- Molecular NameLeflunomide
- Synonymleflunomide; Leflunomidum [INN-Latin]; Lefunomide [INN-Spanish]
- Weight270.21
- Drugbank_IDDB01097
- ACS_NO75706-12-6
- Show 2D model
- LogP (experiment)2.659
- LogP (predicted, AB/LogP v2.0)2.81
- pka10.8
- LogD (pH=7, predicted)2.81
- Solubility (experiment)0.021 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-3.6
- LogSw (predicted, AB/LogsW2.0)0.29
- Sw (mg/ml) (predicted, ACD/Labs)0.07
- No.of HBond Donors1
- No.of HBond Acceptors4
- No.of Rotatable Bonds3
- TPSA55.13
- StatusFDA approved
- AdministrationN/A
- PharmacologyA medication of the DMARD type, used in active moderate to severe rheumatoid arthritis and psoriatic arthritis. It is a pyrimidine synthesis inhibitor.
- Absorption_valueN/A
- Absorption (description)N/A
- Caco_2N/A
- Bioavailability80.0
- Protein binding99.4
- Volume of distribution (VD)0.18 L/kg (active metabolite)
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmLeflunomide is a prodrug that is converted almost completely (95%) to an active metabolite A77-1726 (2-cyano-3-hydroxy-N-(4-trifluoromethylphenyl)-crotonamide). All pharmacokinetic data reported are for the active metabolite.
- Half life377 h
- ExcretionElimination of the metabolite is very slow (6 to 40 days) and approx. 90% of the dose is recovered in faeces and urine. In faeces, leflunomide is primarily excreted as the metabolite, and in urine as leflunomide glucuronides and the oxanilic acid derivative of the metabolite. Small amounts are distributed into breast milk. Steady state concentrations are reached after approx. 20 weeks of leflunomide dosing.
- Urinary ExcretionNegligible
- Clerance0.0012 ml/min/kg (metabolite)
- ToxicityLD50=100-250 mg/kg
- LD50 (rat)N/A
- LD50 (mouse)N/A