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Substance Name: Leflunomide [USAN:USP:INN:BAN]
RN: 75706-12-6
UNII: G162GK9U4W
InChIKey: VHOGYURTWQBHIL-UHFFFAOYSA-N

Note

  • Inhibits dihydroorotate dehydrogenase, the fourth enzyme in the pyrimidine biosynthetic pathway; antagonizes growth-factor mediated smooth muscle cell proliferation in vitro.

Molecular Formula

  • C12-H9-F3-N2-O2

Molecular Weight

  • 270.2091
 

Classification Codes

  • Antineoplastic (Blocks PDGF Receptor Function, Inhibiting the Growth and Survival of Human Tumor Cells When Administered Intravenously)
  • Antirheumatic Agents
  • Drug / Therapeutic Agent
  • Enzyme Inhibitors
  • Immunologic Factors
  • Immunosuppressive Agents
  • Used in the Treatment of Rheumatoid Arthritis When Administered Orally

Names and Synonyms

Name of Substance

  • Leflunomide
  • Leflunomide [USAN:USP:INN:BAN]

Synonyms

  • 4-Isoxazolecarboxamide, 5-methyl-N-(4-(trifluoromethyl)phenyl)-
  • 5-Methyl-N-(4-(trifluoromethyl)phenyl)-4-isoxazolecarboxamide
  • 5-Methylisoxazole-4-carboxylic acid (4-trifluoromethyl)anilide
  • Arava
  • HSDB 7289
  • HWA 486
  • HWA-486
  • Leflunomida
  • Leflunomida [INN-Spanish]
  • Leflunomide
  • Leflunomidum
  • Leflunomidum [INN-Latin]
  • N-(4'-Trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide
  • SU 101 (pharmaceutical)
  • SU101
  • UNII-G162GK9U4W

Systematic Names

  • 4-Isoxazolecarboxamide, 5-methyl-N-(4-(trifluoromethyl)phenyl)-
  • alpha,alpha,alpha-Trifluoro-5-methyl-4-isoxazolecarboxy-p-toluidide

Registry Numbers

CAS Registry Number

  • 75706-12-6

FDA UNII

  • G162GK9U4W

Other Registry Number

  • 210165-51-8

System Generated Number

  • 0075706126

Structure Descriptors

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

Smiles

Cc1c(cno1)C(=O)Nc2ccc(cc2)C(F)(F)F

Toxicity

Organism Test Type Route Reported Dose (Normalized Dose) Effect Source
mouse LD50 intraperitoneal 185mg/kg (185mg/kg)   United States Patent Document. Vol. #5494911,
mouse LD50 oral 445mg/kg (445mg/kg)   United States Patent Document. Vol. #5494911,
rat LD50 intraperitoneal 170mg/kg (170mg/kg)   United States Patent Document. Vol. #5494911,
rat LD50 oral 235mg/kg (235mg/kg)   United States Patent Document. Vol. #5494911,