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Methotrexate

Generic Name
Methotrexate
Brand Names
Metoject, Nordimet, Otrexup, Rasuvo, Reditrex, Trexall, Xatmep, Jylamvo
Drug Type
Small Molecule
Chemical Formula
C20H22N8O5
CAS Number
59-05-2
Unique Ingredient Identifier
YL5FZ2Y5U1
Background

Methotrexate is a folate derivative that inhibits several enzymes responsible for nucleotide synthesis. This inhibition leads to suppression of inflammation as well as prevention of cell division. Because of these effects, methotrexate is often used to treat inflammation caused by arthritis or to control cell division in neoplastic diseases such as breast cancer and non-Hodgkin's lymphoma.

Due to the toxic effects of methotrexate, it is indicated for treatment of some forms of arthritis and severe psoriasis only if first line treatment has failed or patients are intolerant of those treatments.

Methotrexate was granted FDA approval on 7 December 1953.

Indication

Methotrexate oral solution is indicated for pediatric acute lymphoblastic leukemia and pediatric polyarticular juvenile idiopathic arthritis. Methotrexate injections for subcutaneous use are indicated for severe active rheumatoid arthritis, polyarticular juvenile idiopathic arthritis and severe, recalcitrant, disabling psoriasis.

Other formulations are indicated to treat gestational choriocarcinoma, chorioadenoma destruens, hydatiform mole, breast cancer, epidermoid cancer of the head and neck, advanced mycosis fungoides, lung cancer, and advanced non-Hodgkin's lymphoma. It is also used in the maintenance of acute lymphocytic leukemia. Methotrexate is also given before treatment with leucovorin to prolong relapse-free survival following surgical removal of a tumour in non-metastatic osteosarcoma.

Associated Conditions
Acute Lymphoblastic Leukemia (ALL), Acute Promyelocytic Leukemia, Bladder Cancer, Breast Cancer, Central Nervous System Lymphoma, Crohn's Disease (CD), Dermatomyositis (DM), Extrauterine Pregnancy, Gestational Trophoblastic Neoplasia, Graft-versus-host Disease (GVHD), Meningeal leukemia, Multiple Sclerosis, Mycosis Fungoides (MF), Non-Hodgkin's Lymphoma (NHL), Non-Hodgkin's Lymphoma, Relapsed, Osteosarcoma, Polyarticular Juvenile Idiopathic Arthritis, Polymyositis, Rheumatoid Arthritis, Soft Tissue Sarcoma, Squamous Cell Carcinoma of the Head and Neck (SCCHN), Systemic Lupus Erythematosus, Uveitis, Nonleukemic meningeal cancer, Refractory Non-Hodgkin's lymphoma, Refractory Takayasu arteritis, Severe Psoriasis
Associated Therapies
Medically induced abortion

A Pharmacokinetic and Pharmacodynamic Study of MabThera (Rituximab) Plus Methotrexate in Patients With Rheumatoid Arthritis (RA)

Phase 2
Terminated
Conditions
Rheumatoid Arthritis
Interventions
First Posted Date
2007-01-17
Last Posted Date
2014-07-16
Lead Sponsor
Hoffmann-La Roche
Target Recruit Count
3
Registration Number
NCT00422942

Study of the Optimal Protocol for Methotrexate and Adalimumab Combination Therapy in Early Rheumatoid Arthritis

Phase 4
Completed
Conditions
Rheumatoid Arthritis
Interventions
Biological: adalimumab
Drug: methotrexate
Biological: placebo
First Posted Date
2007-01-11
Last Posted Date
2012-04-18
Lead Sponsor
Abbott
Target Recruit Count
1032
Registration Number
NCT00420927
Locations
🇺🇸

Site Reference ID/Investigator# 4548, Chicago, Illinois, United States

🇺🇸

Site Reference ID/Investigator# 4538, Houston, Texas, United States

🇺🇸

Site Reference ID/Investigator# 4605, Wichita, Kansas, United States

and more 167 locations

Combination Chemotherapy and Rituximab in Treating Patients With Newly Diagnosed Primary CNS Lymphoma

Not Applicable
Completed
Conditions
Brain and Central Nervous System Tumors
Lymphoma
Interventions
First Posted Date
2006-12-28
Last Posted Date
2015-08-20
Lead Sponsor
University of California, San Francisco
Target Recruit Count
10
Registration Number
NCT00416819

