Details
Stereochemistry | ACHIRAL |
Molecular Formula | C12H9F3N2O2 |
Molecular Weight | 270.2073 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 1 |
Charge | 0 |
Stereo Comments | Teriflunomide then can interconvert between the E and Z enolic forms (and the corresponding keto-amide), with the Z-enol being the most stable and therefore most predominant form (https://en.wikipedia.org/wiki/Leflunomide) |
SHOW SMILES / InChI
SMILES
C\C(O)=C(/C#N)C(=O)NC1=CC=C(C=C1)C(F)(F)F
InChI
InChIKey=UTNUDOFZCWSZMS-YFHOEESVSA-N
InChI=1S/C12H9F3N2O2/c1-7(18)10(6-16)11(19)17-9-4-2-8(3-5-9)12(13,14)15/h2-5,18H,1H3,(H,17,19)/b10-7-
Molecular Formula | C12H9F3N2O2 |
Molecular Weight | 270.2073 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 1 |
Optical Activity | NONE |
DescriptionSources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020905s031lbl.pdfhttp://www.accessdata.fda.gov/drugsatfda_docs/label/2016/202992s003lbl.pdfCurator's Comment: description was created based on several sources, including
https://clinicaltrials.gov/ct2/show/NCT00622700?term=teriflunomide&rank=8
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020905s031lbl.pdfhttp://www.accessdata.fda.gov/drugsatfda_docs/label/2016/202992s003lbl.pdf
Curator's Comment: description was created based on several sources, including
https://clinicaltrials.gov/ct2/show/NCT00622700?term=teriflunomide&rank=8
Teriflunomide (trade name Aubagio, marketed by Sanofi) is the active metabolite of leflunomide and it acts as an immunomodulatory agent by inhibiting pyrimidine synthesis by blocking the enzyme dihydroorotate dehydrogenase. Teriflunomide was investigated in the Phase III clinical trial TEMSO as a medication for multiple sclerosis (MS). The drug was approved by the FDA on September 13, 2012 and in the European Union on August 26, 2013. It is uncertain whether this explains its effect on MS lesions. Teriflunomide inhibits rapidly dividing cells, including activated T cells, which are thought to drive the disease process in MS. Teriflunomide may decrease the risk of infections compared to chemotherapy-like drugs because of its more-limited effects on the immune system. It has been found that teriflunomide blocks the transcription factor NF-κB. It also inhibits tyrosine kinase enzymes, but only in high doses not clinically used.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/?term=23637535http://www.ncbi.nlm.nih.gov/pubmed/?term=18782502
Curator's Comment: Has only limited penetration across the blood–brain barrier
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: Q02127 Gene ID: 1723.0 Gene Symbol: DHODH Target Organism: Homo sapiens (Human) |
160.0 nM [Ki] | ||
Target ID: CHEMBL1966 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9666414 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | AUBAGIO Approved UseIndicated for the treatment of patients with relapsing forms of multiple sclerosis. Launch Date1.34740797E12 |
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Palliative | ARAVA Approved UseLeflunomide is indicated in adults for the treatment of active rheumatoid arthritis (RA): to reduce signs and symptoms to inhibit structural damage as evidenced by X-ray erosions and joint space narrowing to improve physical function (see CLINICAL STUDIES ). Aspirin, nonsteroidal anti-inflammatory agents and/or low dose corticosteroids may be continued during treatment with leflunomide (see PRECAUTIONS: Drug Interactions: NSAIDs ). The combined use of leflunomide with antimalarials, intramuscular or oral gold, D penicillamine, azathioprine, or methotrexate has not been adequately studied (see WARNINGS: Immunosuppression Potential/Bone Marrow Suppression ). Launch Date9.0538561E11 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.06 μg/mL |
7 mg single, oral dose: 7 mg route of administration: Oral experiment type: SINGLE co-administered: |
TERIFLUNOMIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
100 μg × h/mL |
7 mg single, oral dose: 7 mg route of administration: Oral experiment type: SINGLE co-administered: |
TERIFLUNOMIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
243 h |
7 mg single, oral dose: 7 mg route of administration: Oral experiment type: SINGLE co-administered: |
TERIFLUNOMIDE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1% |
TERIFLUNOMIDE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
14 mg 1 times / day multiple, oral Recommended Dose: 14 mg, 1 times / day Route: oral Route: multiple Dose: 14 mg, 1 times / day Sources: Page: p.923 |
unhealthy, 36 n = 250 Health Status: unhealthy Condition: Multiple sclerosis Age Group: 36 Sex: M+F Population Size: 250 Sources: Page: p.923 |
