| Drug ID: | Drug64 |
|---|---|
| Drug Name: | Methotrexate |
| CID: | 126941 |
| DrugBank ID: | DB00563 |
| Modality: | Small Molecule |
| Groups: | approved |
| US Approved: | YES |
| Other Approved: | YES |
| Identifier: | NCT00035074, , NCT02413047, , NCT01393405, , NCT00498589 |
| Molecular Formula: | C20H22N8O5 |
| Molecular Weight: | 454.4 g/mol |
| Isomeric SMILES: | CN(CC1=CN=C2C(=N1)C(=NC(=N2)N)N)C3=CC=C(C=C3)C(=O)N[C@@H](CCC(=O)O)C(=O)O |
| Synonyms: | methotrexate; 59-05-2; Rheumatrex; Amethopterin; Methylaminopterin; Metatrexan; Hdmtx; Ledertrexate; Methylaminopterinum; MTX |
| Phase 0: | 18 |
| Phase 1: | 204 |
| Phase 2: | 717 |
| Phase 3: | 465 |
| Phase 4: | 225 |
| Description: | An antineoplastic antimetabolite with immunosuppressant properties. It is an inhibitor of tetrahydrofolate dehydrogenase and prevents the formation of tetrahydrofolate, necessary for synthesis of thymidylate, an essential component of DNA. [PubChem] |
Molecular Structure
Knowledge Graph
| dtID | CID | Compound Name | Gene ID | Gene Name | Species | PubMed IDs | Action |
|---|---|---|---|---|---|---|---|
| dt570 | 126941 | Methotrexate | 3417 | IDH1 | Homo sapiens (human) | None | |
| dt571 | 126941 | Methotrexate | 1014 | CDH16 | Homo sapiens (human) | Inhibitor | |
| dt572 | 126941 | Methotrexate | 10919 | EHMT2 | Homo sapiens (human) | None | |
| dt573 | 126941 | Methotrexate | 5423 | POLB | Homo sapiens (human) | None | |
| dt574 | 126941 | Methotrexate | 93777387 | folA | Escherichia coli K-12 | 16873019 | None |
| dt575 | 126941 | Methotrexate | 1719 | DHFR | Homo sapiens (human) | 12872145 | DHFR protein polymorphism results in decreased susceptibility to folic acid antagonists |
| dt576 | 126941 | Methotrexate | 2940 | GSTA3 | Rattus norvegicus (Norway rat) | 12872145 | GSTA3 protein results in decreased susceptibility to folic acid antagonists |
| dt577 | 126941 | Methotrexate | 23435 | TARDBP | Homo sapiens (human) | None | |
| dt578 | 126941 | Methotrexate | 4780 | NFE2L2 | Homo sapiens (human) | None |
- No data available
Phase Distribution
Phase Description
- Phase 0: Exploratory trials to assess drug behavior in humans
- Phase 1: Safety trials to determine safe dosage range
- Phase 2: Efficacy trials to evaluate therapeutic effects
- Phase 3: Large-scale trials to confirm efficacy and safety
- Phase 4: Post-marketing surveillance for long-term safety and efficacy
| Trial ID | Title | Phase | Status | Sponsor | Indications | Interventions | |
|---|---|---|---|---|---|---|---|
| NCT00498589 | Comparison of Methotrexate vs Placebo in Corticosteroid-dependent Ulcerative Colitis | PHASE2 | COMPLETED | Centre Hospitalier Universitaire de Besancon | Ulcerative Colitis | DRUG: methotrexate|DRUG: placebo | Details |
| NCT01393405 | Methotrexate in Induction and Maintenance of Steroid Free Remission in Ulcerative Colitis | PHASE2 | COMPLETED | University of North Carolina, Chapel Hill | Ulcerative Colitis | DRUG: Methotrexate | Details |
| NCT04205734 | Methotrexate Polyglutamate Measurements in Patients With Inflammatory Bowel Disease | None | SUSPENDED | Boston Children's Hospital | IBD | DIAGNOSTIC_TEST: MTX Assessment | Details |
| NCT04196920 | Methotrexate-associated Anti-TNF Combination Therapy, the Neglected One ! | None | UNKNOWN | University Hospital, Montpellier | Chronic Inflammatory Bowel Disease | None | Details |
| NCT00035074 | A Pharmacokinetic Study to Determine the Oral Bioavailability of Methotrexate in Patients With Inflammatory Bowel Disease | None | COMPLETED | National Center for Research Resources (NCRR) | Inflammatory Bowel Disease | DRUG: Methotrexate | Details |
| NL-OMON48064 | Methotrexate to suppress immunogenicity to anti-tumor necrosis factor therapy in IBD patients with loss of response - Immunix | Not Available | None | Academisch Medisch Centrum | Inflammatory Bowel Disease (Crohn's Disease and U… | Addition of methotrexaat to anti-therapy (inflixi… | Details |
| NCT03860012 | Evaluating the Efficacy of Weekly Folic Acid in Pediatric Inflammatory Bowel Disease Patients on Methotrexate | PHASE4 | Recruiting | Le Bonheur Children's Hospital | Inflammatory Bowel Diseases | Drug: Folic Acid | Details |
