Drug General Information
Drug ID
D08ROP
Former ID
DAP000636
Drug Name
Leflunomide
Synonyms
Arava; Leflunomid; Leflunomida; Leflunomidum; Lefunamide; Aventis Behring Brand of Leflunomide; Aventis Brand of Leflunomide; Aventis Pharma Brand of Leflunomide; Hoechst Brand of Leflunomide; HWA 486; L 5025; SU 101; SU101; Arava (TN); Arava, Leflunomide; HWA-486; Leflunomida [INN-Spanish]; Leflunomide [USAN:INN]; Leflunomidum [INN-Latin]; Lefunomide [Inn-Spanish]; RS-34821; SU 101 (pharmaceutical); SU-101; AP-501/42475599; Leflunomide (JAN/USAN/INN); N-(4-trifluoromethyphenyl)-5-methylisoxazole-4-carboxamide; N-(4'-Trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide; Alpha,alpha,alpha-Trifluoro-5-methyl-4-isoxazolecarboxy-p-toluidide; 4-Isoxazolecarboxamide, 5-methyl-N-(4-(trifluoromethyl)phenyl; 4-isoxazolecarboxamide,5-methyl-N-(4-(trifluoromethyl)phenyl); 5-Methyl-N-(4-(trifluoromethyl)phenyl)-4-isoxazolecarboxamide; 5-Methylisoxazole-4-(4-trifluoromethyl)carboxanilide; 5-Methylisoxazole-4-(4-trifluoromethylcarboxanilide); 5-Methylisoxazole-4-carboxylic acid (4-trifluoromethyl)anilide; 5-methyl-N-[4-(trifluoromethyl)phenyl]-1,2-oxazole-4-carboxamide; 5-methyl-N-[4-(trifluoromethyl)phenyl]-4-isoxazolecarboxamide; 5-methyl-N-[4-(trifluoromethyl)phenyl]isoxazole-4-carboxamide
Drug Type
Small molecular drug
Indication Multiple scierosis; Active rheumatoid arthritis [ICD9: 340, 714; ICD10:G35, M05, M06] Approved [532210], [536772], [541907]
Therapeutic Class
Antiinflammatory Agents
Company
Sanofi-Aventis
Structure
Download
2D MOL

3D MOL

Formula
C12H9F3N2O2
InChI
InChI=1S/C12H9F3N2O2/c1-7-10(6-16-19-7)11(18)17-9-4-2-8(3-5-9)12(13,14)15/h2-6H,1H3,(H,17,18)
InChIKey
VHOGYURTWQBHIL-UHFFFAOYSA-N
CAS Number
CAS 75706-12-6
PubChem Compound ID
PubChem Substance ID
ChEBI ID
ChEBI:6402
SuperDrug ATC ID
L04AA13
SuperDrug CAS ID
cas=075706126
Target and Pathway
Target(s) Dihydroorotate dehydrogenase, mitochondrial Target Info Inhibitor [534936], [537837], [538007], [538113]
KEGG Pathway Pyrimidine metabolism
Metabolic pathways
PathWhiz Pathway Pyrimidine Metabolism
Reactome Pyrimidine biosynthesis
WikiPathways Metabolism of nucleotides
References
Ref 532210Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
Ref 536772New drugs in development for the treatment of endometriosis. Expert Opin Investig Drugs. 2008 Aug;17(8):1187-202.
Ref 541907(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6825).
Ref 534936Identification and characterization of potential new therapeutic targets in inflammatory and autoimmune diseases. Eur J Biochem. 1999 Dec;266(3):1184-91.
Ref 537837Inhibition of dihydroorotate dehydrogenase by the immunosuppressive agent leflunomide. Biochem Pharmacol. 1995 Sep 7;50(6):861-7.
Ref 538007Dihydroorotate dehydrogenase is a target for the biological effects of leflunomide. Transplant Proc. 1996 Dec;28(6):3088-91.
Ref 538113Expression, purification, and characterization of histidine-tagged rat and human flavoenzyme dihydroorotate dehydrogenase. Protein Expr Purif. 1998 Aug;13(3):414-22.

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