy and safety of Iguratimod as an add-on therapy for refractory lupus nephritis: A preliminary investigational study.
Bao, C; Dai, M; Du, F; Kang, Y; Li, Q; Liu, B; Yan, Q; Ye, P; Zhang, M, 2023
)
1.22
" Three mild to moderate adverse events were recorded."( Efficacy and safety of Iguratimod as an add-on therapy for refractory lupus nephritis: A preliminary investigational study.
Bao, C; Dai, M; Du, F; Kang, Y; Li, Q; Liu, B; Yan, Q; Ye, P; Zhang, M, 2023
)
1.22
" In terms of safety endpoints, the total adverse event rates (AEs), leucopenia, gastrointestinal (GI) AEs, skin diseases, and liver dysfunction of the "IGU+MP" group and the "HCQ+MP" group were comparable."( 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 does not increase the risk of adverse events, which means that IGU combined with MP may be a safe and effective strategy for the treatment of pSS and has value for further research exploration."( 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

Pharmacokinetics

ExcerptReferenceRelevance
" 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

Compound-Compound Interactions

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.

ExcerptReferenceRelevance
" 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

Bioavailability

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.

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
" To improve its bioavailability and to alleviate gastrointestinal side effects, we changed the formulation into nanoiguratimod-loaded hydrogel (NanoIGUR-loaded hydrogel) composites for sustained release of therapeutics."( In Situ Forming Injectable Hydrogel For Encapsulation Of Nanoiguratimod And Sustained Release Of Therapeutics.
Le, Y; Li, C; Liu, X; Ma, Z; Qi, S; Sun, L; Tao, C; Wang, J; Zhang, J; Zhao, J, 2019
)
0.96
" The pharmacokinetic parameters showed better bioavailability and longer half-life time with NanoIGUR-loaded hydrogel by subcutaneous administration than oral raw iguratimod."( In Situ Forming Injectable Hydrogel For Encapsulation Of Nanoiguratimod And Sustained Release Of Therapeutics.
Le, Y; Li, C; Liu, X; Ma, Z; Qi, S; Sun, L; Tao, C; Wang, J; Zhang, J; Zhao, J, 2019
)
0.95

Dosage Studied

ExcerptRelevanceReference
" Methotrexate and indomethacin did not exert any preferable effects in a therapeutic dosing schedule."( Effect of iguratimod and other anti-rheumatic drugs on adenocarcinoma colon 26-induced cachexia in mice.
Matsunaga, T; Mikami, M; Ogasawara, M; Suzuki, H; Tanaka, K; Terashima, N; Urata, N, 2007
)
0.74
" After 24 weeks, the 25 mg/d and 50 mg/d dosage groups and the placebo group showed 39."( Safety and efficacy of T-614 in the treatment of patients with active rheumatoid arthritis: a double blind, randomized, placebo-controlled and multicenter trial.
Bao, CD; Han, XH; Li, XF; Lü, LJ; Sun, LY; Teng, JL; Wu, HX; Xu, JH, 2008
)
0.35
" Eighty-six RA patients were assigned into 3 treatment groups randomly: T-614 group 1 (T-614 for the first 4 weeks with an oral dosage of 25mg once daily, and 50mg/day for the subsequent 20 weeks with an oral dosage of 25mg twice daily), T-614 group 2 (T-614 with an oral dosage of 25mg twice daily), or the MTX group (MTX 10 mg/week orally for the first 4 weeks and 15 mg/week for the subsequent 20 weeks)."( T-614 alters the production of matrix metalloproteinases (MMP-1 andMMP-3) and inhibits the migratory expansion of rheumatoid synovial fibroblasts, in vitro.
Bao, CD; Du, F; Lü, LJ; Shen, N; Teng, JL; Ye, P, 2012
)
0.38
" MTX at dosage of 6 or 8 mg/week was administered to patients in both groups."( Concomitant iguratimod therapy in patients with active rheumatoid arthritis despite stable doses of methotrexate: a randomized, double-blind, placebo-controlled trial.
Hara, M; Ishiguro, N; Katayama, K; Kondo, M; Mimori, T; Nagai, K; Soen, S; Sumida, T; Yamaguchi, T; Yamamoto, K, 2013
)
0.77
" The dosage of iguratimod used in this study showed no significant cytotoxic effects in vivo and no overt side-effects were observed."( Prevention of immune nephritis by the small molecular weight immunomodulator iguratimod in MRL/lpr mice.
Bao, C; Chen, S; Dai, D; Du, F; Fu, Q; Huang, X; Yan, Q, 2014
)
0.98
" T-614 was orally administered at a dosage of 50 mg/day (25 mg twice daily) for 24 weeks."( Efficacy and safety evaluation of a combination of iguratimod and methotrexate therapy for active rheumatoid arthritis patients: a randomized controlled trial.
Duan, XW; Mao, SY; Shang, JJ; Shi, XD; Zhang, XL, 2015
)
0.67
" The median prednisone dosage was 10 mg/d (IQR 0-10 mg/day)."( Iguratimod as an alternative induction therapy for refractory lupus nephritis: a preliminary investigational study.
Bao, C; Dai, M; Dai, Q; Du, F; Fu, Q; Kang, Y; Lu, L; Wang, R; Wu, C; Yan, Q; Ye, P, 2020
)
2
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
organic molecular entityAny 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 Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AR proteinHomo sapiens (human)Potency17.18340.000221.22318,912.5098AID743036; AID743042; AID743054; AID743063
estrogen nuclear receptor alphaHomo sapiens (human)Potency10.10140.000229.305416,493.5996AID743069; AID743075
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency35.48130.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Macrophage migration inhibitory factorHomo sapiens (human)IC50 (µMol)6.81000.03803.09109.8000AID1384609
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (35)