| NCT03204136 | Tacrolimus Versus Methotrexate as Rescue Therapy for Refractory Inflammatory Bowel Disease: an Open-label, Retrospective Study | Not Available | Not recruiting | Key Laboratory of Gastroenterology and Hepatology, Ministry of Health, China | Inflammatory Bowel Diseases;Inflammatory Bowel Di… | None | Details |
| ISRCTN23541842 | The auxiliary diagnostic value of fissured tongue on axial and peripheral joint dysfunction in Ankylosing Spondylitis | Not Available | Not Recruiting | Zhejiang University Of Chinese Medicine | Ankylosing spondylitis Musculoskeletal Diseases … | Participants are screened and undergo a clinical … | Details |
| NCT03531593 | Dose Effect Relationship of Methotrexate and Hepatic Fibrosis in Patients With Inflammatory Bowel Disease | Not Available | Not recruiting | Children's Mercy Hospital Kansas City | Inflammatory Bowel Diseases;Liver Fibroses;Methot… | Diagnostic Test: Ultrasound Elastography | Details |
| EUCTR2016-000522-18-FR | Risk stratified randomized controlled trial in paediatric Crohn Disease: Methotrexate versus azathioprine or adalimumab for maintaining remission in patients at low or at high risk for aggressive disease course, respectively a treatment strategy - REDUCE-RISKincd-PIBD-TRIAL | PHASE4 | Not Available | PIBDNet | Crohn disease;Therapeutic area: Diseases [C] - Di… | Product Name: humira Pharmaceutical Form: Solutio… | Details |
| NCT02461784 | The Effect of Methotrexate on Sperm Quality in Men With Inflammatory Bowel Disease | None | TERMINATED | University of Wisconsin, Madison | Inflammatory Bowel Disease (IBD) | PROCEDURE: Semen & Data Collection | Details |
| NCT05927064 | Study Evaluating the Persistence, Efficacy and Tolerability of Methotrexate in Inflammatory Bowel Disease Patients | None | COMPLETED | Central Hospital, Nancy, France | Inflammatory Bowel Diseases|Crohn Disease|Ulcerat… | None | Details |
| NCT02413047 | Evaluate if Response to Infliximab or Adalimumab May be Regained With an Immunomodulator | None | TERMINATED | Indiana University | Inflammatory Bowel Disease|Ulcerative Colitis|Cro… | DRUG: Azathioprine|DRUG: 6 mercaptopurine|DRUG: M… | Details |
| NCT01716039 | Pharmacokinetics of Adalimumab With Methotrexate for Treatment of Patients With Ulcerative Colitis (UC) | PHASE2 | TERMINATED | Alimentiv Inc. | Ulcerative Colitis | DRUG: MTX 12.5|DRUG: MTX 25|DRUG: Adalimumab | Details |
| Disease ID | Disease Name | Definition | Category | Related Drugs | Mechanism | |
|---|---|---|---|---|---|---|
| No data available | ||||||
| Strategy ID | Therapeutic Strategy | Synonyms | Related Drugs | Mechanism | |
|---|---|---|---|---|---|
| S02 | Immunosuppression | Classic immunosuppressive drugs | azathioprine; 6-mercaptopurine; methotrexate; ciclosporin-A; tacrolimus | Ciclosporin-A and tacrolimus bind to specific intracellular… | Details |
Thiopurines Have Longer Treatment Durability than Methotrexate in Adults and Ch…
PMID: 37099729
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Thiopurines and methotrexate have long been used to maintain remission in Crohn's disease [CD]. In this nationwide study, we aimed to com…
Weekly Folic Acid Is a Convenient and Well-Tolerated Alternative to Daily Dosin…
PMID: 37049427
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Inflammatory bowel disease (IBD) is a chronic autoimmune disorder that affects the gastrointestinal tract. Methotrexate is a folate analo…
Comparative Effectiveness of Anti-TNF in Combination With Low-Dose Methotrexate…
PMID: 37004887
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND & AIMS: Tumor necrosis factor inhibitors, including infliximab and adalimumab, are a mainstay of pediatric Crohn's disease therapy; howeve…
Cumulative dose and length of methotrexate treatment were not shown to be predi…
PMID: 36811460
Year: 2023
Relationship Type:
Treatment
Score: 6.5
OBJECTIVE: Methotrexate is used in several inflammatory diseases, such as rheumatoid arthritis (RA), spondyloarthritis (SpA) or inflammatory bowel di…
Methotrexate showed efficacy both in Crohn's disease and ulcerative colitis, pr…
PMID: 36225564
Year: 2022
Relationship Type:
Treatment
Score: 6.5
Objective: This study aimed to evaluate methotrexate efficacy in patients with Crohn's disease (CD) and ulcerative colitis (UC), and identify predict…
Association Between Low-Dose Methotrexate Exposure and Melanoma: A Systematic R…
PMID: 36044236
Year: 2022
Relationship Type:
Treatment
