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163451-81-8
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Basic Info
CAS Number
163451-81-8
Pharmacopoeia
ChP
Grade
In-house Standards
Is Manufacturer
YES
Packaging & Delivery
Minimum Order Quantity
Any
Delivery Cycle
Negotiable
Product Description
Reference Standards &Impurity
AI Product Description
*The following content is generated by AI and is for reference only.
Leflunomide is a potent immunomodulatory and anti-inflammatory agent primarily utilized in the management of rheumatoid arthritis (RA). Chemically, it functions as an active prodrug that is rapidly converted into its pharmacologically active metabolite, teriflunomide, upon oral administration. The molecular formula of leflunomide is C12H4F3N3O, reflecting its complex structure containing fluorine atoms which contribute to its specific biological activity. Its unique chemical identity is cataloged under the CAS number 75706-98-4.
The primary mechanism of action involves the reversible inhibition of dihydroorotate dehydrogenase (DHODH), a key enzyme in the pyrimidine synthesis pathway. By blocking this enzyme, leflunomide effectively reduces the proliferation of activated T-lymphocytes, which are central drivers of autoimmune inflammation and joint destruction in RA patients. Unlike some other disease-modifying antirheumatic drugs (DMARDs) that broadly suppress the immune system, leflunomide offers a more targeted approach by interfering with nucleotide production specifically in rapidly dividing cells. This makes it highly effective for slowing disease progression and alleviating symptoms such as joint pain, swelling, and stiffness.
Clinically, leflunomide is indicated for adult patients with moderately to severely active rheumatoid arthritis, often used as monotherapy or in combination with methotrexate when monotherapy proves insufficient. It has also shown efficacy in managing psoriatic arthritis in certain cases. Due to its long half-life, particularly that of teriflunomide, therapeutic effects can persist for months after discontinuation, necessitating careful monitoring and potentially requiring an elimination procedure using cholestyramine if severe toxicity occurs. While generally well-tolerated, common side effects may include diarrhea, elevated liver enzymes, hypertension, and hair thinning. Patients must undergo regular blood tests to monitor hepatic function and blood counts. As a cornerstone therapy in modern rheumatology, leflunomide remains a critical option for improving quality of life and preserving joint integrity in chronic autoimmune conditions.
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