PRINTO (the Paediatric Rheumatology International Trials Organisation)

Conditions
Juvenile Idiopathic Arthritis
First Posted Date
2006-12-25
Last Posted Date
2006-12-25
Lead Sponsor
Institute of Child Health
Registration Number
NCT00415935
Locations
🇬🇧

Rheumatology ICH, London, United Kingdom

A Phase III Study of Abatacept in Patients With Rheumatoid Arthritis and an Inadequate Response to Methotrexate

Phase 3
Completed
Conditions
Rheumatoid Arthritis
Interventions
First Posted Date
2006-12-11
Last Posted Date
2013-08-08
Lead Sponsor
Bristol-Myers Squibb
Target Recruit Count
113
Registration Number
NCT00409838
Locations
🇰🇷

Local Institution, Seoul, Korea, Republic of

Combination Chemotherapy in Treating Young Patients With Newly Diagnosed T-Cell Acute Lymphoblastic Leukemia or T-cell Lymphoblastic Lymphoma

First Posted Date
2006-12-05
Last Posted Date
2025-01-03
Lead Sponsor
National Cancer Institute (NCI)
Target Recruit Count
1895
Registration Number
NCT00408005
Locations
🇺🇸

Scott and White Memorial Hospital, Temple, Texas, United States

🇺🇸

Henry Ford Health Saint John Hospital, Detroit, Michigan, United States

🇺🇸

Children's Hospital of Alabama, Birmingham, Alabama, United States

and more 212 locations

Sirolimus/Tacrolimus Versus Tacrolimus/Methotrexate for Preventing Graft-Versus-Host Disease (GVHD) (BMT CTN 0402)

Phase 3
Completed
Conditions
Leukemia, Lymphocytic, Acute
Myelodysplastic Syndromes
Leukemia, Myelocytic, Acute
Leukemia, Myeloid, Chronic
Interventions
First Posted Date
2006-12-04
Last Posted Date
2023-01-04
Lead Sponsor
Medical College of Wisconsin
Target Recruit Count
304
Registration Number
NCT00406393
Locations
🇺🇸

Stanford Hospital and Clinics, Stanford, California, United States

🇺🇸

Washington University/Barnes Jewish Hospital, Saint Louis, Missouri, United States

🇺🇸

City of Hope National Medical Center, Duarte, California, United States

and more 21 locations

A Study of Ocrelizumab Compared to Placebo in Patients With Active Rheumatoid Arthritis Continuing Methotrexate Treatment (STAGE)

Phase 3
Terminated
Conditions
Rheumatoid Arthritis
Interventions
First Posted Date
2006-12-04
Last Posted Date
2020-11-27
Lead Sponsor
Genentech, Inc.
Target Recruit Count
1015
Registration Number
NCT00406419
Locations
🇺🇸

Trial Information Support Line, South San Francisco, California, United States

Rheumatoid Arthritis: Comparison of Active Therapies in Patients With Active Disease Despite Methotrexate Therapy

Not Applicable
Completed
Conditions
Rheumatoid Arthritis
Interventions
First Posted Date
2006-11-30
Last Posted Date
2013-12-03
Lead Sponsor
US Department of Veterans Affairs
Target Recruit Count
353
Registration Number
NCT00405275
Locations
🇺🇸

VA Medical Center, Loma Linda, Loma Linda, California, United States

🇺🇸

VA Pittsburgh Health Care System, Pittsburgh, Pennsylvania, United States

🇺🇸

Geisinger Medical Group - State College, State College, Pennsylvania, United States

and more 34 locations

Alloreactive NK Cells for Allogeneic Stem Cell Transplantation for Acute Myeloid Leukemia (AML) and Myelodysplastic Syndrome (MDS)

Phase 1
Completed
Conditions
Leukemia
Myelodysplastic Syndrome
Interventions
First Posted Date
2006-11-22
Last Posted Date
2015-05-08
Lead Sponsor
M.D. Anderson Cancer Center
Target Recruit Count
15
Registration Number
NCT00402558
Locations
🇺🇸

UT MD Anderson Cancer Center, Houston, Texas, United States

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