| 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 |
Combating Methotrexate Resistance in Cancer Treatment: A Review on Navigating P…
PMID: 40270992
Year: 2025
Relationship Type:
Treatment
Score: 7.5
Methotrexate (MTX), a potent analogue and antagonist of folic acid, is a first-line treatment for rheumatoid arthritis, IBD and cancer. The developme…
Erythrocyte Methotrexate-Polyglutamate Concentrations in Pediatric Inflammatory…
PMID: 39982703
Year: 2025
Relationship Type:
Treatment
Score: 7.5
BACKGROUND AND AIMS: Therapeutic drug monitoring (TDM) of methotrexate (MTX) is challenging due to its pharmacokinetics and short plasma half-life. I…
Effectiveness and Tolerability of Methotrexate Combined with Biologics in Patie…
PMID: 38217678
Year: 2024
Relationship Type:
Treatment
Score: 7.5
BACKGROUND: Methotrexate (MTX) combination therapy with biological agents has gained increasing interest. Here, we assessed the efficacy and tolerabi…
Oral Versus Subcutaneous Methotrexate in Immune-Mediated Inflammatory Disorders…
PMID: 37768405
Year: 2023
Relationship Type:
Treatment
Score: 7.5
PURPOSE: This review aims to critically evaluate the potential benefit of either oral or subcutaneous administration of methotrexate (MTX) in various…
Therapeutic drug monitoring of methotrexate in patients with Crohn's disease
PMID: 37767910
Year: 2023
Relationship Type:
Treatment
Score: 7.5
BACKGROUND: Therapeutic drug monitoring (TDM) has the potential to improve efficacy and diminish side effects. Measuring methotrexate-polyglutamate (…
Colon-specific delivery of methotrexate using hyaluronic acid modified pH-respo…
PMID: 36804523
Year: 2023
Relationship Type:
Treatment
Score: 7.5
Oral immunosuppressant methotrexate (MTX) is an effective method for the treatment of inflammatory bowel disease (IBD). To overcome the defects of cl…
The Effectiveness and Safety of Methotrexate as the First-Line Immunomodulator …
PMID: 36754081
Year: 2023
Relationship Type:
Treatment
Score: 7.5
OBJECTIVES: Methotrexate (MTX) has been used as maintenance therapy for Crohn disease (CD) in adults and children. However, there are only a few stud…
A meta-analysis of methotrexate polyglutamates in relation to efficacy and toxi…
PMID: 36326810
Year: 2023
Relationship Type:
Treatment
Score: 7.5
AIMS: In immune-mediated inflammatory diseases (IMIDs), early symptom control is a key therapeutic goal. Methotrexate (MTX) is the first-line treatme…
Subcutaneous administration, higher age and lower renal function are associated…
PMID: 35907797
Year: 2022
Relationship Type:
Treatment
Score: 7.5
BACKGROUND: Methotrexate is an immunomodulatory drug for patients with Crohn's disease. Erythrocyte MTX-polyglutamates (MTX-PG(1-5)) may be used for …
Methotrexate for Primary Maintenance Therapy in Mild-to-Moderate Crohn Disease …
PMID: 35758420
Year: 2022
Relationship Type:
Treatment
Score: 7.5
OBJECTIVES: Despite limited data, methotrexate (MTX) is often used as primary maintenance therapy in pediatric Crohn disease (CD). We sought to asses…
Mucosal healing with methotrexate versus azathioprine treatment in pediatric Cr…
PMID: 35373937
Year: 2022
Relationship Type:
Treatment
Score: 7.5
BACKGROUND/OBJECTIVES: The current treatment goal for inflammatory bowel disease (IBD) is achievement of mucosal healing (MH). While established with…
Short-term tolerability and effectiveness of methotrexate monotherapy in adult …
PMID: 34539814
Year: 2021
Relationship Type:
Treatment
Score: 7.5
INTRODUCTION: Immunomodulators remain fundamental for the medical treatment of Crohn's disease (CD). Methotrexate (MTX) is widely used as a second-li…
Cost-Effectiveness Analysis of Parenteral Methotrexate for the Treatment of Cro…
PMID: 33426625
Year: 2021
Relationship Type:
Treatment
Score: 7.5
BACKGROUND: Despite worldwide use of parenteral methotrexate (pMTX), health economic evidence for its use in Crohn's disease (CD) is limited. The low…
Pharmacogenetic studies of thiopurine methyltransferase genotype-phenotype conc…
PMID: 32865889
Year: 2021
Relationship Type:
Treatment
Score: 7.5
The discovery and implementation of thiopurine methyltransferase (TPMT) pharmacogenetics has been a success story and has reduced the suffering from …
Protocol for a multinational risk-stratified randomised controlled trial in pae…
PMID: 32611737
Year: 2020
Relationship Type:
Treatment
Score: 7.5
INTRODUCTION: Immunomodulators such as thiopurines (azathioprine (AZA)/6-mercaptopurine (6MP)), methotrexate (MTX) and biologics such as adalimumab (…
How does methotrexate work?
PMID: 32239204
Year: 2020
Relationship Type:
Treatment
Score: 7.5
Developed over 70 years ago as an anti-folate chemotherapy agent, methotrexate (MTX) is a WHO 'essential medicine' that is now widely employed as a f…
Analytical methodologies for determination of methotrexate and its metabolites …
PMID: 31890337
Year: 2019
Relationship Type:
Treatment
Score: 7.5
Methotrexate (MTX) is a folate antagonist drug used for several diseases, such as cancers, various malignancies, rheumatoid arthritis (RA) and inflam…
[Successful treatment of gangrenous pyoderma with methotrexate in a patient wit…
PMID: 31333236
Year: 2019
Relationship Type:
Treatment
Score: 7.5
Pyoderma gangrenosum (PG) is a neutrophilic, cutaneous-ulcerative, non-infectious dermatosis that occurs in up to 2% of patients with Crohn's disease…
A single-center experience with methotrexate in the treatment of Chinese Crohn'…
PMID: 30516330
Year: 2018
Relationship Type:
Treatment
Score: 7.3
OBJECTIVE: Methotrexate (MTX) can be used as an alternative for patients with Crohn's disease (CD) who are intolerant of thiopurine. This retrospecti…
Methotrexate and Thioguanine Rescue Therapy for Conventional Thiopurine Failing…
PMID: 29668998
Year: 2018
Relationship Type:
Treatment
Score: 7.3
BACKGROUND: Patients with active ulcerative colitis (UC) failing conventional therapies are in need of rescue strategies. Due to the fact that accept…