Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C20H20N8O5.2Na |
| Molecular Weight | 498.4029 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[Na+].[Na+].CN(CC1=NC2=C(N)N=C(N)N=C2N=C1)C3=CC=C(C=C3)C(=O)N[C@@H](CCC([O-])=O)C([O-])=O
InChI
InChIKey=DASQOOZCTWOQPA-GXKRWWSZSA-L
InChI=1S/C20H22N8O5.2Na/c1-28(9-11-8-23-17-15(24-11)16(21)26-20(22)27-17)12-4-2-10(3-5-12)18(31)25-13(19(32)33)6-7-14(29)30;;/h2-5,8,13H,6-7,9H2,1H3,(H,25,31)(H,29,30)(H,32,33)(H4,21,22,23,26,27);;/q;2*+1/p-2/t13-;;/m0../s1
DescriptionSources: http://www.drugbank.ca/drugs/DB00563Curator's Comment: Description was created based on several sources, including
https://www.drugs.com/methotrexate.html
Sources: http://www.drugbank.ca/drugs/DB00563
Curator's Comment: Description was created based on several sources, including
https://www.drugs.com/methotrexate.html
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.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL202 Sources: http://www.drugbank.ca/drugs/DB00563 |
5.19 pM [Ki] | ||
Target ID: CHEMBL3167 |
0.18 mM [IC50] | ||
Target ID: CHEMBL614580 |
15.0 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | OTREXUP Approved UseOtrexup is a folate analog metabolic inhibitor indicated for the:
• Management of patients with severe, active rheumatoid arthritis (RA) and polyarticular juvenile idiopathic arthritis (pJIA), who are intolerant of or had an inadequate response to first-line therapy
• Symptomatic control of severe, recalcitrant, disabling psoriasis in adults who are not adequately responsive to other forms of therapy Launch Date1952 |
|||
| Primary | TREXALL Approved UseNeoplastic Diseases
Methotrexate, USP is indicated in the treatment of gestational choriocarcinoma, chorioadenoma destruens and hydatidiform mole.
In acute lymphocytic leukemia, methotrexate, USP is indicated in the prophylaxis of meningeal leukemia and is used in maintenance therapy in combination with other chemotherapeutic agents. Methotrexate, USP is also indicated in the treatment of meningeal leukemia.
Methotrexate, USP 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, USP is also used in combination with other chemotherapeutic agents in the treatment of advanced stage non-Hodgkin's lymphomas.
Methotrexate, USP in high doses followed by leucovorin rescue in combination with other chemotherapeutic agents is effective in prolonging relapse-free survival in patients with non-metastatic osteosarcoma who have undergone surgical resection or amputation for the primary tumor.
Psoriasis
Methotrexate, USP is indicated in the symptomatic control of severe, recalcitrant, disabling psoriasis that is not adequately responsive to other forms of therapy, but only when the diagnosis has been established, as by biopsy and/or after dermatologic consultation. It is important to ensure that a psoriasis "flare" is not due to an undiagnosed concomitant disease affecting immune responses.
Rheumatoid Arthritis including Polyarticular-Course Juvenile Rheumatoid Arthritis
Methotrexate, USP is indicated in the management of selected adults with severe, active rheumatoid arthritis (ACR criteria), or children with active polyarticular-course juvenile rheumatoid arthritis, who have had an insufficient therapeutic response to, or are intolerant of, an adequate trial of first-line therapy including full dose non-steroidal anti-inflammatory agents (NSAIDs). Launch Date2001 |
|||
| Primary | TREXALL Approved UseNeoplastic Diseases
Methotrexate, USP is indicated in the treatment of gestational choriocarcinoma, chorioadenoma destruens and hydatidiform mole.
In acute lymphocytic leukemia, methotrexate, USP is indicated in the prophylaxis of meningeal leukemia and is used in maintenance therapy in combination with other chemotherapeutic agents. Methotrexate, USP is also indicated in the treatment of meningeal leukemia.
Methotrexate, USP 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, USP is also used in combination with other chemotherapeutic agents in the treatment of advanced stage non-Hodgkin's lymphomas.
Methotrexate, USP in high doses followed by leucovorin rescue in combination with other chemotherapeutic agents is effective in prolonging relapse-free survival in patients with non-metastatic osteosarcoma who have undergone surgical resection or amputation for the primary tumor.
