- Molecular NameSorafenib
- Synonymsorafenib; Sorafenib tosylate
- Weight464.831
- Drugbank_IDDB00398
- ACS_NO284461-73-0
- Show 3D model
- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)4.27
- pkaN/A
- LogD (pH=7, predicted)4.27
- Solubility (experiment)Insoluble
- LogS (predicted, ACD/Labs)(ph=7)-6.47
- LogSw (predicted, AB/LogsW2.0)0.0
- Sw (mg/ml) (predicted, ACD/Labs)0.0
- No.of HBond Donors3
- No.of HBond Acceptors7
- No.of Rotatable Bonds6
- TPSA92.35
- StatusFDA approved
- AdministrationN/A
- PharmacologyA drug approved for the treatment of primary kidney cancer (advanced renal cell carcinoma) and advanced primary liver cancer (hepatocellular carcinoma).
- Absorption_valueN/A
- Absorption (description)The mean relative bioavailability is 38-49% for the tablet form, when compared to an oral solution. With a high-fat meal, bioavailability is reduced by 29% compared to administration in the fasted state.
- Caco_2N/A
- Bioavailability39.0
- Protein binding99.5
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmSorafenib is metabolized primarily in the liver, undergoing oxidative metabolism, mediated by CYP3A4, as well as glucuronidation mediated by UGT1A9. Sorafenib accounts for approximately 70-85% of the circulating analytes in plasma at steady- state. Eight metabolites of sorafenib have been identified, of which five have been detected in plasma. The main circulating metabolite of sorafenib in plasma, the pyridine N-oxide, shows in vitro potency similar to that of sorafenib. This metabolite comprises approximately 9-16% of circulating analytes at steady-state.
- Half life25~48 h
- ExcretionFecal (77%) and renal (19%)
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityThe highest dose of sorafenib studied clinically is 800 mg twice daily. The adverse reactions observed at this dose were primarily diarrhea and dermatologic events. No information is available on symptoms of acute overdose in animals because of the saturation of absorption in oral acute toxicity studies conducted in animals.
- LD50 (rat)N/A
- LD50 (mouse)N/A