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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 Study With Tocilizumab [RoActemra/Actemra] Monotherapy or in Combination With Methotrexate in Patients With Rheumatoid Arthritis (PICTURE)

Phase 3
Completed
Conditions
Rheumatoid Arthritis
Interventions
First Posted Date
2010-02-05
Last Posted Date
2017-08-21
Lead Sponsor
Hoffmann-La Roche
Target Recruit Count
107
Registration Number
NCT01063062
Locations
🇪🇬

Banha Educational Hospital; Rheumatology, Banha, Egypt

🇪🇬

Kasr El Ainy Hospital; Rheumatology, Cairo, Egypt

🇪🇬

Manial Specialized Hospital; Rheumatology, Cairo, Egypt

and more 6 locations

Evaluation of Sarilumab (SAR153191/REGN88) on Top of Methotrexate in Rheumatoid Arthritis Patients

Phase 2
Completed
Conditions
Rheumatoid Arthritis
Interventions
First Posted Date
2010-02-03
Last Posted Date
2017-06-28
Lead Sponsor
Sanofi
Target Recruit Count
1675
Registration Number
NCT01061736
Locations
🇦🇷

Investigational Site Number 032002, Cordoba, Argentina

🇦🇷

Investigational Site Number 032004, Tucuman, Argentina

🇦🇷

Investigational Site Number 032003, Córdoba, Argentina

and more 259 locations

A Safety and Efficacy Study of Ustekinumab in Patients With Plaque Psoriasis Who Have Had an Inadequate Response to Methotrexate

Phase 4
Completed
Conditions
Psoriasis
Interventions
First Posted Date
2010-02-01
Last Posted Date
2014-11-24
Lead Sponsor
Janssen-Cilag International NV
Target Recruit Count
490
Registration Number
NCT01059773

Fludarabine Phosphate, Busulfan, and Anti-Thymocyte Globulin Followed By Donor Peripheral Blood Stem Cell Transplant, Tacrolimus, and Methotrexate in Treating Patients With Myeloid Malignancies

Phase 2
Completed
Conditions
Adult Acute Myeloid Leukemia With Del(5q)
Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)
Adult Acute Myeloid Leukemia With t(15;17)(q22;q12)
Blastic Phase Chronic Myelogenous Leukemia
de Novo Myelodysplastic Syndromes
Myelodysplastic/Myeloproliferative Neoplasm, Unclassifiable
Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities
Childhood Acute Myeloid Leukemia in Remission
Childhood Myelodysplastic Syndromes
Recurrent Adult Acute Myeloid Leukemia
Interventions
Drug: fludarabine phosphate
Drug: busulfan
Biological: anti-thymocyte globulin
Drug: tacrolimus
Drug: methotrexate
Procedure: peripheral blood stem cell transplantation
Procedure: allogeneic hematopoietic stem cell transplantation
Other: laboratory biomarker analysis
First Posted Date
2010-01-26
Last Posted Date
2016-05-06
Lead Sponsor
Fred Hutchinson Cancer Center
Target Recruit Count
23
Registration Number
NCT01056614
Locations
🇺🇸

Fred Hutchinson Cancer Research Center/University of Washington Cancer Consortium, Seattle, Washington, United States

A Study of Tocilizumab and Methotrexate in Combination or as Monotherapy in Treatment-Naïve Patients With Early Rheumatoid Arthritis

Phase 3
Completed
Conditions
Rheumatoid Arthritis
Interventions
First Posted Date
2009-12-17
Last Posted Date
2016-07-11
Lead Sponsor
Hoffmann-La Roche
Target Recruit Count
317
Registration Number
NCT01034137

Cyclophosphamide, Methotrexate, and Fluorouracil, With or Without Epirubicin Hydrochloride, in Treating Women Who Have Undergone Surgery for Breast Cancer (Group III Closed to New Patients as of 12/7/2009)

Phase 3
Conditions
Breast Cancer
First Posted Date
2009-12-14
Last Posted Date
2013-08-02
Lead Sponsor
Istituto Scientifico Romagnolo per lo Studio e la cura dei Tumori
Target Recruit Count
800
Registration Number
NCT01031030

Donor Stem Cell Transplant in Treating Patients With High-Risk Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma

Phase 2
Completed
Conditions
Leukemia
Lymphoma
Interventions
First Posted Date
2009-12-07
Last Posted Date
2023-05-06
Lead Sponsor
Alliance for Clinical Trials in Oncology
Target Recruit Count
68
Registration Number
NCT01027000
Locations
🇺🇸

Cleveland Clinic Taussig Cancer Center, Cleveland, Ohio, United States

🇺🇸

Massachusetts General Hospital, Boston, Massachusetts, United States

🇺🇸

Dana-Farber/Brigham and Women's Cancer Center, Boston, Massachusetts, United States

and more 22 locations

Donor Stem Cell Transplant or Bone Marrow Transplant in Treating Patients With Acute Myeloid Leukemia in Remission

Phase 2
Completed
Conditions
Leukemia
Interventions
Biological: anti-thymocyte globulin
Drug: busulfan
Drug: cyclophosphamide
Drug: cyclosporine
Drug: fludarabine phosphate
Drug: methotrexate
Procedure: allogeneic hematopoietic stem cell transplantation
First Posted Date
2009-11-25
Last Posted Date
2015-12-31
Lead Sponsor
Asan Medical Center
Target Recruit Count
263
Registration Number
NCT01020734
Locations
🇰🇷

Inje University - Haeundae Paik Hospital, Busan, Korea, Republic of

🇰🇷

Asan Medical Center - University of Ulsan College of Medicine, Seoul, Korea, Republic of

Intercontinental Multidisciplinary Registry and Treatment Optimization Study for Choroid Plexus Tumors

First Posted Date
2009-11-17
Last Posted Date
2019-08-20
Lead Sponsor
Tufts Medical Center
Target Recruit Count
27
Registration Number
NCT01014767
Locations
🇳🇿

Christchurch Hospital, Christchurch, New Zealand

🇺🇸

Tufts Medical Center, Boston, Massachusetts, United States

🇭🇺

Semmelweis University, Budapest, Hungary

and more 2 locations

Trial for Patients With Newly Diagnosed Primary Central Nervous System (CNS) Lymphoma

Phase 2
Completed
Conditions
Central Nervous System Lymphoma
Interventions
First Posted Date
2009-11-11
Last Posted Date
2017-08-23
Lead Sponsor
International Extranodal Lymphoma Study Group (IELSG)
Target Recruit Count
126
Registration Number
NCT01011920
Locations
🇨🇭

IOSI - Oncology Institute of Southern Switzerland, Bellinzona, Switzerland

🇮🇹

A.O. SS. Antonio e Biagio e Cesare Arrigo, Alessandria, Italy

🇩🇪

Uniklinik Freiburg, Freiburg, Germany

and more 20 locations
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