Psoriasis
Methotrexate, USP is indicated in the symptomatic control of severe, recalcitrant, disabling psoriasis that is not adequately responsive to other forms of therapy, but only when the diagnosis has been established, as by biopsy and/or after dermatologic consultation. It is important to ensure that a psoriasis "flare" is not due to an undiagnosed concomitant disease affecting immune responses.
Rheumatoid Arthritis including Polyarticular-Course Juvenile Rheumatoid Arthritis
Methotrexate, USP is indicated in the management of selected adults with severe, active rheumatoid arthritis (ACR criteria), or children with active polyarticular-course juvenile rheumatoid arthritis, who have had an insufficient therapeutic response to, or are intolerant of, an adequate trial of first-line therapy including full dose non-steroidal anti-inflammatory agents (NSAIDs). Launch Date2001 |
|||
| Primary | TREXALL Approved UseNeoplastic Diseases
Methotrexate, USP is indicated in the treatment of gestational choriocarcinoma, chorioadenoma destruens and hydatidiform mole.
In acute lymphocytic leukemia, methotrexate, USP is indicated in the prophylaxis of meningeal leukemia and is used in maintenance therapy in combination with other chemotherapeutic agents. Methotrexate, USP is also indicated in the treatment of meningeal leukemia.
Methotrexate, USP 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, USP is also used in combination with other chemotherapeutic agents in the treatment of advanced stage non-Hodgkin's lymphomas.
Methotrexate, USP in high doses followed by leucovorin rescue in combination with other chemotherapeutic agents is effective in prolonging relapse-free survival in patients with non-metastatic osteosarcoma who have undergone surgical resection or amputation for the primary tumor.
Psoriasis
Methotrexate, USP is indicated in the symptomatic control of severe, recalcitrant, disabling psoriasis that is not adequately responsive to other forms of therapy, but only when the diagnosis has been established, as by biopsy and/or after dermatologic consultation. It is important to ensure that a psoriasis "flare" is not due to an undiagnosed concomitant disease affecting immune responses.
Rheumatoid Arthritis including Polyarticular-Course Juvenile Rheumatoid Arthritis
Methotrexate, USP is indicated in the management of selected adults with severe, active rheumatoid arthritis (ACR criteria), or children with active polyarticular-course juvenile rheumatoid arthritis, who have had an insufficient therapeutic response to, or are intolerant of, an adequate trial of first-line therapy including full dose non-steroidal anti-inflammatory agents (NSAIDs). Launch Date2001 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1.205 μM |
20 mg/m² single, oral dose: 20 mg/m² route of administration: Oral experiment type: SINGLE co-administered: |
METHOTREXATE plasma | Homo sapiens population: UNHEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
3533 nM × h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/8485020 |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
METHOTREXATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
55 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/8485020 |
15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered: |
METHOTREXATE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
3.25 h |
20 mg/m² single, oral dose: 20 mg/m² route of administration: Oral experiment type: SINGLE co-administered: |
METHOTREXATE plasma | Homo sapiens population: UNHEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
50% |
METHOTREXATE serum | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
75 mg single, oral Overdose |
unknown, 10-19 years n = 1 Health Status: unknown Age Group: 10-19 years Sex: M Population Size: 1 Sources: |
Other AEs: Nausea, Vomiting... |
87.5 mg single, oral Overdose |
unknown, 10-19 years n = 1 Health Status: unknown Age Group: 10-19 years Sex: F Population Size: 1 Sources: |
Other AEs: Nausea, Vomiting... |
50 mg single, oral Overdose |
unknown, 40-49 years n = 1 Health Status: unknown Age Group: 40-49 years Sex: M Population Size: 1 Sources: |
|
