• Molecular NameTacrolimus
  • SynonymFK-506; FK5; K506; Tacarolimus; tacrolimus; tacrolimus hydrate
  • Weight804.031
  • Drugbank_IDDB00864
  • ACS_NO104987-11-3
  • Show 3D model
  • LogP (experiment)N/A
  • LogP (predicted, AB/LogP v2.0)6.52
  • pkaN/A
  • LogD (pH=7, predicted)6.52
  • Solubility (experiment)Insoluble
  • LogS (predicted, ACD/Labs)(ph=7)-4.16
  • LogSw (predicted, AB/LogsW2.0)0.01
  • Sw (mg/ml) (predicted, ACD/Labs)0.06
  • No.of HBond Donors3
  • No.of HBond Acceptors13
  • No.of Rotatable Bonds7
  • TPSA178.36
  • StatusFDA approved
  • AdministrationN/A
  • PharmacologyAn immunosuppressive drug whose main use is after allogeneic organ transplant to reduce the activity of the patient's immune system and so lower the risk of organ rejection.
  • Absorption_valueN/A
  • Absorption (description)20% bioavailability; less after eating food rich in fat
  • Caco_2N/A
  • Bioavailability25.0
  • Protein binding98.5
  • Volume of distribution (VD)0.91 L/kg
  • Blood/Plasma Partitioning ratio (D_blood)N/A
  • MetabollsmMetabolized by CYP3A; also a substrate for P-glycoprotein
  • Half life43 h in healthy volunteers and 12 to 16 h in transplant patients.
  • ExcretionMostly faecal
  • Urinary Excretion<1
  • Clerance0.90 ml/min/kg
  • ToxicitySide effects can be severe and include blurred vision, liver and kidney problems (it is nephrotoxic), seizures, tremors, hypertension, hypomagnesemia, diabetes mellitus, hyperkalemia, itching, insomnia, confusion. LD50=134-194 mg/kg (rat).
  • LD50 (rat)N/A
  • LD50 (mouse)LD50=25 (intravenous)