• Molecular NameCiclosporin
  • SynonymCiclosporin; Cyclosporin A; cyclosporine
  • Weight1202.64
  • Drugbank_IDN/A
  • ACS_NO59865-13-3
  • Show 2D model
  • LogP (experiment)-3.3
  • LogP (predicted, AB/LogP v2.0)N/A
  • pkaN/A
  • LogD (pH=7, predicted)N/A
  • Solubility (experiment)N/A
  • LogS (predicted, ACD/Labs)(ph=7)N/A
  • LogSw (predicted, AB/LogsW2.0)N/A
  • Sw (mg/ml) (predicted, ACD/Labs)N/A
  • No.of HBond DonorsN/A
  • No.of HBond AcceptorsN/A
  • No.of Rotatable BondsN/A
  • TPSAN/A
  • StatusN/A
  • Administrationoral, IV, ophthalmic
  • PharmacologyAn immunosuppressant drug widely used in post-allogeneic organ transplant to reduce the activity of the patient's immune system and, so, the risk of organ rejection.
  • Absorption_valueN/A
  • Absorption (description)After oral administration of conventional formulations absorption is very variable; absolute bioavailability can vary from less than 10% in liver transplant patients to up to 89% in some renal transplant patients.
  • Caco_2N/A
  • Bioavailability30.0
  • Protein binding98.6
  • Volume of distribution (VD)N/A
  • Blood/Plasma Partitioning ratio (D_blood)his is concentration and temperature dependent. Approx. 40% is taken up in erythrocytes and the remainder extensively binds plasma proteins. At high concentrations the binding to blood cells becomes saturated.
  • MetabollsmIt is extensively metabolised by CYP4503A mainly in the liver (some also in the gastro-intestinal tract and kidney)
  • Half life24 h
  • ExcretionExcreted primarily in faeces via the bile; only about 6% is excreted in the urine. The low oral bioavailability of ciclosporin is due to first-pass metabolism in the gastro-intestinal wall rather than the liver. It crosses the placenta and is distributed into breast milk. Dialysis does not affect clearance significantly.
  • Urinary ExcretionN/A
  • CleranceBlood clearance, 0.71 L/h/kg (paediatrics); 0.34 L/h/kg (adults).
  • ToxicityNephrotoxicity is the major toxic effect; doses must be adjusted individually and kidney function must be monitored during therapy.
  • LD50 (rat)N/A
  • LD50 (mouse)LD50=107