Active Ingredient History
Methotrexate is an antineoplastic anti-metabolite. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the "S" phase (of the cell cycle), stopping normal development and division. Methotrexate inhibits folic acid reductase which is responsible for the conversion of folic acid to tetrahydrofolic acid. At two stages in the biosynthesis of purines and at one stage in the synthesis of pyrimidines, one-carbon transfer reactions occur which require specific coenzymes synthesized in the cell from tetrahydrofolic acid. Tetrahydrofolic acid itself is synthesized in the cell from folic acid with the help of an enzyme, folic acid reductase. Methotrexate looks a lot like folic acid to the enzyme, so it binds to it quite strongly and inhibits the enzyme. Thus, DNA synthesis cannot proceed because the coenzymes needed for one-carbon transfer reactions are not produced from tetrahydrofolic acid because there is no tetrahydrofolic acid. Methotrexate selectively affects the most rapidly dividing cells (neoplastic and psoriatic cells). Methotrexate is indicated in the treatment of gestational choriocarcinoma, chorioadenoma destruens and hydatidiform mole. In acute lymphocytic leukemia, methotrexate is indicated in the prophylaxis of meningeal leukemia and is used in maintenance therapy in combination with other chemotherapeutic agents. Methotrexate is also indicated in the treatment of meningeal leukemia. Methotrexate is used alone or in combination with other anticancer agents in the treatment of breast cancer, epidermoid cancers of the head and neck, advanced mycosis fungoides (cutaneous T cell lymphoma), and lung cancer, particularly squamous cell and small cell types. Methotrexate is also used in combination with other chemotherapeutic agents in the treatment of advanced stage non-Hodgkin’s lymphomas. Methotrexate is indicated in the symptomatic control of severe, recalcitrant, disabling psoriasis. Methotrexate is indicated in the management of selected adults with severe, active rheumatoid arthritis (ACR criteria), or children with active polyarticular-course juvenile rheumatoid arthritis. NCATS
Drug Pricing (per unit)
Note: This drug pricing data is preliminary, incomplete, and may contain errors.
Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
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Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
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Arthritis, Rheumatoid (approved 1952)
Breast Neoplasms (approved 2001)
Choriocarcinoma (approved 2001)
Lung Neoplasms (approved 2001)
Adalimumab (Phase 4)
Allogeneic Cells (Phase 3)
Anemia (Phase 2)
Anemia, Aplastic (Phase 3)
Anemia, Diamond-Blackfan (Phase 2)
Anterior Wall Myocardial Infarction (Phase 2/Phase 3)
Arthralgia (Phase 2)
Arthritis (Phase 3)
Arthritis, Juvenile (Phase 3)
Arthritis, Psoriatic (Phase 4)
Arthritis, Rheumatoid (Phase 4)
Ascites (Phase 1/Phase 2)
Atherosclerosis (Phase 2/Phase 3)
Autoimmune Diseases (Phase 3)
Axial Spondyloarthritis (Phase 4)
Azathioprine (Phase 3)
beta-Thalassemia (Phase 4)
Bevacizumab (Phase 1/Phase 2)
Biomarkers (Phase 2)
Bone Marrow Cells (Phase 2)
Bone Marrow Failure Disorders (Phase 2)
Brain Diseases (Phase 1)
Brain Neoplasms (Phase 3)
Breast Neoplasms (Phase 3)
Burkitt Lymphoma (Phase 4)
Carcinoma, Non-Small-Cell Lung (Phase 2)
Carcinoma, Transitional Cell (Phase 3)
Castleman Disease (Phase 1)
Chronic Urticaria (Phase 3)
Colorectal Neoplasms (Phase 2)
Conjunctivitis (Phase 2)
Coronary Artery Disease (Phase 2/Phase 3)
Coronavirus (Phase 1/Phase 2)
COVID-19 (Phase 3)
Crohn Disease (Phase 4)
Dermatitis, Atopic (Phase 4)
Dermatology (Phase 2)
Dermatomyositis (Phase 2)
Diabetic Retinopathy (Early Phase 1)
Down Syndrome (Phase 3)
Drug Interactions (Phase 1)
Drugs, Investigational (Phase 4)
