| 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 |
The safety and tolerability of methotrexate for treating patients with Crohn's …
PMID: 21224737
Year: 2011
Relationship Type:
Treatment
Score: 6.1
GOALS: To determine the safety and tolerance of methotrexate for treating patients with Crohn's disease in clinical practice. BACKGROUND: Methotrexat…
Methotrexate-induced pneumonitis in a patient with Crohn's disease
PMID: 21122509
Year: 2010
Relationship Type:
Treatment
Score: 6.1
Pulmonary toxicity is a well recognised but infrequent adverse event of treatment with methotrexate. The vast majority of cases have occurred in pati…
Methotrexate in paediatric ulcerative colitis: a retrospective survey at a sing…
PMID: 20937047
Year: 2010
Relationship Type:
Adverse Effect
Score: 6.1
BACKGROUND: Patients with ulcerative colitis often receive thiopurines as immunomodulators (IMs) to maintain remission and avoid corticosteroids. If …
Combined approach with infliximab, surgery, and methotrexate in severe fistuliz…
PMID: 20623697
Year: 2011
Relationship Type:
Treatment
Score: 6.1
BACKGROUND: Infliximab is the only medical therapy that has been proven to be effective in fistulizing Crohn's disease (CD), but the recurrence rate …
Clinical experience of methotrexate in Crohn's disease: response, safety and mo…
PMID: 20354043
Year: 2010
Relationship Type:
Treatment
Score: 6.1
BACKGROUND: Methotrexate is an immunosuppressant used in the treatment of patients with Crohn's disease who are intolerant or refractory to azathiopr…
Efficacy of methotrexate in ulcerative colitis: failure or promise
PMID: 20186931
Year: 2010
Relationship Type:
Treatment
Score: 6.1
BACKGROUND: Low-dose methotrexate is a widely used and efficacious therapy in chronic inflammatory disorders such as psoriasis and rheumatoid arthrit…
Methotrexate for induction of remission in ulcerative colitis
PMID: 17943916
Year: 2007
Relationship Type:
Treatment
Score: 6.1
Update in Cochrane Database Syst Rev. 2018 Aug 11;8:CD005984. BACKGROUND: Prevention of relapse is a major issue in the management of Crohn's d…
[The use of methotrexate in an inflammatory bowel diseases based on the review …
PMID: 27487545
Year: 2016
Relationship Type:
Treatment
Score: 5.3
M ethotrexate (MTX) as an immunomodulatory drug has numerous applications in autoimmune diseases. Autoimmune patomechanism is one of the factors resp…