Processvia Protein(s)Taxonomy
prostaglandin biosynthetic processMacrophage migration inhibitory factorHomo sapiens (human)
positive regulation of cytokine productionMacrophage migration inhibitory factorHomo sapiens (human)
negative regulation of mature B cell apoptotic processMacrophage migration inhibitory factorHomo sapiens (human)
inflammatory responseMacrophage migration inhibitory factorHomo sapiens (human)
cell surface receptor signaling pathwayMacrophage migration inhibitory factorHomo sapiens (human)
positive regulation of cell population proliferationMacrophage migration inhibitory factorHomo sapiens (human)
negative regulation of gene expressionMacrophage migration inhibitory factorHomo sapiens (human)
positive regulation of protein kinase A signalingMacrophage migration inhibitory factorHomo sapiens (human)
negative regulation of macrophage chemotaxisMacrophage migration inhibitory factorHomo sapiens (human)
carboxylic acid metabolic processMacrophage migration inhibitory factorHomo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorMacrophage migration inhibitory factorHomo sapiens (human)
negative regulation of cell migrationMacrophage migration inhibitory factorHomo sapiens (human)
positive regulation of B cell proliferationMacrophage migration inhibitory factorHomo sapiens (human)
positive regulation of lipopolysaccharide-mediated signaling pathwayMacrophage migration inhibitory factorHomo sapiens (human)
positive regulation of tumor necrosis factor productionMacrophage migration inhibitory factorHomo sapiens (human)
negative regulation of myeloid cell apoptotic processMacrophage migration inhibitory factorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationMacrophage migration inhibitory factorHomo sapiens (human)
positive regulation of phosphorylationMacrophage migration inhibitory factorHomo sapiens (human)
regulation of macrophage activationMacrophage migration inhibitory factorHomo sapiens (human)
negative regulation of apoptotic processMacrophage migration inhibitory factorHomo sapiens (human)
negative regulation of DNA damage response, signal transduction by p53 class mediatorMacrophage migration inhibitory factorHomo sapiens (human)
innate immune responseMacrophage migration inhibitory factorHomo sapiens (human)
positive regulation of fibroblast proliferationMacrophage migration inhibitory factorHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationMacrophage migration inhibitory factorHomo sapiens (human)
positive chemotaxisMacrophage migration inhibitory factorHomo sapiens (human)
negative regulation of protein metabolic processMacrophage migration inhibitory factorHomo sapiens (human)
positive regulation of prostaglandin secretion involved in immune responseMacrophage migration inhibitory factorHomo sapiens (human)
positive regulation of myeloid leukocyte cytokine production involved in immune responseMacrophage migration inhibitory factorHomo sapiens (human)
protein homotrimerizationMacrophage migration inhibitory factorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeMacrophage migration inhibitory factorHomo sapiens (human)
positive regulation of arachidonic acid secretionMacrophage migration inhibitory factorHomo sapiens (human)
cellular senescenceMacrophage migration inhibitory factorHomo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorMacrophage migration inhibitory factorHomo sapiens (human)
positive regulation of chemokine (C-X-C motif) ligand 2 productionMacrophage migration inhibitory factorHomo sapiens (human)
negative regulation of cellular senescenceMacrophage migration inhibitory factorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
protease bindingMacrophage migration inhibitory factorHomo sapiens (human)
dopachrome isomerase activityMacrophage migration inhibitory factorHomo sapiens (human)
cytokine activityMacrophage migration inhibitory factorHomo sapiens (human)
cytokine receptor bindingMacrophage migration inhibitory factorHomo sapiens (human)
protein bindingMacrophage migration inhibitory factorHomo sapiens (human)
chemoattractant activityMacrophage migration inhibitory factorHomo sapiens (human)
identical protein bindingMacrophage migration inhibitory factorHomo sapiens (human)
phenylpyruvate tautomerase activityMacrophage migration inhibitory factorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
extracellular regionMacrophage migration inhibitory factorHomo sapiens (human)
extracellular spaceMacrophage migration inhibitory factorHomo sapiens (human)
nucleoplasmMacrophage migration inhibitory factorHomo sapiens (human)
cytoplasmMacrophage migration inhibitory factorHomo sapiens (human)
cytosolMacrophage migration inhibitory factorHomo sapiens (human)
plasma membraneMacrophage migration inhibitory factorHomo sapiens (human)
cell surfaceMacrophage migration inhibitory factorHomo sapiens (human)
vesicleMacrophage migration inhibitory factorHomo sapiens (human)
secretory granule lumenMacrophage migration inhibitory factorHomo sapiens (human)
extracellular exosomeMacrophage migration inhibitory factorHomo sapiens (human)
ficolin-1-rich granule lumenMacrophage migration inhibitory factorHomo sapiens (human)
extracellular spaceMacrophage migration inhibitory factorHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (6)

Assay IDTitleYearJournalArticle
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
AID1384609Inhibition of recombinant human MIF tautomerase activity using L-dopachrome methyl ester as substrate measured for 20 secs2018Journal 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]

Research

Studies (133)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's7 (5.26)18.2507
2000's16 (12.03)29.6817
2010's52 (39.10)24.3611
2020's58 (43.61)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 67.66

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.

MetricThis Compound (vs All)
Research Demand Index67.66 (24.57)
Research Supply Index5.04 (2.92)
Research Growth Index5.31 (4.65)
Search Engine Demand Index113.07 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (67.66)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials19 (14.18%)5.53%
Reviews18 (13.43%)6.00%
Case Studies7 (5.22%)4.05%
Observational5 (3.73%)0.25%
Other85 (63.43%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]