| 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 | |
|---|---|---|---|---|---|---|---|
| NCT07138898 | Immunosuppressant Management in Rheumatology Patients Undergoing Elective Total Shoulder Arthroplasty | PHASE2 | NOT_YET_RECRUITING | NYU Langone Health | Rheumatic Disease | DRUG: Methotrexate|DRUG: Sulfasalazine|DRUG: Hydr… | Details |
| NCT05072782 | Management of Moderate POstoperative Recurrence in Crohn's Disease: a randoMizEd contROLled Trial of Therapeutic Escalation, the POMEROL Trial. (POMEROL) | PHASE4 | UNKNOWN | Groupe d'Etude Therapeutique des Affections Inflammatoires Digestives | Crohn Disease | DRUG: Infliximab CT-P13|DRUG: Immunosuppressors (… | Details |
| NCT05040464 | Comparison of Azathioprine to Methotrexate in Combination Therapy With Adalimumab in Crohn's Disease: an Open-label Randomized Controlled Trial | PHASE3 | RECRUITING | Centre Hospitalier Universitaire, Amiens | Crohn Disease|Azathioprine|Methotrexate | DRUG: AZA capsules|DRUG: MTX|BIOLOGICAL: blood sa… | Details |
| NCT04205734 | Methotrexate Polyglutamate Measurements in Patients With Inflammatory Bowel Disease | NULL | SUSPENDED | Boston Children's Hospital | IBD | DIAGNOSTIC_TEST: MTX Assessment | Details |
| NCT04196920 | Methotrexate-associated Anti-TNF Combination Therapy, the Neglected One ! | NULL | UNKNOWN | University Hospital, Montpellier | Chronic Inflammatory Bowel Disease | None | Details |
| NCT03531593 | Dose Effect Relationship of MTX and IBD | NULL | COMPLETED | Children's Mercy Hospital Kansas City | Inflammatory Bowel Diseases|Liver Fibroses|Methot… | DIAGNOSTIC_TEST: Ultrasound Elastography | Details |
| NCT03204136 | Tacrolimus Versus Methotrexate as Rescue Therapy for Refractory Inflammatory Bowel Disease | NULL | UNKNOWN | Key Laboratory of Gastroenterology and Hepatology, Ministry of Health, China | Inflammatory Bowel Diseases | None | Details |
| NCT02852694 | Reduce Risk for Crohn's Disease Patients | PHASE4 | COMPLETED | PIBD-Net | Crohn's Disease | DRUG: Methotrexate|DRUG: Adalimumab|DRUG: Azathio… | Details |
| NCT02764762 | Triple Combination Therapy in High Risk Crohn's Disease (CD) | PHASE4 | COMPLETED | Takeda | Crohn Disease | DRUG: Vedolizumab|DRUG: Adalimumab|DRUG: Methotre… | Details |
| NCT02461784 | The Effect of Methotrexate on Sperm Quality in Men With Inflammatory Bowel Disease | NULL | TERMINATED | University of Wisconsin, Madison | Inflammatory Bowel Disease (IBD) | PROCEDURE: Semen & Data Collection | Details |
| NCT02413047 | Evaluate if Response to Infliximab or Adalimumab May be Regained With an Immunomodulator | NA | TERMINATED | Indiana University | Inflammatory Bowel Disease|Ulcerative Colitis|Cro… | DRUG: Azathioprine|DRUG: 6 mercaptopurine|DRUG: M… | Details |
| NCT02269358 | Salvage Therapy With High/Low Methotrexate for Loss of Response to Infliximab Dose Escalation | PHASE4 | COMPLETED | Prof. Arie Levine | Crohn's Disease | DRUG: METHOTREXATE | Details |
| NCT02177071 | A proSpective Randomized Controlled Trial comParing infliximAb-antimetabolites Combination Therapy to Anti-metabolites monotheRapy and Infliximab monothErapy in Crohn's Disease Patients in Sustained Steroid-free Remission on Combination Therapy | PHASE4 | COMPLETED | Groupe d'Etude Therapeutique des Affections Inflammatoires Digestives | Crohn's Disease | DRUG: INFLIXIMAB|DRUG: AZATHIOPRINE|DRUG: MERCAPT… | Details |