Disc. AE: ALT increased, Hepatic enzyme increased... AEs leading to discontinuation/dose reduction: ALT increased (3.6%) Sources: Page: p.923Hepatic enzyme increased (0.4%) |
14 mg 1 times / day multiple, oral Recommended Dose: 14 mg, 1 times / day Route: oral Route: multiple Dose: 14 mg, 1 times / day Sources: Page: p.8,9 |
unhealthy, 37 Health Status: unhealthy Condition: Multiple sclerosis Age Group: 37 Sex: M+F Sources: Page: p.8,9 |
Disc. AE: ALT increased... AEs leading to discontinuation/dose reduction: ALT increased (2.6%) Sources: Page: p.8,9 |
14 mg 1 times / day multiple, oral Recommended Dose: 14 mg, 1 times / day Route: oral Route: multiple Dose: 14 mg, 1 times / day Sources: Page: p.2781 |
unhealthy, 37.8 ± 9.7 n = 43 Health Status: unhealthy Condition: Multiple sclerosis Age Group: 37.8 ± 9.7 Sex: M+F Population Size: 43 Sources: Page: p.2781 |
Disc. AE: ALT increased, AST increased... AEs leading to discontinuation/dose reduction: ALT increased (4.7%) Sources: Page: p.2781AST increased (4.7%) Neutropenia (4.7%) |
672 mg single, oral Overdose |
unknown |
|
14 mg 1 times / day multiple, oral Recommended Dose: 14 mg, 1 times / day Route: oral Route: multiple Dose: 14 mg, 1 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Multiple sclerosis Sources: Page: p.1 |
Disc. AE: Hepatotoxicity, Liver injury... AEs leading to discontinuation/dose reduction: Hepatotoxicity Sources: Page: p.1Liver injury (severe) Liver failure (grade 5) Disorder fetal |
14 mg 1 times / day multiple, oral Recommended Dose: 14 mg, 1 times / day Route: oral Route: multiple Dose: 14 mg, 1 times / day Sources: Page: p.7 |
unhealthy Health Status: unhealthy Condition: Multiple sclerosis Sources: Page: p.7 |
Disc. AE: Peripheral neuropathy... AEs leading to discontinuation/dose reduction: Peripheral neuropathy (1.9%) Sources: Page: p.7 |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Hepatic enzyme increased | 0.4% Disc. AE |
14 mg 1 times / day multiple, oral Recommended Dose: 14 mg, 1 times / day Route: oral Route: multiple Dose: 14 mg, 1 times / day Sources: Page: p.923 |
unhealthy, 36 n = 250 Health Status: unhealthy Condition: Multiple sclerosis Age Group: 36 Sex: M+F Population Size: 250 Sources: Page: p.923 |
ALT increased | 3.6% Disc. AE |
14 mg 1 times / day multiple, oral Recommended Dose: 14 mg, 1 times / day Route: oral Route: multiple Dose: 14 mg, 1 times / day Sources: Page: p.923 |
unhealthy, 36 n = 250 Health Status: unhealthy Condition: Multiple sclerosis Age Group: 36 Sex: M+F Population Size: 250 Sources: Page: p.923 |
ALT increased | 2.6% Disc. AE |
14 mg 1 times / day multiple, oral Recommended Dose: 14 mg, 1 times / day Route: oral Route: multiple Dose: 14 mg, 1 times / day Sources: Page: p.8,9 |
unhealthy, 37 Health Status: unhealthy Condition: Multiple sclerosis Age Group: 37 Sex: M+F Sources: Page: p.8,9 |
ALT increased | 4.7% Disc. AE |
14 mg 1 times / day multiple, oral Recommended Dose: 14 mg, 1 times / day Route: oral Route: multiple Dose: 14 mg, 1 times / day Sources: Page: p.2781 |
unhealthy, 37.8 ± 9.7 n = 43 Health Status: unhealthy Condition: Multiple sclerosis Age Group: 37.8 ± 9.7 Sex: M+F Population Size: 43 Sources: Page: p.2781 |
AST increased | 4.7% Disc. AE |
14 mg 1 times / day multiple, oral Recommended Dose: 14 mg, 1 times / day Route: oral Route: multiple Dose: 14 mg, 1 times / day Sources: Page: p.2781 |
unhealthy, 37.8 ± 9.7 n = 43 Health Status: unhealthy Condition: Multiple sclerosis Age Group: 37.8 ± 9.7 Sex: M+F Population Size: 43 Sources: Page: p.2781 |
Neutropenia | 4.7% Disc. AE |
14 mg 1 times / day multiple, oral Recommended Dose: 14 mg, 1 times / day Route: oral Route: multiple Dose: 14 mg, 1 times / day Sources: Page: p.2781 |
unhealthy, 37.8 ± 9.7 n = 43 Health Status: unhealthy Condition: Multiple sclerosis Age Group: 37.8 ± 9.7 Sex: M+F Population Size: 43 Sources: Page: p.2781 |
Disorder fetal | Disc. AE | 14 mg 1 times / day multiple, oral Recommended Dose: 14 mg, 1 times / day Route: oral Route: multiple Dose: 14 mg, 1 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Multiple sclerosis Sources: Page: p.1 |
Hepatotoxicity | Disc. AE | 14 mg 1 times / day multiple, oral Recommended Dose: 14 mg, 1 times / day Route: oral Route: multiple Dose: 14 mg, 1 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Multiple sclerosis Sources: Page: p.1 |
Liver failure | grade 5 Disc. AE |
14 mg 1 times / day multiple, oral Recommended Dose: 14 mg, 1 times / day Route: oral Route: multiple Dose: 14 mg, 1 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Multiple sclerosis Sources: Page: p.1 |
Liver injury | severe Disc. AE |
