| 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 |
Therapeutic role of methotrexate in pediatric Crohn's disease
PMID: 29338679
Year: 2018
Relationship Type:
Treatment
Score: 7.3
The main role of therapy in Crohn's disease (CD) is to achieve long-term clinical remission, and to allow for normal growth and development of childr…
The Influence of Methotrexate Treatment on Male Fertility and Pregnancy Outcome…
PMID: 28267049
Year: 2017
Relationship Type:
Treatment
Score: 7.3
BACKGROUND: Inflammatory bowel disease incidence peaks during the reproductive years. Methotrexate (MTX) is frequently used for inflammatory bowel di…
Methotrexate Polyglutamate Monitoring in Patients With Crohn's Disease
PMID: 27274011
Year: 2017
Relationship Type:
Treatment
Score: 7.3
Methotrexate is an efficacious immunosuppressant for induction and maintenance of remission in Crohn's disease. The goal of this pilot study was to d…
Methotrexate for Inflammatory Bowel Diseases - New Developments
PMID: 26981630
Year: 2016
Relationship Type:
Treatment
Score: 7.3
Methotrexate (MTX) is an established therapy for patients with steroid-dependent Crohn's disease (CD). MTX is also frequently used in combination wit…
[A Case of Crohn's Disease Showing Favorable Response to Induction and Maintena…
PMID: 26493510
Year: 2015
Relationship Type:
Treatment
Score: 7.3
Thanks to the introduction of immumomodulators and biologics, therapeutic approaches in Crohn's disease have changed significantly during the past de…
Use of Methotrexate in the Treatment of Inflammatory Bowel Diseases
PMID: 26457382
Year: 2016
Relationship Type:
Treatment
Score: 7.3
Low-dose methotrexate (MTX) therapy is a well-recognized therapy for many inflammatory conditions such as rheumatoid arthritis, psoriatic arthritis, …
Methotrexate for maintaining remission in paediatric Crohn's patients with prio…
PMID: 25656249
Year: 2015
Relationship Type:
Treatment
Score: 7.3
BACKGROUND AND AIMS: Methotrexate [MTX] is an immunomodulating drug that can be used to maintain remission in patients with Crohn's disease [CD], but…
Methotrexate: an old new drug in autoimmune disease
PMID: 25245537
Year: 2014
Relationship Type:
Treatment
Score: 7.3
Methotrexate (MTX) is currently considered, among disease-modifying anti-rheumatic drugs (DMARDs), the 'anchor-drug' in the treatment of rheumatoid a…
[The efficacy and safety of methotrexate in refractory Crohn's disease]
PMID: 24767205
Year: 2014
Relationship Type:
Treatment
Score: 7.3
OBJECTIVE: To assess the efficacy and safety of methotrexate(MTX) on refractory Crohn's disease(CD). METHODS: A total of 35 consecutive refractory CD…
Pharmacokinetic profiles for oral and subcutaneous methotrexate in patients wit…
PMID: 23190184
Year: 2013
Relationship Type:
Adverse Effect
Score: 7.1
BACKGROUND: Methotrexate (MTX) is administered subcutaneously to Crohn's Disease (CD) patients. There are very few studies evaluating the use of oral…
Evaluation of liver fibrosis by transient elastography in methotrexate treated …
PMID: 21719043
Year: 2011
Relationship Type:
Treatment
Score: 7.1
BACKGROUND AND AIMS: Methotrexate (MTX) safety is questioned by the risk of inducing liver fibrosis (LF). As transient elastography (FibroScan(R)) is…
Short-course ondansetron for the prevention of methotrexate-induced nausea in c…
PMID: 21681112
Year: 2011
Relationship Type:
Treatment
Score: 7.1
OBJECTIVES: Methotrexate (MTX) is an effective treatment for Crohn disease (CD); however, its application may be limited by the occurrence of nausea.…
Mucosal healing with methotrexate in Crohn's disease: a prospective comparative…
PMID: 21235604
Year: 2011
Relationship Type:
Treatment
Score: 7.1
BACKGROUND: Mucosal healing has become a new therapeutic goal in Crohn's disease and can be achieved with azathioprine (AZA) or biologics. Methotrexa…
Use of methotrexate in patients with inflammatory bowel diseases
PMID: 21044450
Year: 2010
Relationship Type:
Treatment
Score: 7.1
Methotrexate (MTX) is one of the immunosuppressants commonly used in inflammatory bowel diseases. There is very good evidence for its use in patients…
Methotrexate for maintenance of remission in chronic active Crohn's disease: lo…
PMID: 19924799
Year: 2010
Relationship Type:
Treatment
Score: 7.1
BACKGROUND: According to current guidelines methotrexate (MTX) should be considered as a second-line immunomodulator in patients with chronic active …
Methotrexate and Tumor Necrosis Factor Inhibitors Independently Decrease Neutra…
PMID: 39340091
Year: 2024
Relationship Type:
Association
Score: 6.5
Objective: SARS-CoV-2 remains the third most common cause of death in North America. We studied the effects of methotrexate and tumor necrosis factor…
Systematic review: Methotrexate-A poorly understood and underused medication in…
PMID: 39076140
Year: 2024
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Methotrexate, an immunosuppressant used for the treatment of inflammatory bowel disease (IBD) for over 30 years, remains underused compar…
Vedolizumab, Adalimumab, and Methotrexate Combination Therapy in Crohn's Diseas…
PMID: 37743037
Year: 2024
Relationship Type:
Treatment
Score: 6.5
BACKGROUND & AIMS: Although biologics have revolutionized the treatment of Crohn's disease (CD), an efficacy ceiling has been reached. Combining biol…
Effectiveness and tolerability of methotrexate monotherapy in Crohn's disease p…
PMID: 37655055
Year: 2023
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: Methotrexate monotherapy is recommended as a maintenance therapy for Crohn's disease (CD). However, long-term follow-up data are scarce. …
The Role of Low-Dose Oral Methotrexate in Increasing Anti-TNF Drug Levels and R…
PMID: 37445417
Year: 2023
Relationship Type:
Treatment
Score: 6.5
Concomitant immunomodulation is utilised in combination with anti-TNF therapy for IBD primarily to increase drug levels and prevent anti-drug antibod…