- Molecular NameRosiglitazone
- SynonymRosigliazone maleate; rosiglitazone; Rosiglitazone maleate
- Weight357.434
- Drugbank_IDDB00412
- ACS_NO122320-73-4
- Show 2D model
- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)2.68
- pkaN/A
- LogD (pH=7, predicted)1.52
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-3.4
- LogSw (predicted, AB/LogsW2.0)0.03
- Sw (mg/ml) (predicted, ACD/Labs)0.1
- No.of HBond Donors1
- No.of HBond Acceptors6
- No.of Rotatable Bonds7
- TPSA96.83
- StatusFDA approved
- AdministrationN/A
- PharmacologyAn anti-diabetic drug in the thiazolidinedione class of drugs.
- Absorption_value100.0
- Absorption (description)The absolute bioavailability of rosiglitazone is 99%. Peak plasma concentrations are observed about 1 hour after dosing. Administration of rosiglitazone with food resulted in no change in overall exposure (AUC), but there was an approximately 28% decrease in Cmax and a delay in Tmax (1.75 hours). These changes are not likely to be clinically significant; therefore, rosiglitazone may be administered with or without food.
- Caco_2N/A
- Bioavailability99.0
- Protein binding99.8
- Volume of distribution (VD)0.25 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmMetabolized primarily by CYP2C8.
- Half life3~4 h
- ExcretionRenal (64%) and fecal (23%)
- Urinary ExcretionNegligible
- Clerance0.68 ml/min/kg
- ToxicitySide effects include fluid retention, congestive heart failure (CHF), liver disease
- LD50 (rat)N/A
- LD50 (mouse)N/A