DGIdb - LEFLUNOMIDE Drug Record

LEFLUNOMIDE chembl:CHEMBL960 ApprovedAntineoplasticImmunotherapy

Alternate Names:

SULOL
LEFLUNOMIDE
SU-101
ARAVA
HWA-486
L04AA13
SU101
5-METHYL-N-(4-(TRIFLUOROMETHYL)PHENYL)-4-ISOXAZOLECARBOXAMIDE
HWA 486
LEFUNOMIDE
ARAVA®
LEFLUNOMIDA
ALPHA,ALPHA,ALPHA-TRIFLUORO-5-METHYL-4-ISOXAZOLECARBOXY-P-TOLUIDIDE
5-METHYLISOXAZOLE-4-CARBOXYLIC ACID (4-TRIFLUOROMETHYL)ANILIDE
LEFUNAMIDE
LEFLUNOMIDUM
ARABLOC®
chembl:CHEMBL960
drugbank:01097
chemidplus:75706-12-6
rxcui:27169
pubchem.compound:3899

Drug Info:

Year of Approval	1998
Drug Class	antirheumatic agents
FDA Approval	1998
Drug Class	small molecule
Drug Indications	Antirheumatic Agents
Drug Categories	agents causing muscle toxicity
Drug Categories	cytochrome p-450 cyp2c9 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	disease-modifying antirheumatic agents
Drug Categories	isoxazoles

(6 More Sources)

Publications:

Schattenkirchner, 2000, The use of leflunomide in the treatment of rheumatoid arthritis: an experimental and clinical review., Immunopharmacology
Herrmann et al., 2000, Leflunomide: an immunomodulatory drug for the treatment of rheumatoid arthritis and other autoimmune diseases., Immunopharmacology
Wozel et al., 2002, [Leflunomide--a new drug for pharmacological immunomodulation]., Hautarzt
Reitzik et al., 1975, Familial polyostotic fibrous dysplasia., Oral Surg. Oral Med. Oral Pathol.
Li et al., 2004, Leflunomide in the treatment of rheumatoid arthritis., Clin Ther
Fukushima et al., Teratogenicity study of the dihydroorotate-dehydrogenase inhibitor and protein tyrosine kinase inhibitor Leflunomide in mice., Reprod. Toxicol.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Goldenberg, 1999, Leflunomide, a novel immunomodulator for the treatment of active rheumatoid arthritis., Clin Ther
Prakash et al., 1999, Leflunomide: a review of its use in active rheumatoid arthritis., Drugs
Fox, 1998, Mechanism of action of leflunomide in rheumatoid arthritis., J Rheumatol Suppl
Sanders et al., 2002, Leflunomide for the treatment of rheumatoid arthritis and autoimmunity., Am. J. Med. Sci.
Breedveld et al., 2000, Leflunomide: mode of action in the treatment of rheumatoid arthritis., Ann. Rheum. Dis.
Pawlik A et al., 2009, The effect of exon (19C>A) dihydroorotate dehydrogenase gene polymorphism on rheumatoid arthritis treatment with leflunomide., Pharmacogenomics
Bohanec Grabar P et al., 2009, Investigation of the influence of CYP1A2 and CYP2C19 genetic polymorphism on 2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide (A77 1726) pharmacokinetics in leflunomide-treated patients with rheumatoid arthritis., Drug Metab Dispos
Bohanec Grabar P et al., 2008, Genetic polymorphism of CYP1A2 and the toxicity of leflunomide treatment in rheumatoid arthritis patients., Eur J Clin Pharmacol
Hu et al., 2007, Induction of cyp1a1 is a nonspecific biomarker of aryl hydrocarbon receptor activation: results of large scale screening of pharmaceuticals and toxicants in vivo and in vitro., Mol. Pharmacol.
O'Donnell et al., 2010, The anti-inflammatory drug leflunomide is an agonist of the aryl hydrocarbon receptor., PLoS ONE
Kullich et al., Inhibitory effects of leflunomide therapy on the activity of matrixmetalloproteinase-9 and the release of cartilage oligomeric matrix protein in patients with rheumatoid arthritis., Clin. Exp. Rheumatol.
Steeghs et al., 2007, Small molecule tyrosine kinase inhibitors in the treatment of solid tumors: an update of recent developments., Ann. Surg. Oncol.
Pytel et al., 2009, Tyrosine kinase blockers: new hope for successful cancer therapy., Anticancer Agents Med Chem
Kraan et al., 2000, Inhibition of neutrophil migration soon after initiation of treatment with leflunomide or methotrexate in patients with rheumatoid arthritis: findings in a prospective, randomized, double-blind clinical trial in fifteen patients., Arthritis Rheum.
Dziedziejko V et al., 2011, The effect of ESR1 and ESR2 gene polymorphisms on the outcome of rheumatoid arthritis treatment with leflunomide., Pharmacogenomics