| NCT01802593 | Comparison of 2 Immunomodulator Withdrawal Schemes for Infliximab Monotherapy in Active Pediatric Crohn's Disease After Thiopurine Failure | PHASE4 | TERMINATED | Prof. Arie Levine | Crohn's Disease | DRUG: AZATHIOPRINE or METHOTREXATE|DRUG: AZATHIOP… | 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 |
| 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 |
| NCT00546546 | Early Immunosuppressants in Crohn's Disease | PHASE4 | COMPLETED | Groupe d'Etude Therapeutique des Affections Inflammatoires Digestives | Crohn's Disease | DRUG: early immunosuppressants (azathioprine, met… | Details |
| 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 |
| NCT00132899 | COMMIT (Combination Of Maintenance Methotrexate-Infliximab Trial) | PHASE3 | COMPLETED | University of Western Ontario, Canada | Crohn's Disease | DRUG: Methotrexate|DRUG: Placebo | Details |
| NCT00035074 | A Pharmacokinetic Study to Determine the Oral Bioavailability of Methotrexate in Patients With Inflammatory Bowel Disease | NULL | COMPLETED | National Center for Research Resources (NCRR) | Inflammatory Bowel Disease | DRUG: Methotrexate | 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 |
Neuroradiological worsening of brain abscess after adalimumab and methotrexate …
PMID: 30611629
Year: 2019
Relationship Type:
Treatment
Score: 6.5
The incidence of brain abscess is higher among immunosuppressed patients. We report a case of a brain abscess in the temporal lobe in a patient under…
Higher Mucosal Healing with Tumor Necrosis Factor Inhibitors in Combination wit…
PMID: 30560332
Year: 2019
Relationship Type:
Treatment
Score: 6.5
BACKGROUND: The differential impact of anti-tumor necrosis factor (anti-TNF) therapy with methotrexate versus thiopurine co-therapy on endoscopic rem…
Update on the Use of Thiopurines and Methotrexate in Inflammatory Bowel Disease
PMID: 30267281
Year: 2018
Relationship Type:
Treatment
Score: 6.3
PURPOSE OF REVIEW: The increased use of biologic agents over the past two decades has led to a reappraisal of the role of the immunomodulators (thiop…
Methotrexate and lung disease in rheumatoid arthritis
PMID: 27711025
Year: 2017
Relationship Type:
Treatment
Score: 6.3
Rheumatoid arthritis (RA) is a common chronic inflammatory disease affecting many tissues and resulting in substantial morbidity and increased mortal…
Review of the bioanalytical methods for the determination of methotrexate and i…
PMID: 27623319
Year: 2017
Relationship Type:
Treatment
Score: 6.3
Methotrexate is an old drug that has found use in several therapeutic areas, such as cancer to treat various malignancies, rheumatoid arthtritis and …
Inadvertent yellow fever vaccination of a patient with Crohn's disease treated …
PMID: 27571912
Year: 2016
Relationship Type:
Treatment
Score: 6.3
We present a case of a 56-year-old woman with Crohn's disease, treated with methotrexate and infliximab, who inadvertently received yellow fever vacc…
Safety profile of methotrexate in inflammatory bowel disease
PMID: 27462711
Year: 2016
Relationship Type:
Treatment
Score: 6.3
INTRODUCTION: Methotrexate, which was initially developed in 1948 for the treatment of leukemia, is known to be an immunomodulatory and anti-inflamma…
A case of enteropathic arthritis successfully treated with methotrexate
PMID: 27320938
Year: 2016
Relationship Type:
Association
Score: 6.3
We report a 36-year-old male patient who suffered from polyarthritis after the remission of ulcerative colitis. He was diagnosed with enteropathic ar…
