Lefunomide

Lefunomide Brand names, Lefunomide Analogs

Lefunomide Brand Names Mixture

No information avaliable

Lefunomide Chemical_Formula

C₁₂H₉F₃N₂O₂

Lefunomide RX_link

http://www.rxlist.com/cgi/generic3/leflunomide.htm

Lefunomide fda sheet

Lefunomide FDA

Lefunomide msds (material safety sheet)

Lefunomide MSDS

Lefunomide Synthesis Reference

No information avaliable

Lefunomide Molecular Weight

270.207 g/mol

Lefunomide Melting Point

165-166 ^oC

Lefunomide H₂O Solubility

21 mg/L (poorly soluble)

Lefunomide State

Solid

Lefunomide LogP

2.659

Lefunomide Dosage Forms

Tablet

Lefunomide Indication

For the treatment of active rheumatoid arthritis (RA).

Lefunomide Pharmacology

Leflunomide is a pyrimidine synthesis inhibitor indicated in adults for the treatment of active rheumatoid arthritis (RA). RA is an auto-immune disease characterized by high T-cell activity. T cells have two pathways to synthesize pyrimidines: the salvage pathways and the de novo synthesis. At rest, T lymphocytes meet their metabolic requirements by the salvage pathway. Activated lymphocytes need to expand their pyrimidine pool 7- to 8-fold, while the purine pool is expanded only 2- to 3-fold. To meet the need for more pyrimidines, activated T cells use the de novo pathway for pyrimidine synthesis. Therefore, activated T cells, which are dependent on de novo pyrimidine synthesis, will be more affected by leflunomide's inhibition of dihydroorotate dehydrogenase than other cell types that use the salvage pathway of pyrimidine synthesis.

Lefunomide Absorption

Well absorbed, peak plasma concentrations appear 6-12 hours after dosing

Lefunomide side effects and Toxicity

LD₅₀=100-250 mg/kg (acute oral toxicity)

Lefunomide Patient Information