LEFLUNOMIDE DHODH

Interaction Score: 3.69

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Dihydroorotate dehydrogenase inhibitor

Trial Name -

PMIDs:
10878295 10878294 12063741 1060033 15189743 17604599 11752352 10890256 10651393 9666414 12003373 11053058 19207032

Sources:
DTC DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB
LEFLUNOMIDE PTK2B

Interaction Score: 0.71

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
17604599 17103252 19149483

Sources:
DrugBank
LEFLUNOMIDE MMP1

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16762150

Sources:
NCI
LEFLUNOMIDE AHR

Interaction Score: 0.16

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
17327465 20957046

Sources:
DrugBank
LEFLUNOMIDE CXCL8

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10902750

Sources:
NCI
LEFLUNOMIDE ESR1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21174621

Sources:
PharmGKB
LEFLUNOMIDE SMN2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
LEFLUNOMIDE SMN1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
LEFLUNOMIDE RAB9A

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
LEFLUNOMIDE CYP1A2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
19581389 18496682

Sources:
DTC PharmGKB
LEFLUNOMIDE HTT

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
LEFLUNOMIDE ATAD5

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
LEFLUNOMIDE NFE2L2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
LEFLUNOMIDE CYP3A4

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

DrugBank: DB01097

Version: 5.1.7

Alternate Names:

Accel-leflunomide Drug Brand

Apo-leflunomide Drug Brand

LEFLUNOMIDE DrugBank Drug Name

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Steeghs et al., 2007, Small molecule tyrosine kinase inhibitors in the treatment of solid tumors: an update of recent developments., Ann. Surg. Oncol.

Pytel et al., 2009, Tyrosine kinase blockers: new hope for successful cancer therapy., Anticancer Agents Med Chem

Fukushima et al., Teratogenicity study of the dihydroorotate-dehydrogenase inhibitor and protein tyrosine kinase inhibitor Leflunomide in mice., Reprod. Toxicol.

TEND: LEFLUNOMIDE
- Version: 01-August-2011
Alternate Names:

LEFLUNOMIDE Primary Drug Name

Drug Info:

Drug Class antirheumatic agents

Year of Approval 1998

Publications:
TdgClinicalTrial: LEFLUNOMIDE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications Antirheumatic Agents

Drug Class small molecule

FDA Approval 1998

Publications:

NCI: LEFLUNOMIDE

Version: 14-September-2017

Alternate Names:

C1128 NCI drug code

Drug Info:

Publications:

Kraan et al., 2000, Inhibition of neutrophil migration soon after initiation of treatment with leflunomide or methotrexate in patients with rheumatoid arthritis: findings in a prospective, randomized, double-blind clinical trial in fifteen patients., Arthritis Rheum.

Kullich et al., Inhibitory effects of leflunomide therapy on the activity of matrixmetalloproteinase-9 and the release of cartilage oligomeric matrix protein in patients with rheumatoid arthritis., Clin. Exp. Rheumatol.