3 g/m2 multiple, intravenous Highest studied dose Dose: 3 g/m2 Route: intravenous Route: multiple Dose: 3 g/m2 Co-administed with:: calcium folinate(oral, 50 mg at H24 and pursued this treatment every 6 h during 3 days (until day 4) for a total of 12 administrations) Sources: |
unhealthy, 41 years (range: 17–60 years) n = 103 Health Status: unhealthy Condition: aggressive lymphoma Age Group: 41 years (range: 17–60 years) Sex: M+F Population Size: 103 Sources: |
Disc. AE: Toxicity renal... AEs leading to discontinuation/dose reduction: Toxicity renal (grade 1-2, 2 patients) Sources: |
3 g/m2 multiple, intravenous Highest studied dose Dose: 3 g/m2 Route: intravenous Route: multiple Dose: 3 g/m2 Co-administed with:: (oral, 50 mg at H24 and pursued this treatment every 6 h during 3 days (until day 4) for a total of 12 administrations) Sources: |
unhealthy, 41 years (range: 17–60 years) n = 103 Health Status: unhealthy Condition: aggressive lymphoma Age Group: 41 years (range: 17–60 years) Sex: M+F Population Size: 103 Sources: |
Disc. AE: Cytolysis, Neutropenia... AEs leading to discontinuation/dose reduction: Cytolysis (grade 2-3, 2 patients) Sources: Neutropenia (grade 3, 1 patient) Digestion impaired (grade 3, 1 patient) |
50 mg 1 times / week multiple, oral Overdose Dose: 50 mg, 1 times / week Route: oral Route: multiple Dose: 50 mg, 1 times / week Sources: |
unhealthy, 50-59 years n = 1 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: 50-59 years Sex: F Population Size: 1 Sources: |
Other AEs: Skin lesion, Mucosal ulceration... Other AEs: Skin lesion (1 patient) Sources: Mucosal ulceration (1 patient) Abdominal pain (1 patient) |
10 mg 1 times / week multiple, oral Recommended Dose: 10 mg, 1 times / week Route: oral Route: multiple Dose: 10 mg, 1 times / week Co-administed with:: adalimumab(40 mg per every other week; 3 years) Sources: guratimod(50 mg/day for approximately 3 years.) |
unhealthy, 54 years n = 1 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: 54 years Sex: F Population Size: 1 Sources: |
Disc. AE: Lymphoproliferative disorder... AEs leading to discontinuation/dose reduction: Lymphoproliferative disorder (1 patient) Sources: |
70 mg 1 times / week multiple, oral Overdose Dose: 70 mg, 1 times / week Route: oral Route: multiple Dose: 70 mg, 1 times / week Sources: |
unhealthy, 60-79 years n = 2 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: 60-79 years Sex: F Population Size: 2 Sources: |
Other AEs: Mucosal ulceration... |
17.5 mg 1 times / week multiple, oral Overdose Dose: 17.5 mg, 1 times / week Route: oral Route: multiple Dose: 17.5 mg, 1 times / week Sources: |
unhealthy, 70-79 years n = 1 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: 70-79 years Sex: F Population Size: 1 Sources: |
Other AEs: Mucosal ulceration, Nausea... Other AEs: Mucosal ulceration (1 patient) Sources: Nausea (1 patient) Vomiting (1 patient) Diarrhea (1 patient) Abdominal pain (1 patient) |
10 mg 1 times / day multiple, oral Overdose Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, adult n = 1 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: adult Population Size: 1 Sources: |
Other AEs: Adverse event... |
15 mg 1 times / day multiple, oral Overdose Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Sources: |
unhealthy, adult n = 1 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: adult Population Size: 1 Sources: |
Other AEs: Adverse event... |
2.5 mg 2 times / day multiple, oral Overdose Dose: 2.5 mg, 2 times / day Route: oral Route: multiple Dose: 2.5 mg, 2 times / day Sources: |
unhealthy, adult n = 1 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: adult Population Size: 1 Sources: |
Other AEs: Adverse event... |
25 mg 1 times / week steady, oral Recommended Dose: 25 mg, 1 times / week Route: oral Route: steady Dose: 25 mg, 1 times / week Sources: |
pregnant, adult Health Status: pregnant Age Group: adult Sex: F Sources: |
Other AEs: Fetal damage... Other AEs: Fetal damage (severe|grade 5) Sources: |
25 mg 1 times / week steady, oral Recommended Dose: 25 mg, 1 times / week Route: oral Route: steady Dose: 25 mg, 1 times / week Sources: |
unhealthy, adult Health Status: unhealthy Condition: Mycosis fungoides Age Group: adult Sources: |