Molluscum contagiosum of the eyelid: case report in a man receiving methotrexat…
PMID: 27136625
Year: 2016
Relationship Type:
Treatment
Score: 6.3
BACKGROUND: Molluscum contagiosum is a benign viral infection of the skin. Lesions typically present as dome-shaped, flesh-colored, umbilicated papul…
European experience with methotrexate treatment in Crohn's disease: a multicent…
PMID: 26894634
Year: 2016
Relationship Type:
Treatment
Score: 6.3
Comment in Gastroenterology. 2015 May;148(5):877-80. BACKGROUND & AIMS: The medical management of ulcerative colitis (UC) has improved through …
Methotrexate for the Management of Crohn's Disease in Children
PMID: 26511908
Year: 2016
Relationship Type:
Treatment
Score: 6.3
OBJECTIVE: To review the literature evaluating methotrexate as a treatment option for Crohn's disease (CD) in pediatric patients. DATA SOURCES: A sea…
Risk of liver injury among methotrexate users: A meta-analysis of randomised co…
PMID: 26088004
Year: 2015
Relationship Type:
Treatment
Score: 6.3
OBJECTIVE: Methotrexate is an effective treatment for a variety of inflammatory diseases. Robust evidence on the risk of serious liver injury is lack…
Methotrexate use and risk of lung disease in psoriasis, psoriatic arthritis, an…
PMID: 25770113
Year: 2015
Relationship Type:
Adverse Effect
Score: 6.3
OBJECTIVE: To evaluate the relative risk of pulmonary disease among patients with psoriasis, psoriatic arthritis, and inflammatory bowel disease trea…
[Reccomendations of the Spanish Working Group on Crohn's Disease and Ulcerative…
PMID: 25454602
Year: 2015
Relationship Type:
Treatment
Score: 6.3
Methotrexate is an immunosuppressant that may be useful in several clinical scenarios in inflammatory bowel disease. In this article, we review the a…
Methotrexate for maintenance of remission in Crohn's disease
PMID: 25157445
Year: 2014
Relationship Type:
Treatment
Score: 6.3
Update of Cochrane Database Syst Rev. 2007;(4):CD006618. BACKGROUND: Ulcerative colitis (UC) is a chronic inflammatory bowel disease. Corticost…
Methotrexate: underused and ignored?
PMID: 23295701
Year: 2012
Relationship Type:
Treatment
Score: 6.1
For more than a decade, methotrexate has been known to be an effective therapeutic agent in the treatment of steroid-dependent active Crohn's disease…
Efficacy and tolerability of methotrexate therapy for refractory Crohn's diseas…
PMID: 22112005
Year: 2012
Relationship Type:
Treatment
Score: 6.1
BACKGROUND: Randomised controlled trials demonstrate that methotrexate is effective in inducing remission and preventing relapse of Crohn's disease (…
The use of methotrexate for treatment of inflammatory bowel disease in clinical…
PMID: 22051323
Year: 2012
Relationship Type:
Treatment
Score: 6.1
BACKGROUND: Methotrexate is considered a treatment for Crohn's disease, whilst few data in ulcerative colitis are available. AIM: To evaluate frequen…
Incidence of liver toxicity in inflammatory bowel disease patients treated with…
PMID: 21751301
Year: 2012
Relationship Type:
Adverse Effect
Score: 6.1
Update in Cochrane Database Syst Rev. 2015;8:CD007560. BACKGROUND: Methotrexate, a folate antagonist, is an immunosuppressant drug that is effe…
Methotrexate: a drug of the future in ulcerative colitis?
PMID: 21466494
Year: 2011
Relationship Type:
Treatment
Score: 6.1
Ulcerative colitis (UC) is a chronic inflammatory bowel disease that is thought to affect 1780000 patients in USA and Europe. Its incidence is increa…