• Molecular NameLevocabastine
  • SynonymLevocabastin; Levocabastina [Spanish]; Levocabastinum [Latin]
  • Weight420.528
  • Drugbank_IDDB01106
  • ACS_NO79516-68-0
  • Show 3D model
  • LogP (experiment)N/A
  • LogP (predicted, AB/LogP v2.0)5.27
  • pkaN/A
  • LogD (pH=7, predicted)2.77
  • Solubility (experiment)N/A
  • LogS (predicted, ACD/Labs)(ph=7)-3.82
  • LogSw (predicted, AB/LogsW2.0)0.01
  • Sw (mg/ml) (predicted, ACD/Labs)0.06
  • No.of HBond Donors1
  • No.of HBond Acceptors4
  • No.of Rotatable Bonds5
  • TPSA64.33
  • StatusFDA approved; US withdrawn
  • Administrationophthalmic
  • PharmacologyA selective second-generation H1-receptor antagonist which was discovered at Janssen Pharmaceutica in 1979. It is used for allergic conjunctivitis.
  • Absorption_valueN/A
  • Absorption (description)Levocabastine is rapidly and completely absorbed after intranasal, ocular and oral administration, but peak plasma concentrations are low.
  • Caco_2N/A
  • BioavailabilityN/A
  • Protein binding55.0
  • Volume of distribution (VD)1.14 L/kg
  • Blood/Plasma Partitioning ratio (D_blood)N/A
  • MetabollsmFirst-pass metabolism is negligible and it is excreted in urine as the unchanged drug (70%) and as an acetylglucuronide metabolite which is biologically inactive (10%).
  • Half life33~40 h
  • ExcretionThe remaining proportion of the unchanged drug is excreted in faeces (20%). Trace amounts of the drug are found in breast milk.
  • Urinary ExcretionN/A
  • Clerance1.8 L/h
  • ToxicityAdverse effects include visual disturbances, dry mouth, cough, nausea, eyelid edema and lacrimation.
  • LD50 (rat)N/A
  • LD50 (mouse)N/A