Other AEs: Gastrointestinal disorder (NOS), Hepatic and hepatobiliary disorders... Other AEs: Gastrointestinal disorder (NOS) Sources: Hepatic and hepatobiliary disorders (serious) Respiratory tract disorders NEC (serious) Skin and subcutaneous conditions NEC (serious) Kidney disorder (serious) |
7.5 mg 1 times / week steady, subcutaneous Recommended Dose: 7.5 mg, 1 times / week Route: subcutaneous Route: steady Dose: 7.5 mg, 1 times / week Sources: |
pregnant, adult Health Status: pregnant Age Group: adult Sex: F Sources: |
Other AEs: Fetal damage... Other AEs: Fetal damage (severe|grade 5) Sources: |
7.5 mg 1 times / week steady, subcutaneous Recommended Dose: 7.5 mg, 1 times / week Route: subcutaneous Route: steady Dose: 7.5 mg, 1 times / week Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Other AEs: Skin and subcutaneous conditions NEC... Other AEs: Skin and subcutaneous conditions NEC (severe|grade 5) Sources: |
7.5 mg 1 times / week steady, subcutaneous Recommended Dose: 7.5 mg, 1 times / week Route: subcutaneous Route: steady Dose: 7.5 mg, 1 times / week Sources: |
unhealthy, adult Health Status: unhealthy Condition: rheumatoid arthritis Age Group: adult Sources: |
Disc. AE: Interstitial pneumonitis... Other AEs: Hepatic and hepatobiliary disorders, Respiratory tract disorders NEC... AEs leading to discontinuation/dose reduction: Interstitial pneumonitis (serious) Other AEs:Hepatic and hepatobiliary disorders (serious) Sources: Respiratory tract disorders NEC (serious) Skin and subcutaneous conditions NEC (serious) Kidney disorder (serious) |
30 mg 1 times / week multiple, subcutaneous Dose: 30 mg, 1 times / week Route: subcutaneous Route: multiple Dose: 30 mg, 1 times / week Co-administed with:: Nonsteroidal anti-inflammatory drugs Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Other AEs: Bone marrow depression, Aplastic anemia... Other AEs: Bone marrow depression (severe|grade 5) Sources: Aplastic anemia (severe|grade 5) Gastrointestinal toxicity (severe|grade 5) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Nausea | 1 patient | 75 mg single, oral Overdose |
unknown, 10-19 years n = 1 Health Status: unknown Age Group: 10-19 years Sex: M Population Size: 1 Sources: |
| Vomiting | 1 patient | 75 mg single, oral Overdose |
unknown, 10-19 years n = 1 Health Status: unknown Age Group: 10-19 years Sex: M Population Size: 1 Sources: |
| Nausea | 1 patient | 87.5 mg single, oral Overdose |
unknown, 10-19 years n = 1 Health Status: unknown Age Group: 10-19 years Sex: F Population Size: 1 Sources: |
| Vomiting | 1 patient | 87.5 mg single, oral Overdose |
unknown, 10-19 years n = 1 Health Status: unknown Age Group: 10-19 years Sex: F Population Size: 1 Sources: |
| Toxicity renal | grade 1-2, 2 patients Disc. AE |
3 g/m2 multiple, intravenous Highest studied dose Dose: 3 g/m2 Route: intravenous Route: multiple Dose: 3 g/m2 Co-administed with:: calcium folinate(oral, 50 mg at H24 and pursued this treatment every 6 h during 3 days (until day 4) for a total of 12 administrations) Sources: |
unhealthy, 41 years (range: 17–60 years) n = 103 Health Status: unhealthy Condition: aggressive lymphoma Age Group: 41 years (range: 17–60 years) Sex: M+F Population Size: 103 Sources: |
| Cytolysis | grade 2-3, 2 patients Disc. AE |
3 g/m2 multiple, intravenous Highest studied dose Dose: 3 g/m2 Route: intravenous Route: multiple Dose: 3 g/m2 Co-administed with:: (oral, 50 mg at H24 and pursued this treatment every 6 h during 3 days (until day 4) for a total of 12 administrations) Sources: |
unhealthy, 41 years (range: 17–60 years) n = 103 Health Status: unhealthy Condition: aggressive lymphoma Age Group: 41 years (range: 17–60 years) Sex: M+F Population Size: 103 Sources: |
| Digestion impaired | grade 3, 1 patient Disc. AE |
3 g/m2 multiple, intravenous Highest studied dose Dose: 3 g/m2 Route: intravenous Route: multiple Dose: 3 g/m2 Co-administed with:: (oral, 50 mg at H24 and pursued this treatment every 6 h during 3 days (until day 4) for a total of 12 administrations) Sources: |
unhealthy, 41 years (range: 17–60 years) n = 103 Health Status: unhealthy Condition: aggressive lymphoma Age Group: 41 years (range: 17–60 years) Sex: M+F Population Size: 103 Sources: |
| Neutropenia | grade 3, 1 patient Disc. AE |
