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 Date2012 |
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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 Date1998 |
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: |
unhealthy, 36 |
Disc. AE: ALT increased, Hepatic enzyme increased... AEs leading to discontinuation/dose reduction: ALT increased (3.6%) Sources: Hepatic 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: |
unhealthy, 37 Health Status: unhealthy Age Group: 37 Sex: M+F Sources: |
Disc. AE: ALT increased... AEs leading to discontinuation/dose reduction: ALT increased (2.6%) Sources: |
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: |
unhealthy, 37.8 ± 9.7 Health Status: unhealthy Age Group: 37.8 ± 9.7 Sex: M+F Sources: |
Disc. AE: ALT increased, AST increased... AEs leading to discontinuation/dose reduction: ALT increased (4.7%) Sources: AST 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: |
unhealthy Health Status: unhealthy Sources: |
Disc. AE: Hepatotoxicity, Liver injury... AEs leading to discontinuation/dose reduction: Hepatotoxicity Sources: Liver 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: |
unhealthy Health Status: unhealthy Sources: |
Disc. AE: Peripheral neuropathy... AEs leading to discontinuation/dose reduction: Peripheral neuropathy (1.9%) Sources: |
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: |
unhealthy, 36 |
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: |
unhealthy, 36 |
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: |
unhealthy, 37 Health Status: unhealthy Age Group: 37 Sex: M+F Sources: |
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: |
unhealthy, 37.8 ± 9.7 Health Status: unhealthy Age Group: 37.8 ± 9.7 Sex: M+F Sources: |
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: |
unhealthy, 37.8 ± 9.7 Health Status: unhealthy Age Group: 37.8 ± 9.7 Sex: M+F Sources: |
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: |
unhealthy, 37.8 ± 9.7 Health Status: unhealthy Age Group: 37.8 ± 9.7 Sex: M+F Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
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: |
unhealthy Health Status: unhealthy Sources: |
PubMed
Title | Date | PubMed |
---|---|---|
Differential modulation of pro- and anti-inflammatory cytokine receptors by N-(4-trifluoromethylphenyl)-2-cyano-3-hydroxy-crotonic acid amide (A77 1726), the physiologically active metabolite of the novel immunomodulator leflunomide. | 1998 May 1 |
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Structural and functional comparison of agents interfering with dihydroorotate, succinate and NADH oxidation of rat liver mitochondria. | 1998 Oct 15 |
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Leflunomide, a novel immunomodulator for the treatment of active rheumatoid arthritis. | 1999 Nov |
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The use of leflunomide in the treatment of rheumatoid arthritis: an experimental and clinical review. | 2000 May |
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Leflunomide: an immunomodulatory drug for the treatment of rheumatoid arthritis and other autoimmune diseases. | 2000 May |
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Leflunomide: mode of action in the treatment of rheumatoid arthritis. | 2000 Nov |
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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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Slowing of disease progression in rheumatoid arthritis patients during long-term treatment with leflunomide or sulfasalazine. | 2001 |
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Bone loss. Therapeutic approaches for preventing bone loss in inflammatory arthritis. | 2001 |
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A multi-institutional phase ii study of SU101, a platelet-derived growth factor receptor inhibitor, for patients with hormone-refractory prostate cancer. | 2001 Apr |
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The Saccharomyces cerevisiae MLF6/YPL244C gene, which encodes a possible yeast homologue of mammalian UDP-galactose transporter, confers resistance to the immunosuppressive drug, leflunomide. | 2001 Aug |
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[Evidence-based medicine and applying new therapies in general practice: wish and reality]. | 2001 Dec |
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Acetyl-coa: alcohol acetyltransferase activity and aroma formation in ripening melon fruits. | 2001 Feb |
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Teratogen update: reproductive risks of leflunomide (Arava); a pyrimidine synthesis inhibitor: counseling women taking leflunomide before or during pregnancy and men taking leflunomide who are contemplating fathering a child. | 2001 Feb |
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Combination of antilymphocyte globulin and leflunomide leads to superior grafts. | 2001 Feb-Mar |
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Flow cytometric quantitation of calcium-dependent and -independent mitogen-stimulation of T cell functions in whole blood: inhibition by immunosuppressive drugs in vitro. | 2001 Jul 1 |
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Beneficial effects of leflunomide in glucocorticoid- and methotrexate-resistant Takayasu's arteritis. | 2001 Jul-Aug |
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Treatment of immune-mediated skin diseases: future perspectives. | 2001 Jul-Aug |
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Treating early rheumatoid arthritis in the younger patient. | 2001 Jun |
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Conventional DMARD options for patients with a suboptimal response to methotrexate. | 2001 Jun |
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Novel therapies for anti-neutrophil cytoplasmic antibody-associated vasculitis. | 2001 Mar |
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Comorbidity in rheumatoid arthritis. | 2001 May |
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Leflunomide-associated weight loss in rheumatoid arthritis. | 2001 May |
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[Chronic polyarthritis]. | 2001 May 24 |
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[Leflunomide--a new disease modifying anti-rheumatic agent]. | 2001 Nov 10 |
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Severe liver damage with leflunomide. | 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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Is there a place for leflunomide in the treatment of rheumatoid arthritis? | 2001 Oct 13 |
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Etanercept therapy for immune-mediated cochleovestibular disorders: preliminary results in a pilot study. | 2001 Sep |
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Economic comparison of leflunomide and methotrexate in patients with rheumatoid arthritis: an evaluation based on a 1-year randomised controlled trial. | 2002 |
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Experiences with leflunomide in solid organ transplantation. | 2002 Feb 15 |
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Leflunomide induced fevers, thrombocytosis, and leukocytosis in a patient with relapsing polychondritis. | 2002 Jan |
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Design and synthesis of potent inhibitors of the malaria parasite dihydroorotate dehydrogenase. | 2007 Jan 25 |
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Hepatic cytochrome P450s attenuate the cytotoxicity induced by leflunomide and its active metabolite A77 1726 in primary cultured rat hepatocytes. | 2011 Aug |
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Systems pharmacological analysis of drugs inducing stevens-johnson syndrome and toxic epidermal necrolysis. | 2015 May 18 |
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
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on
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Record UNII |
1C058IKG3B
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Record Status |
Validated (UNII)
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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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TERIFLUNOMIDE
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Teriflunomide
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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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1310520
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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 |
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Related Record | Type | Details | ||
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PARENT -> IMPURITY |
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ACTIVE MOIETY |
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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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