14 mg 1 times / day multiple, oral Recommended Dose: 14 mg, 1 times / day Route: oral Route: multiple Dose: 14 mg, 1 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Multiple sclerosis Sources: Page: p.1 |
Peripheral neuropathy | 1.9% Disc. AE |
14 mg 1 times / day multiple, oral Recommended Dose: 14 mg, 1 times / day Route: oral Route: multiple Dose: 14 mg, 1 times / day Sources: Page: p.7 |
unhealthy Health Status: unhealthy Condition: Multiple sclerosis Sources: Page: p.7 |
PubMed
Title | Date | PubMed |
---|---|---|
Vasculitis occurring during leflunomide therapy. | 2001 |
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The heterotopic tracheal allograft as an animal model of obliterative bronchiolitis. | 2001 |
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A clinical and economic review of disease-modifying antirheumatic drugs. | 2001 |
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A randomized, controlled, single-blind trial of leflunomide in the treatment of rheumatoid arthritis. | 2001 |
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New therapeutic approaches to the management of rheumatoid arthritis. | 2001 |
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Slowing of disease progression in rheumatoid arthritis patients during long-term treatment with leflunomide or sulfasalazine. | 2001 |
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Leflunomide and rheumatoid arthritis: new preparation. Neither the safest nor the most effective slow-acting antirheumatic drug. | 2001 Apr |
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Novel therapies in the treatment of systemic lupus erythematosus. | 2001 Aug |
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[Leflunomide plus methotrexate. Hope for patients with rheumatoid arthritis]. | 2001 Aug 23 |
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Leflunomide-mediated suppression of antiviral antibody and Tcell responses: differential restoration by uridine. | 2001 Aug 27 |
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[New basic therapeutic drugs from the viewpoint of evidence-based therapy]. | 2001 Dec |
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[Evidence-based medicine and applying new therapies in general practice: wish and reality]. | 2001 Dec |
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Progress in the treatment of rheumatoid arthritis. | 2001 Dec 12 |
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Leflunomide Aventis Pharma. | 2001 Feb |
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Discussion. Treatment algorithm: managing rheumatoid arthritis. | 2001 Jul |
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Economic and quality-of-life impact of rheumatoid arthritis. | 2001 Jul |
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Beneficial effects of leflunomide in glucocorticoid- and methotrexate-resistant Takayasu's arteritis. | 2001 Jul-Aug |
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Hamster cardiac xenografts are protected against antibody mediated damage, early after transplantation to Lewis rats. | 2001 Nov |
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Rationally designed anti-mitotic agents with pro-apoptotic activity. | 2001 Nov |
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[Leflunomide--a new disease modifying anti-rheumatic agent]. | 2001 Nov 10 |
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Inhibition of angiogenesis-related endothelial activity by the experimental immunosuppressive agent leflunomide. | 2001 Nov 15 |
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Use of leflunomide in human renal transplantation. | 2001 Nov 27 |
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Severe liver damage with leflunomide. | 2001 Oct |
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[New therapy developments in rheumatoid arthritis]. | 2001 Oct |
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Platelet-derived growth factor receptors: a therapeutic target in solid tumors. | 2001 Oct |
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Current and emerging lupus treatments. | 2001 Oct |
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Leflunomide for the treatment of systemic lupus erythematosus: comment on the article by McMurray. | 2001 Oct |
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Treatment of active rheumatoid arthritis with leflunomide: two year follow up of a double blind, placebo controlled trial versus sulfasalazine. | 2001 Oct |