3 g/m2 multiple, intravenous Highest studied dose Dose: 3 g/m2 Route: intravenous Route: multiple Dose: 3 g/m2 Co-administed with:: (oral, 50 mg at H24 and pursued this treatment every 6 h during 3 days (until day 4) for a total of 12 administrations) Sources: |
unhealthy, 41 years (range: 17–60 years) n = 103 Health Status: unhealthy Condition: aggressive lymphoma Age Group: 41 years (range: 17–60 years) Sex: M+F Population Size: 103 Sources: |
| Abdominal pain | 1 patient | 50 mg 1 times / week multiple, oral Overdose Dose: 50 mg, 1 times / week Route: oral Route: multiple Dose: 50 mg, 1 times / week Sources: |
unhealthy, 50-59 years n = 1 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: 50-59 years Sex: F Population Size: 1 Sources: |
| Mucosal ulceration | 1 patient | 50 mg 1 times / week multiple, oral Overdose Dose: 50 mg, 1 times / week Route: oral Route: multiple Dose: 50 mg, 1 times / week Sources: |
unhealthy, 50-59 years n = 1 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: 50-59 years Sex: F Population Size: 1 Sources: |
| Skin lesion | 1 patient | 50 mg 1 times / week multiple, oral Overdose Dose: 50 mg, 1 times / week Route: oral Route: multiple Dose: 50 mg, 1 times / week Sources: |
unhealthy, 50-59 years n = 1 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: 50-59 years Sex: F Population Size: 1 Sources: |
| Lymphoproliferative disorder | 1 patient Disc. AE |
10 mg 1 times / week multiple, oral Recommended Dose: 10 mg, 1 times / week Route: oral Route: multiple Dose: 10 mg, 1 times / week Co-administed with:: adalimumab(40 mg per every other week; 3 years) Sources: guratimod(50 mg/day for approximately 3 years.) |
unhealthy, 54 years n = 1 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: 54 years Sex: F Population Size: 1 Sources: |
| Mucosal ulceration | 2 patients | 70 mg 1 times / week multiple, oral Overdose Dose: 70 mg, 1 times / week Route: oral Route: multiple Dose: 70 mg, 1 times / week Sources: |
unhealthy, 60-79 years n = 2 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: 60-79 years Sex: F Population Size: 2 Sources: |
| Abdominal pain | 1 patient | 17.5 mg 1 times / week multiple, oral Overdose Dose: 17.5 mg, 1 times / week Route: oral Route: multiple Dose: 17.5 mg, 1 times / week Sources: |
unhealthy, 70-79 years n = 1 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: 70-79 years Sex: F Population Size: 1 Sources: |
| Diarrhea | 1 patient | 17.5 mg 1 times / week multiple, oral Overdose Dose: 17.5 mg, 1 times / week Route: oral Route: multiple Dose: 17.5 mg, 1 times / week Sources: |
unhealthy, 70-79 years n = 1 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: 70-79 years Sex: F Population Size: 1 Sources: |
| Mucosal ulceration | 1 patient | 17.5 mg 1 times / week multiple, oral Overdose Dose: 17.5 mg, 1 times / week Route: oral Route: multiple Dose: 17.5 mg, 1 times / week Sources: |
unhealthy, 70-79 years n = 1 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: 70-79 years Sex: F Population Size: 1 Sources: |
| Nausea | 1 patient | 17.5 mg 1 times / week multiple, oral Overdose Dose: 17.5 mg, 1 times / week Route: oral Route: multiple Dose: 17.5 mg, 1 times / week Sources: |
unhealthy, 70-79 years n = 1 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: 70-79 years Sex: F Population Size: 1 Sources: |
| Vomiting | 1 patient | 17.5 mg 1 times / week multiple, oral Overdose Dose: 17.5 mg, 1 times / week Route: oral Route: multiple Dose: 17.5 mg, 1 times / week Sources: |
unhealthy, 70-79 years n = 1 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: 70-79 years Sex: F Population Size: 1 Sources: |
| Adverse event | grade 5 | 10 mg 1 times / day multiple, oral Overdose Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: |
unhealthy, adult n = 1 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: adult Population Size: 1 Sources: |
| Adverse event | grade 5 | 15 mg 1 times / day multiple, oral Overdose Dose: 15 mg, 1 times / day Route: oral Route: multiple Dose: 15 mg, 1 times / day Sources: |
unhealthy, adult n = 1 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: adult Population Size: 1 Sources: |
| Adverse event | grade 5 | 2.5 mg 2 times / day multiple, oral Overdose Dose: 2.5 mg, 2 times / day Route: oral Route: multiple Dose: 2.5 mg, 2 times / day Sources: |
unhealthy, adult n = 1 Health Status: unhealthy Condition: rheumatoid arthritis Age Group: adult Population Size: 1 Sources: |