Endothelial Cells (Phase 4)
Eye Diseases, Hereditary (Phase 1)
Fusion Proteins, bcr-abl (Phase 2)
General Surgery (Phase 3)
Gestational Trophoblastic Disease (Phase 3)
Giant Cell Arteritis (Phase 3)
Glycogen Storage Disease Type II (Phase 3)
Gout (Phase 4)
Graft vs Host Disease (Phase 4)
Granulomatosis with Polyangiitis (Phase 4)
Head and Neck Neoplasms (Phase 3)
Healthy Volunteers (Phase 1)
Heart Disease Risk Factors (Phase 4)
Heart Diseases (Phase 3)
Hematologic Diseases (Phase 1/Phase 2)
Hematologic Neoplasms (Phase 2)
Hematopoietic Stem Cell Transplantation (Phase 4)
Hemoglobinuria, Paroxysmal (Phase 2)
Hodgkin Disease (Phase 3)
Hydatidiform Mole (Phase 3)
Hypophosphatasia (Phase 4)
Immunosuppression Therapy (Phase 4)
Inflammation (Phase 2/Phase 3)
Infliximab (Phase 4)
Influenza, Human (Phase 3)
Intraocular Lymphoma (Phase 2)
Leukemia (Phase 3)
Leukemia, Biphenotypic, Acute (Phase 2)
Leukemia, Large Granular Lymphocytic (Phase 2/Phase 3)
Leukemia, Lymphocytic, Chronic, B-Cell (Phase 2)
Leukemia, Lymphoid (Phase 1)
Leukemia-Lymphoma, Adult T-Cell (Phase 1/Phase 2)
Leukemia, Myeloid (Phase 2)
Leukemia, Myeloid, Acute (Phase 3)
Leukemia, Myeloid, Chronic-Phase (Phase 3)
Leukemia, Myelomonocytic, Chronic (Phase 1/Phase 2)
Leukemia, T-Cell (Phase 2/Phase 3)
Lung Diseases (Phase 4)
Lung Diseases, Interstitial (Phase 4)
Lupus Erythematosus, Systemic (Phase 2)
Lymphoma (Phase 4)
Lymphoma, B-Cell (Phase 3)
Lymphoma, Extranodal NK-T-Cell (Phase 1/Phase 2)
Lymphoma, Follicular (Phase 1/Phase 2)
Lymphoma, Large B-Cell, Diffuse (Phase 4)
Lymphoma, Large-Cell, Anaplastic (Phase 3)
Lymphoma, Large-Cell, Immunoblastic (Phase 4)
Lymphoma, Mantle-Cell (Phase 3)
Lymphoma, Non-Hodgkin (Phase 4)
Lymphoma, T-Cell (Phase 3)
Lymphoma, T-Cell, Peripheral (Phase 2)
Medulloblastoma (Phase 2)
Melanoma (Phase 2)
Membranes (Phase 2)
Meningeal Carcinomatosis (Phase 3)
Metabolic Syndrome (Phase 4)
Methotrexate (Phase 4)
Mucopolysaccharidoses (Phase 4)
Mucopolysaccharidosis II (Phase 4)
Multiple Sclerosis (Phase 2)
Mutation (Phase 2)
Myelodysplastic Syndromes (Phase 3)
Myeloproliferative Disorders (Phase 2)
Nasal Polyps (Phase 2)
Natural Killer T-Cells (Phase 2/Phase 3)
Neoadjuvant Therapy (Phase 2)
Neoplasm Metastasis (Phase 4)
Neoplasms (Phase 2)
Neoplasms, Connective and Soft Tissue (Phase 2/Phase 3)
Neoplasms, Connective Tissue (Phase 2/Phase 3)
Neuroblastoma (Phase 2)
Only Child (Phase 4)
Organ Transplantation (Phase 3)
Osteoarthritis (Phase 4)
Osteosarcoma (Phase 2/Phase 3)
Pain (Phase 4)
Pemphigoid, Bullous (Phase 4)
Pemphigus (Phase 2)
Plasmacytoma (Phase 2)
Pregnancy Complications (Phase 4)
Pregnancy, Ectopic (Phase 1/Phase 2)
Primary Myelofibrosis (Phase 2)
Prostatic Neoplasms (Phase 3)
Psoriasis (Phase 4)
Radiotherapy (Phase 1/Phase 2)
Rectal Neoplasms (Phase 1/Phase 2)
Retinitis Pigmentosa (Phase 2)
Rheumatic Diseases (Phase 4)
Sarcoidosis (Phase 3)
Sarcoidosis, Pulmonary (Phase 4)
Sarcoma (Phase 2/Phase 3)
Schizophrenia (Phase 2)
Sclerosis (Phase 2)
Shwachman-Diamond Syndrome (Phase 2)
Spondylitis, Ankylosing (Phase 4)
Squamous Cell Carcinoma of Head and Neck (Phase 3)
Substance Withdrawal Syndrome (Phase 3)
Survival (Phase 2)
Takayasu Arteritis (Phase 4)
Testicular Neoplasms (Phase 3)
Therapeutics (Phase 4)
Thyroid Gland (Phase 2)
Translocation, Genetic (Phase 2)
Ureteral Neoplasms (Phase 3)
Urethral Neoplasms (Phase 3)
Urinary Bladder Neoplasms (Phase 3)
Uveitis (Phase 3)
Uveitis, Anterior (Phase 4)
Uveitis, Intermediate (Phase 1/Phase 2)
Uveitis, Posterior (Phase 1/Phase 2)
Vaccines (Phase 3)
Vascular Stiffness (Phase 4)
Ventricular Remodeling (Phase 2/Phase 3)
Vitiligo (Phase 4)
Vitreoretinopathy, Proliferative (Phase 3)
Vitreous Body (Early Phase 1)
Trial | Phase | Start Date | Organizations | Indications |
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