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Inhibition of HIV replication by A77 1726, the active metabolite of leflunomide, in combination with pyrimidine nucleoside reverse transcriptase inhibitors. | 2001 Oct 1 |
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Is there a place for leflunomide in the treatment of rheumatoid arthritis? | 2001 Oct 13 |
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Nerve injury proximal or distal to the DRG induces similar spinal glial activation and selective cytokine expression but differential behavioral responses to pharmacologic treatment. | 2001 Oct 15 |
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Comparison of rheumatoid arthritis care costs in patients starting therapy with leflunomide versus etanercept. | 2001 Sep |
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Two-year, blinded, randomized, controlled trial of treatment of active rheumatoid arthritis with leflunomide compared with methotrexate. Utilization of Leflunomide in the Treatment of Rheumatoid Arthritis Trial Investigator Group. | 2001 Sep |
|
Etanercept therapy for immune-mediated cochleovestibular disorders: preliminary results in a pilot study. | 2001 Sep |
|
[Rheumatic pain]. | 2001 Sep |
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Improved functional ability in patients with rheumatoid arthritis--longterm treatment with leflunomide versus sulfasalazine. European Leflunomide Study Group. | 2001 Sep |
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Suppression of experimental autoimmune neuritis by leflunomide. | 2001 Sep |
|
Modulation of inducible nitric oxide synthase activation by immunosuppressive drugs. | 2001 Sep |
|
[Treatment of rheumatoid arthritis by inhibition of tumor necrosis factor with infliximab or etanercept]. | 2001 Sep 29 |
|
Leflunomide metabolite analogue alpha-cyano-beta-hydroxy-beta-methyl-N-[3-(trifluoromethyl)phenyl]propenamide inhibits IgE/FcepsilonRI receptor-mediated mast cell leukotriene release and allergic asthma in mice. | 2001 Sep-Oct |
|
Treating rheumatoid arthritis with new disease modifying drugs. | 2002 |
|
Economic comparison of leflunomide and methotrexate in patients with rheumatoid arthritis: an evaluation based on a 1-year randomised controlled trial. | 2002 |
|
Treatment of severe psoriasis and psoriatic arthritis with leflunomide. | 2002 Feb |
|
Comparative assessment of leflunomide and methotrexate for the treatment of rheumatoid arthritis, by dynamic enhanced magnetic resonance imaging. | 2002 Feb |
|
Experiences with leflunomide in solid organ transplantation. | 2002 Feb 15 |
|
[Treatment of cutaneous leishmaniasis--an update]. | 2002 Jan |
|
Leflunomide induced fevers, thrombocytosis, and leukocytosis in a patient with relapsing polychondritis. | 2002 Jan |
|
Effect of hemodialysis on leflunomide plasma concentrations. | 2002 Jan |
|
Update on the treatment of systemic lupus erythematosus: therapeutic highlights from the Sixth International Lupus Conference. | 2002 Jan |
|
Current treatment of juvenile rheumatoid arthritis. | 2002 Jan |
Patents
Sample Use Guides
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17764417
Cell cultures were inoculated with feline herpesvirus-1 (FHV-1) and treated simultaneously with concentrations of A77 (active metabolite of leflunomide, A77 1726) ranging from 0 to 200 uM. Concentrations of A77 > or = 20 uM were associated with substantial reduction in plaque number and viral load. Concentrations > or = 100 uM were associated with complete suppression of plaque formation. At low concentrations of A77, clusters of intracytoplasmic virus particles that appeared to lack tegument and an external membrane were detected.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 16 17:58:24 UTC 2022
by
admin
on
Fri Dec 16 17:58:24 UTC 2022
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Record UNII |
1C058IKG3B
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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LIVERTOX |
NBK548525
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WHO-VATC |
QL04AA31
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NCI_THESAURUS |
C471
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EMA ASSESSMENT REPORTS |
AUBAGIO (AUTHORIZED: MULTIPLE SCLEROSIS)
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NDF-RT |
N0000185502
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WHO-ATC |
L04AA31
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DB08880
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68540
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54684141
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SUB25218
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1357056