| Fetal damage | severe|grade 5 | 25 mg 1 times / week steady, oral Recommended Dose: 25 mg, 1 times / week Route: oral Route: steady Dose: 25 mg, 1 times / week Sources: |
pregnant, adult Health Status: pregnant Age Group: adult Sex: F Sources: |
| Gastrointestinal disorder (NOS) | 25 mg 1 times / week steady, oral Recommended Dose: 25 mg, 1 times / week Route: oral Route: steady Dose: 25 mg, 1 times / week Sources: |
unhealthy, adult Health Status: unhealthy Condition: Mycosis fungoides Age Group: adult Sources: |
|
| Hepatic and hepatobiliary disorders | serious | 25 mg 1 times / week steady, oral Recommended Dose: 25 mg, 1 times / week Route: oral Route: steady Dose: 25 mg, 1 times / week Sources: |
unhealthy, adult Health Status: unhealthy Condition: Mycosis fungoides Age Group: adult Sources: |
| Kidney disorder | serious | 25 mg 1 times / week steady, oral Recommended Dose: 25 mg, 1 times / week Route: oral Route: steady Dose: 25 mg, 1 times / week Sources: |
unhealthy, adult Health Status: unhealthy Condition: Mycosis fungoides Age Group: adult Sources: |
| Respiratory tract disorders NEC | serious | 25 mg 1 times / week steady, oral Recommended Dose: 25 mg, 1 times / week Route: oral Route: steady Dose: 25 mg, 1 times / week Sources: |
unhealthy, adult Health Status: unhealthy Condition: Mycosis fungoides Age Group: adult Sources: |
| Skin and subcutaneous conditions NEC | serious | 25 mg 1 times / week steady, oral Recommended Dose: 25 mg, 1 times / week Route: oral Route: steady Dose: 25 mg, 1 times / week Sources: |
unhealthy, adult Health Status: unhealthy Condition: Mycosis fungoides Age Group: adult Sources: |
| Fetal damage | severe|grade 5 | 7.5 mg 1 times / week steady, subcutaneous Recommended Dose: 7.5 mg, 1 times / week Route: subcutaneous Route: steady Dose: 7.5 mg, 1 times / week Sources: |
pregnant, adult Health Status: pregnant Age Group: adult Sex: F Sources: |
| Skin and subcutaneous conditions NEC | severe|grade 5 | 7.5 mg 1 times / week steady, subcutaneous Recommended Dose: 7.5 mg, 1 times / week Route: subcutaneous Route: steady Dose: 7.5 mg, 1 times / week Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Hepatic and hepatobiliary disorders | serious | 7.5 mg 1 times / week steady, subcutaneous Recommended Dose: 7.5 mg, 1 times / week Route: subcutaneous Route: steady Dose: 7.5 mg, 1 times / week Sources: |
unhealthy, adult Health Status: unhealthy Condition: rheumatoid arthritis Age Group: adult Sources: |
| Kidney disorder | serious | 7.5 mg 1 times / week steady, subcutaneous Recommended Dose: 7.5 mg, 1 times / week Route: subcutaneous Route: steady Dose: 7.5 mg, 1 times / week Sources: |
unhealthy, adult Health Status: unhealthy Condition: rheumatoid arthritis Age Group: adult Sources: |
| Respiratory tract disorders NEC | serious | 7.5 mg 1 times / week steady, subcutaneous Recommended Dose: 7.5 mg, 1 times / week Route: subcutaneous Route: steady Dose: 7.5 mg, 1 times / week Sources: |
unhealthy, adult Health Status: unhealthy Condition: rheumatoid arthritis Age Group: adult Sources: |
| Skin and subcutaneous conditions NEC | serious | 7.5 mg 1 times / week steady, subcutaneous Recommended Dose: 7.5 mg, 1 times / week Route: subcutaneous Route: steady Dose: 7.5 mg, 1 times / week Sources: |
unhealthy, adult Health Status: unhealthy Condition: rheumatoid arthritis Age Group: adult Sources: |
| Interstitial pneumonitis | serious Disc. AE |
7.5 mg 1 times / week steady, subcutaneous Recommended Dose: 7.5 mg, 1 times / week Route: subcutaneous Route: steady Dose: 7.5 mg, 1 times / week Sources: |
unhealthy, adult Health Status: unhealthy Condition: rheumatoid arthritis Age Group: adult Sources: |
| Aplastic anemia | severe|grade 5 | 30 mg 1 times / week multiple, subcutaneous Dose: 30 mg, 1 times / week Route: subcutaneous Route: multiple Dose: 30 mg, 1 times / week Co-administed with:: Nonsteroidal anti-inflammatory drugs Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Bone marrow depression | severe|grade 5 | 30 mg 1 times / week multiple, subcutaneous Dose: 30 mg, 1 times / week Route: subcutaneous Route: multiple Dose: 30 mg, 1 times / week Co-administed with:: Nonsteroidal anti-inflammatory drugs Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Gastrointestinal toxicity | severe|grade 5 | 30 mg 1 times / week multiple, subcutaneous Dose: 30 mg, 1 times / week Route: subcutaneous Route: multiple Dose: 30 mg, 1 times / week Co-administed with:: Nonsteroidal anti-inflammatory drugs Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Cerebral calcifications associated with intrathecal methotrexate therapy in acute lymphocytic leukemia. | 1976 Apr |
