- Molecular NameCyclosporine_A
- SynonymCiclosporin; Cyclosporin; cyclosporine
- Weight1202.64
- Drugbank_IDDB00091
- ACS_NO59865-13-3
- Show 2D model
- LogP (experiment)4.293
- 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
- StatusFDA approved
- 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. It has been studied in transplants of skin, heart, kidney, liver, lung, pancreas, bone marrow, and small intestine.
- Absorption_value33.0
- Absorption (description)The absorption of cyclosporine from the gastrointestinal tract is incomplete and variable. Compared to an intravenous infusion, the absolute bioavailability of the oral solution is approximately 30% based upon the results in 2 patients.
- Caco_2-6.05
- Bioavailability30.0
- Protein binding93.0
- Volume of distribution (VD)4.5 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmMetabolized by CYP3A to three major metabolites, which are subsequently biotransformed to numerous secondary and tertiary metabolites.
- Half life10.7 h
- Excretionbiliary
- Urinary Excretion<1
- Clerance5.7 ml/min/kg
- Toxicityhe principal adverse reactions of cyclosporine therapy are renal dysfunction, tremor, hirsutism, hypertension, and gum hyperplasia.
- LD50 (rat)N/A
- LD50 (mouse)N/A