- Molecular NameGefitinib
- SynonymZD-1839; ZD1839
- Weight446.91
- Drugbank_IDDB00317
- ACS_NO184475-35-2
- Show 2D model
- LogP (experiment)3.46
- LogP (predicted, AB/LogP v2.0)3.95
- pka5.4, 7.2
- LogD (pH=7, predicted)3.64
- Solubility (experiment)Sparingly soluble
- LogS (predicted, ACD/Labs)(ph=7)-5.61
- LogSw (predicted, AB/LogsW2.0)0.0
- Sw (mg/ml) (predicted, ACD/Labs)0.0
- No.of HBond Donors1
- No.of HBond Acceptors7
- No.of Rotatable Bonds8
- TPSA68.74
- StatusFDA approved
- AdministrationN/A
- PharmacologyA drug used in the treatment of certain types of cancer. Gefitinib is an EGFR inhibitor, like erlotinib, selectively targeting proteins in malignant cells. It is marketed by AstraZeneca and Teva.
- Absorption_valueN/A
- Absorption (description)N/A
- Caco_2N/A
- Bioavailability60.0
- Protein binding90.0
- Volume of distribution (VD)20 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmEliminated primarily by CYP3A4-dependent metabolism. A major circulating metabolite, O-demethyl gefitinib, has pharmacological activity and may contribute to the efficacy. No apparent age or gender differences.
- Half life48 h
- ExcretionFaecal
- Urinary Excretion<1
- Clerance7.3 ml/min/kg
- ToxicityThe most common adverse events reported at the recommended 250 mg daily dose were diarrhea, rash, acne, dry skin, nausea, and vomiting
- LD50 (rat)N/A
- LD50 (mouse)N/A