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Intermediates&Fine Chemicals

Leflunomide

Category:

Intermediates&Fine Chemicals

CAS NO:

75706-12-6

Standard:

In-house Standards,

Price Range:

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Main Sales Markets:

North America,Central/South America,Western Europe,Eastern Europe,Australasia,Asia,Middle East,Africa

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INNER MONGOLIA YUANHONG FINE CHEMICAL CO., LTD.

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Basic Info

CAS Number

75706-12-6

Pharmacopoeia

In-house Standards

Grade

Pharmaceutical Grade

Is Manufacturer

Samples Provided

Product Description

Leflunomide 75706-12-6

AI Product Description

*The following content is generated by AI and is for reference only.

Leflunomide is a potent immunosuppressive and anti-inflammatory agent primarily utilized in the management of rheumatoid arthritis (RA). Chemically, it belongs to the class of isoxazole derivatives. Its molecular formula is C12H9F3N2O2, reflecting its complex structure which includes a trifluoromethyl group essential for its biological activity. The compound is uniquely identified by the CAS number 75706-49-3. Upon oral administration, leflunomide undergoes rapid absorption and extensive first-pass metabolism in the liver to form its active metabolite, A77 1726. This active metabolite acts as a reversible inhibitor of dihydroorotate dehydrogenase (DHODH), a key mitochondrial enzyme involved in pyrimidine synthesis. By blocking this pathway, the drug effectively halts the proliferation of activated T-lymphocytes and other immune cells that drive the inflammatory processes characteristic of autoimmune diseases. Beyond rheumatoid arthritis, leflunomide has demonstrated efficacy in treating psoriatic arthritis and has been investigated for use in systemic lupus erythematosus and certain vasculitides. It is often prescribed when patients fail to respond adequately to methotrexate or other conventional disease-modifying antirheumatic drugs (DMARDs). The medication is available in tablet formulations, typically dosed with an initial loading phase followed by a lower maintenance dose to achieve therapeutic blood levels while minimizing toxicity. Due to its long half-life, which can extend up to two weeks, plasma concentrations remain stable even after discontinuation, necessitating a specific elimination procedure using cholestyramine if severe adverse reactions occur. Common side effects include diarrhea, nausea, elevated liver enzymes, hypertension, and hair thinning. Regular monitoring of liver function tests and complete blood counts is mandatory during therapy. Furthermore, leflunomide is strictly contraindicated in pregnancy due to its teratogenic potential, requiring rigorous contraception measures for both male and female patients before, during, and after treatment cessation. Overall, leflunomide represents a critical therapeutic option for controlling chronic autoimmune inflammation and preserving joint function.