|
| Letter: Vasculitis as a complication of high-dose methotrexate in the treatment of acute leukemia. | 1976 Jun |
|
| Toxicity profile of methotrexate in rheumatoid arthritis. A preliminary survey. | 1999 |
|
| Influence of cyclosporin A on radiological progression in early rheumatoid arthritis patients: a 42-month prospective study. | 2000 |
|
| Methotrexate, uracil and tegafur, and leucovorin chemotherapy for patients with breast cancer in progression after high-dose chemotherapy with peripheral blood progenitor cell transplant: a phase II study. | 2000 Dec |
|
| Atrial fibrillation occurring in a patient taking etanercept plus methotrexate for rheumatoid arthritis. | 2000 Dec |
|
| Identification by RNA-based arbitrarily primed PCR of the involvement of cytochrome c oxidase in the development of resistance to methotrexate. | 2000 Feb 28 |
|
| Impotence in a patient with rheumatoid arthritis treated with methotrexate. | 2000 Jul |
|
| Acute stroke-like encephalopathy associated with high-dose methotrexate impurities. | 2000 Jul-Aug |
|
| Veno-occlusive disease of the liver associated with thiopurines in a child with acute lymphoblastic leukemia. | 2000 Jul-Aug |
|
| Cortical laminar necrosis caused by immunosuppressive therapy and chemotherapy. | 2000 Mar |
|
| Serious liver disease in a patient receiving methotrexate and leflunomide. | 2000 Nov |
|
| White matter changes on MRI during treatment in children with acute lymphoblastic leukemia: correlation with neuropsychological findings. | 2000 Nov |
|
| Acute neurotoxicity in children with B-lineage acute lymphoblastic leukemia (B-ALL) treated with intermediate risk protocols. | 2000 Nov |
|
| Toxicity of methotrexate treatment in psoriasis and psoriatic arthritis--short- and long-term toxicity in 104 patients. | 2001 |
|
| [Conservative therapy in endocrine orbitopathy: "State of the art"]. | 2001 |
|
| Stereoselectivity of the folate transporter in rabbit small intestine: studies with amethopterin enantiomers. | 2001 |
|
| Hospital resources used for ectopic pregnancy treatment by laparoscopy and methotrexate. | 2001 Apr-Jun |
|
| Role of non-alcoholic steatohepatitis in methotrexate-induced liver injury. | 2001 Dec |
|
| Transient posterior encephalopathy induced by chemotherapy in children. | 2001 Feb |
|
| [Listeria arthritis in chronic polyarthritis during low dose prednisolone and methotrexate therapy. Case report and review of the literature]. | 2001 Feb |
|
| A comparison of methods of loco-regional chemotherapy combined with systemic chemotherapy as neo-adjuvant treatment of osteosarcoma of the extremity. | 2001 Feb |
|
| Neoadjuvant chemotherapy for high grade osteosarcoma of the extremities: long-term results for patients treated according to the Rizzoli IOR/OS-3b protocol. | 2001 Feb |
|
| Development of fulminant hepatitis B (precore variant mutant type) after the discontinuation of low-dose methotrexate therapy in a rheumatoid arthritis patient. | 2001 Feb |
|
| [Fatal outcome of a multisystemic sarcoidosis in a 54-year-old patient]. | 2001 Jul |
|
| Long-term cerebral metabolite changes on proton magnetic resonance spectroscopy in patients cured of acute lymphoblastic leukemia with previous intrathecal methotrexate and cranial irradiation prophylaxis. | 2001 Jul 1 |
|
| Relationship between dose-intensity of treatment and outcome for patients with osteosarcoma of the extremity treated with neoadjuvant chemotherapy. | 2001 Jul-Aug |
|
| Successful rescue with leucovorin and thymidine in a patient with high-dose methotrexate induced acute renal failure. | 2001 Jun |
|
| Homocysteine modulation as a reason for continuous folic acid supplementation in methotrexate-treated rheumatoid arthritis patients. | 2001 Jun |
|
