LEFLUNOMIDE

PRODUCT IDENTIFICATION
CAS NO. 75706-12-6

LEFLUNOMIDE

EINECS NO.  
FORMULA C12H9F3N2O2
MOL WT. 270.21

H.S. CODE

  

TOXICITY

  
SYNONYMS ARAVA;
N-(4´-Trifluoromethylphenyl)-5-methylisoxazole-4-carboxamide;  5-Methylisoxazole-4-( 4-trifluoromethyl)carboxanilide; alpha,alpha,alpha-Trifluoro-5-methyl-4- isoxazolecarboxy-p -toluidide;
SMILES

 

CLASSIFICATION

  

PHYSICAL AND CHEMICAL PROPERTIES
PHYSICAL STATE White crystalline powder
MELTING POINT 165 - 166 C
BOILING POINT  
SPECIFIC GRAVITY  
SOLUBILITY IN WATER  
pH  
VAPOR DENSITY

 

AUTOIGNITION

 

NFPA RATINGS

  

REFRACTIVE INDEX

  
FLASH POINT

 

STABILITY Stable under ordinary conditions.

APPLICATIONS

Leflunomide derived from isoxazole is a pyrimidine synthesis inhibitor by interfering with the synthesis of dihydroorotate dehydrogenase(DHODH), resulting in inhibiting T and B cell proliferation or growth. It is used in the treatment of rheumatoid arthritis. It reduces the symptoms of rheumatoid arthritis and slows progressive deformities of the joints. The chemical designation is N-(4´-trifluoromethylphenyl)-5- methylisoxazole-4- carboxamide. It is a white crystals powder; melting point 165 - 166 C; administered orally.
SALES SPECIFICATION

APPEARANCE

 White crystalline powder

IDENTIFICATION

Complies

ASSAY (HPLC)

 99.0% min
MELTING POINT 165 - 166 C

LOSS ON DRYING

1.0% max
HEAVY METALS

10ppm max
SULFATED ASH 0.1% max
TRANSPORTATION
PACKING

 

HAZARD CLASS  
UN NO.  
GENERAL DESCRIPTION OF RHEUMATOID ARTHRITIS
Rheumatoid arthritis is a chronic arthritis in which joints or synovial linings are inflamed, resulting in swelling, pain, and often the disability of function. The exact cause is not known but It is considered an autoimmune diseases characterized by an overactive immune response, whereby the body own immune defense mechanisms are inappropriately directed against the normal tissue that lines the joints and connective tissue in many other parts of the body, such as the blood vessels and lungs, resulting in organ damage or activation of a systemic immune response.

The main categories of drugs to treat or slow down rheumatoid arthritis are nonsteroidal anti-inflammatory drugs (NSAIDs), gold compounds (sodium aurothiomalate, auranofin), analgesics, corticosteroids, immunosuppressive drugs which are originally used to prevent the rejection of transplanted organs and tissues. Immunosuppressive drugs are also used to treat myasthenia gravis, systemic lupus erythematosus, ulcerative colitis. Most of immunosuppressive drugs have their own potentially serious side effects. They should be used in small doses.  They acts by suppressing cell growth or multiplication of both T cells and B cells and interfering with the synthesis of nucleic acids. There are newer biologic therapies such as tumor necrosis factor (TNF) inhibitors and interleukin-1 receptor antagonists.

Some examples of immunosuppressive drugs to slow down rheumatoid arthritis include:

  • Azathioprine
  • Cyclophosphamide
  • Cyclosporine
  • Hydroxychloroquine
  • Leflunomide
  • Methotrexate
  • Penicillamine