Basic Information

Drug ID DDPD00317 ...
Drug Name Gefitinib
Molecular Weight 446.902
Molecular Formula C22H24ClFN4O3
CAS Number 184475-35-2
SMILES COC1=C(OCCCN2CCOCC2)C=C2C(NC3=CC(Cl)=C(F)C=C3)=NC=NC2=C1
External Links
DRUGBANK DB00317
PubChem Compound 123631
PDR 3758
Drugs.com Drugs.com Drug Page

Experimental Physicochemical Property

Property Name Property Value Unit Raw Value Raw Unit Reference
Log P 3.2 - 3.2 - DRUGBANK
pKa 5.4 - 5.4,7.2 - FDA label
pKa 7.2 - 5.4,7.2 - FDA label

Pharmacokinetic/ Toxicokinetic Property

Property Name Property Value Unit Raw Value Raw Unit Annotation Factor Reference
Bioavailability 60.0 % 60.0 % PO, oral; DRUGBANK
Bioavailability 60.0 % 60.0 % PO, oral; The Pharmacological Basis of Therapeutics
C Max 341.0 ng/ml 341±208 ng/ml PO, oral; tumor; The Pharmacological Basis of Therapeutics
T Max 5.0 h 3-7 h PO, oral; DRUGBANK
T Max 5.0 h 5(3-7) h PO, oral; tumor; The Pharmacological Basis of Therapeutics
Clearance 35.7 L/h 595.0 ml/min intravenous injection, IV; DRUGBANK
Clearance 0.44 L/h/kg 7.3(2.8-21) ml/min/kg hydrolysis; tumor; patients; The Pharmacological Basis of Therapeutics
Clearance 0.72 L/h/kg 12 ml/min/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Volume of Distribution 1400.0 L 1400.0 L intravenous injection, IV; DRUGBANK
Volume of Distribution 20.0 L/kg 20(12-39) L/kg hydrolysis; tumor; patients; The Pharmacological Basis of Therapeutics
Volume of Distribution 23.0 L/kg 23 L/kg intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Half-life 48.0 h 48 h intravenous injection, IV; DRUGBANK
Half-life 48.0 h 48(10-136) h The Pharmacological Basis of Therapeutics
Half-life 34.0 h 34 h intravenous injection, IV; human, homo sapiens; Human Intravenous Pharmacokinetic Dataset
Toxicity Lethal Dose 12000.0 mg/m2 12000.0 mg/m2 Single dose; Rattus, Rat; DRUGBANK
Eliminate Route 86.0 % 86 % Faeces excretion; DRUGBANK
Eliminate Route 1.0 % <1 % Urinary excretion; tumor; Unchanged drug; The Pharmacological Basis of Therapeutics
Protein Binding 90.0 % 90 % Plasma Concentration → ; DRUGBANK
Protein Binding 90.0 % 90 % tumor; The Pharmacological Basis of Therapeutics

Maximum Dosage

Property Name Property Value Unit Raw Value Raw Unit Annotation Brand Name Component Reference
Max dose for adults 250.0 mg/day 250 mg/day PO, oral Iressa gefitinib PDR
Max dose for geriatric 250.0 mg/day 250 mg/day PO, oral Iressa gefitinib PDR

Drug Property Radar Chart

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Note: Center: Q1-1.5*IQR, Edge: Q3+1.5*IQR; Q1: Quantile 1, Q3: Quantile 3, IQR: Q3-Q1