| Motor nervous pathway function is impaired after treatment of childhood acute lymphoblastic leukemia: a study with motor evoked potentials. | 2001 Mar |
|
| Inappropriate medical management of spinal epidural abscess. | 2001 Mar |
|
| Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney. | 2001 May |
|
| Neoadjuvant chemotherapy for osteosarcoma of the extremity: long-term results of the Rizzoli's 4th protocol. | 2001 Nov |
|
| Tamoxifen-based treatment induces clinically meaningful responses in multiple myeloma patients with relapsing disease after autotransplantation. | 2001 Nov-Dec |
|
| [Meningeal carcinomatosis as the first manifestation of gastric adenocarcinoma]. | 2001 Oct 11 |
|
| Mutation of Trp1254 in the multispecific organic anion transporter, multidrug resistance protein 2 (MRP2) (ABCC2), alters substrate specificity and results in loss of methotrexate transport activity. | 2001 Oct 12 |
|
| Methylation-dependent silencing of the reduced folate carrier gene in inherently methotrexate-resistant human breast cancer cells. | 2001 Oct 26 |
|
| Isolation of rat dihydrofolate reductase gene and characterization of recombinant enzyme. | 2001 Sep |
|
| Multiple anomalies in a fetus exposed to low-dose methotrexate in the first trimester. | 2002 Apr |
|
| Methotrexate-induced nephrogenic diabetes insipidus: first case report. | 2002 Feb |
|
| Methotrexate-induced systemic vasculitis. | 2002 Feb |
|
| Leukemic leptomeningeal involvement in stage 0 and stage 1 chronic lymphocytic leukemia. | 2002 Jan |
|
| Methotrexate-related nonnecrotizing multifocal axonopathy detected by beta-amyloid precursor protein immunohistochemistry. | 2002 Jan |
|
| Isolation, characterization and differential gene expression of multispecific organic anion transporter 2 in mice. | 2002 Jul |
|
| CYP3A4 induction by drugs: correlation between a pregnane X receptor reporter gene assay and CYP3A4 expression in human hepatocytes. | 2002 Jul |
|
| Oral methotrexate for treatment of ectopic pregnancy. | 2002 Jun |
|
| Radiation myelitis in a 5-year-old girl. | 2002 Mar |
|
| [A case of subacute transient cerebral dysfunction in a osteosarcoma patient following high-dose methotrexate]. | 2002 Mar |
|
| Nephrotoxicity due to intermediate-dose methotrexate without rescue in an obese adolescent with acute lymphoblastic leukemia. | 2002 Mar |
|
| Quantitative MRI assessment of leukoencephalopathy. | 2002 May |
Patents
Sample Use Guides
Usual Adult Dose for Acute Lymphoblastic Leukemia
Induction: 3.3 mg/m2/day orally or IM (in combination with prednisone 60 mg/m2) daily
Usual Adult Dose for Psoriasis
Single Dose: 7.5 mg/week orally, IM, or IV until adequate response is achieved
Divided Dose: 2.5 mg orally, IM, or IV every 12 hours for 3 doses once a week
Maximum weekly dose: 20 mg
Route of Administration:
Other
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NCI_THESAURUS |
C2153
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FDA ORPHAN DRUG |
9985
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NCI_THESAURUS |
C511
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7413-34-5
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SUB03225MIG
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3IG1E710ZN
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C1735
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Methotrexate sodium
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50679
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15475-56-6
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44185
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287734
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11329481
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DBSALT000115
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SUB16442MIG
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231-022-0
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CHEMBL34259
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m7327
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DTXSID3037123
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239-495-5
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100000078565
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3IG1E710ZN
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ACTIVE MOIETY
SUBSTANCE RECORD