PharmGKB: leflunomide

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Bohanec Grabar P et al., 2008, Genetic polymorphism of CYP1A2 and the toxicity of leflunomide treatment in rheumatoid arthritis patients., Eur J Clin Pharmacol

Bohanec Grabar P et al., 2009, Investigation of the influence of CYP1A2 and CYP2C19 genetic polymorphism on 2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide (A77 1726) pharmacokinetics in leflunomide-treated patients with rheumatoid arthritis., Drug Metab Dispos

Pawlik A et al., 2009, The effect of exon (19C>A) dihydroorotate dehydrogenase gene polymorphism on rheumatoid arthritis treatment with leflunomide., Pharmacogenomics

DTC: LEFLUNOMIDE
- Version: 02-September-2020
Alternate Names:

CHEMBL960 ChEMBL Drug ID

Drug Info:

Publications:
GuideToPharmacology: 178103431
- Version: 29-September-2020
Alternate Names:

LEFLUNOMIDE GuideToPharmacology Ligand Name

Drug Info:

Publications:
TTD: Leflunomide
- Version: 2020.06.01
Alternate Names:

D08ROP TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL960
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL960
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Direct Interaction	yes
Mechanism of Interaction	Dihydroorotate dehydrogenase inhibitor
Trial Name	-

Accel-leflunomide	Drug Brand
Apo-leflunomide	Drug Brand
LEFLUNOMIDE	DrugBank Drug Name

Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational

LEFLUNOMIDE Drug Record

LEFLUNOMIDE chembl:CHEMBL960 ApprovedAntineoplasticImmunotherapy

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Dihydroorotate dehydrogenase inhibitor Trial Name -

PMIDs: 10878295 10878294 12063741 1060033 15189743 17604599 11752352 10890256 10651393 9666414 12003373 11053058 19207032

Sources: DTC DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 17604599 17103252 19149483

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16762150

Sources: NCI

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 17327465 20957046

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10902750

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21174621

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 19581389 18496682

Sources: DTC PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

DrugBank: DB01097

Alternate Names: Accel-leflunomide Drug Brand Apo-leflunomide Drug Brand LEFLUNOMIDE DrugBank Drug Name

Drug Info: Drug Type small molecule Drug Groups approved Drug Groups investigational

TEND: LEFLUNOMIDE

Alternate Names: LEFLUNOMIDE Primary Drug Name

Drug Info: Drug Class antirheumatic agents Year of Approval 1998

Publications:

TdgClinicalTrial: LEFLUNOMIDE

Alternate Names:

Drug Info: Drug Indications Antirheumatic Agents Drug Class small molecule FDA Approval 1998

Publications:

NCI: LEFLUNOMIDE

Alternate Names: C1128 NCI drug code

Drug Info:

PharmGKB: leflunomide

Alternate Names:

Drug Info:

DTC: LEFLUNOMIDE

Alternate Names: CHEMBL960 ChEMBL Drug ID

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Dihydroorotate dehydrogenase inhibitor

Trial Name -

PMIDs:
10878295 10878294 12063741 1060033 15189743 17604599 11752352 10890256 10651393 9666414 12003373 11053058 19207032

Sources:
DTC DrugBank TdgClinicalTrial ChemblInteractions TEND GuideToPharmacology PharmGKB

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
17604599 17103252 19149483

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
16762150

Sources:
NCI

Interaction Types & Directionality:

agonist (activating)

PMIDs:
17327465 20957046

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
10902750

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
21174621

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
19581389 18496682

Sources:
DTC PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Alternate Names:

Accel-leflunomide Drug Brand

Apo-leflunomide Drug Brand

LEFLUNOMIDE DrugBank Drug Name

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Alternate Names:

LEFLUNOMIDE Primary Drug Name

Drug Info:

Drug Class antirheumatic agents

Year of Approval 1998

Drug Info:

Drug Indications Antirheumatic Agents

Drug Class small molecule

FDA Approval 1998

Alternate Names:

C1128 NCI drug code

Alternate Names:

CHEMBL960 ChEMBL Drug ID

Alternate Names:

LEFLUNOMIDE GuideToPharmacology Ligand Name

Alternate Names:

D08ROP TTD Drug ID