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C527525
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TERIFLUNOMIDE
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YY-88
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1C058IKG3B
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Teriflunomide
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7761
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N0000185501
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PRIMARY | Dihydroorotate Dehydrogenase Inhibitors [MoA] | ||
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M10578
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CHEMBL973
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108605-62-5
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C76662
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1C058IKG3B
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1310520
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PRIMARY | RxNorm | ||
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DTXSID301043028
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163451-81-8
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Related Record | Type | Details | ||
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METABOLIC ENZYME -> NON-SUBSTRATE | |||
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METABOLIC ENZYME -> NON-SUBSTRATE | |||
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EXCRETED UNCHANGED |
FECAL
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TRANSPORTER -> INHIBITOR |
Terifluniomide is an inhibitor of BCRP, OAT3, OATP1B1, OCT2 in vitro
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TRANSPORTER -> INHIBITOR |
Terifluniomide is an inhibitor of BCRP, OAT3, OATP1B1, OCT2 in vitro
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EXCRETED UNCHANGED |
URINE
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TRANSPORTER -> INHIBITOR |
Terifluniomide is an inhibitor of BCRP, OAT3, OATP1B1, OCT2 in vitro
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TARGET -> INHIBITOR |
INHIBITOR
IC50
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METABOLIC ENZYME -> NON-SUBSTRATE | |||
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METABOLIC ENZYME -> NON-SUBSTRATE | |||
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METABOLIC ENZYME -> NON-SUBSTRATE | |||
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METABOLIC ENZYME -> NON-SUBSTRATE | |||
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TRANSPORTER -> INHIBITOR |
Terifluniomide is an inhibitor of BCRP, OAT3, OATP1B1, OCT2 in vitro
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TRANSPORTER -> SUBSTRATE |
Teriflunomide is a substrate of BCRP in vitro
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METABOLIC ENZYME -> NON-SUBSTRATE | |||
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METABOLIC ENZYME -> NON-SUBSTRATE | |||
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BINDER->LIGAND |
BINDING
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METABOLIC ENZYME -> NON-SUBSTRATE | |||
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METABOLIC ENZYME -> NON-SUBSTRATE |
Related Record | Type | Details | ||
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METABOLITE -> PARENT | |||
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METABOLITE -> PARENT | |||
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METABOLITE -> PARENT |
MINOR
URINE
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METABOLITE -> PARENT |
MINOR
URINE
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METABOLITE -> PARENT | |||
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METABOLITE -> PARENT |
MINOR
URINE
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METABOLITE -> PARENT |
4-TFMA was not detected in the single dose metabolism study, but was detected in very small amount after repeated dosing in clinical trials 4-TFMA plasma concentrations were measurable at relatively low concentrations after repeated teriflunomide doses of 7 mg (?1.7 ng/mL) and 14 mg (?5.31 ng/mL) for 468 weeks.
MINOR
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PRODRUG -> METABOLITE ACTIVE |
Related Record | Type | Details | ||
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PARENT -> IMPURITY |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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DOSE |
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Tmax | PHARMACOKINETIC |
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ORAL ADMINISTRATION |
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