Score: 6.5
IMPORTANCE: Methotrexate is widely used for the treatment of inflammatory disorders, including rheumatoid arthritis. Studies suggest that methotrexat…
Favourable Tolerability and Drug Survival of Tioguanine Versus Methotrexate Aft…
PMID: 35303065
Year: 2022
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIMS: Both methotrexate and tioguanine can be considered as treatment options in patients with Crohn's disease after failure of conven…
Persistently normal blood tests in patients taking methotrexate for RA or azath…
PMID: 35256384
Year: 2022
Relationship Type:
Association
Score: 6.5
BACKGROUND: Disease-modifying anti-rheumatic drugs (DMARDs), including methotrexate and azathioprine, are commonly used to treat rheumatoid arthritis…
Extracorporeal Treatment for Methotrexate Poisoning: Systematic Review and Reco…
PMID: 35236714
Year: 2022
Relationship Type:
Treatment
Score: 6.5
Methotrexate is used in the treatment of many malignancies, rheumatological diseases, and inflammatory bowel disease. Toxicity from use is associated…
Parenteral Methotrexate Is Efficient in the Treatment of Azathioprine Refractor…
PMID: 35115294
Year: 2022
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: There is limited data in the literature analyzing the efficacy of methotrexate in Crohn's disease used after thiopurine analogs. We aimed…
Methotrexate in inflammatory bowel disease: A primer for gastroenterologists
PMID: 35042318
Year: 2022
Relationship Type:
Treatment
Score: 6.5
Methotrexate is an antineoplastic agent that is also used at lower doses for anti-inflammatory properties. Along with thiopurines (azathioprine and 6…
Simultaneous measurement of upadacitinib and methotrexate by UPLC-MS/MS and its…
PMID: 34875493
Year: 2022
Relationship Type:
Treatment
Score: 6.5
Upadacitinib, as a selective and reversible Janus kinase (JAK) inhibitor, has been widely used in the treatment of atopic dermatitis, ulcerative coli…
Triple therapy with adalimumab, ustekinumab and methotrexate for induction of r…
PMID: 34645625
Year: 2021
Relationship Type:
Treatment
Score: 6.5
Induction of remission in biologic-experienced individuals with moderate to severe Crohn's disease (CD) can be a challenge. We hereby present a case …
Increased incidence of inflammatory bowel disease on etanercept in juvenile idi…
PMID: 34508559
Year: 2022
Relationship Type:
Treatment
Score: 6.5
OBJECTIVE: To describe risk factors for IBD development in a cohort of children with JIA. METHODS: JIA patients who developed IBD were identified fro…
Low-dose Methotrexate Therapy Does Not Affect Semen Parameters and Sperm DNA
PMID: 34463329
Year: 2022
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Methotrexate is widely used in inflammatory diseases during the patients' reproductive years. The effect on male fertility and sperm DNA …
The maximum dose and duration in the therapy single use methotrexate to achieve…
PMID: 34214354
Year: 2021
Relationship Type:
Treatment
Score: 6.5
OBJECTIVES: One of the treatments for rheumatoid arthritis (RA) was methotrexate which a disease modifying antirheumatic drug therapy. The use of met…
Effectiveness and safety of methotrexate monotherapy in patients with Crohn's d…
PMID: 33715177
Year: 2021
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Methotrexate can be used to maintain remission in Crohn's disease patients who are intolerant to thiopurines. Data on its use as monother…
A pragmatic non-invasive assessment of liver fibrosis in patients with psoriasi…
PMID: 33602481
Year: 2020
Relationship Type:
Treatment
Score: 6.5
BACKGROUND AND AIMS: The reported hepatotoxicity of methotrexate underlines the need for a repeated non-invasive and reliable evaluation of liver fib…
Noninvasive assessment of liver fibrosis in Crohn's disease patients exposed to…
PMID: 32804842
Year: 2021
Relationship Type:
Adverse Effect
Score: 6.5
BACKGROUND: Methotrexate is widely used to treat some inflammatory chronic disorders, though it is hampered by the risk of liver fibrosis. Many recom…
Aminosalicylates, thiopurines and methotrexate in inflammatory bowel disease: I…
PMID: 30954317
Year: 2019
Relationship Type:
Treatment
Score: 6.5
The current goals of treatment in inflammatory bowel disease, both Crohn's disease and ulcerative colitis, are to achieve clinical, endoscopic and id…