• Molecular NameAcitretin
  • SynonymNA
  • Weight326.436
  • Drugbank_IDDB00459
  • ACS_NO55079-83-9
  • Show 2D model
  • LogP (experiment)6.4
  • LogP (predicted, AB/LogP v2.0)5.38
  • pka3.7
  • LogD (pH=7, predicted)2.79
  • Solubility (experiment)0.0000729 mg/ml
  • LogS (predicted, ACD/Labs)(ph=7)-2.22
  • LogSw (predicted, AB/LogsW2.0)0.0
  • Sw (mg/ml) (predicted, ACD/Labs)0.02
  • No.of HBond Donors1
  • No.of HBond Acceptors3
  • No.of Rotatable Bonds6
  • TPSA46.53
  • StatusFDA approved
  • AdministrationN/A
  • PharmacologyA second generation retinoid. It is taken orally, and is typically used for psoriasis.
  • Absorption_value72.0
  • Absorption (description)Oral absorption of acitretin is optimal when given with food, and is linear and proportional with increasing doses from 25 to 100 mg. Approximately 72% (range 47% to 109%) of the administered dose was absorbed after a single 50 mg dose of acitretin was given to 12 healthy subjects.
  • Caco_2N/A
  • Bioavailability59.0
  • Protein binding99.0
  • Volume of distribution (VD)2.3 to 4.5 L/kg; mean, 3.47 L/kg
  • Blood/Plasma Partitioning ratio (D_blood)N/A
  • MetabollsmIt undergoes extensive metabolism and interconversion by simple isomerisation to 13-cis-acitretin. Both acitretin and 13-cis-acitretin may be conjugated. An additional three metabolites have been identified. Etretinate has been detected following administration of acitretin; this may be a route of metabolism if there is concomitant alcohol consumption.
  • Half life50 h (acitretin); 63 h (13-cis-acitretin)
  • ExcretionIt is excreted in urine and bile.
  • Urinary ExcretionN/A
  • ClerancePlasma, 175.9 ± 81.4 mL/kg/h
  • ToxicityAcitretin is teratogenic. Although acitretin has a relatively short half-life, etretinate has also been detected in the plasma of some patients taking acitretin and since etretinate is also teratogenic and has a much longer half-life than acitretin, pregnancy must be avoided for at least 3 years after stopping acitretin therapy. Plasma concentrations may be a poor guide to presence of etretinate in the body since etretinate concentrates in fatty tissues. The minimum plasma concentrations associated with teratogenicity are unknown. Oral, rat: LD50 = >4000 mg/kg. Symptoms of overdose include headache and vertigo.
  • LD50 (rat)N/A
  • LD50 (mouse)N/A