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QuickView for Erlotinib (compound)

Name: erlotinib
PubChem Compound ID: 11954378
Molecular formula: C22H24ClN3O4
Molecular weight: 429.896 g/mol
Erlotinib hydrochloride; 183319-69-9; Tarceva; Erlotinib hydrochloride (JAN/USAN); Tarceva (TN); D04023
Name: erlotinib
Name (isomeric): DB00530
Drug Type: small molecule
Brand: Tarceva
Category: Protein Kinase Inhibitors
CAS number: 183321-74-6
Indication: For the treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of at least one prior chemotherapy regimen. Also for use, in combination with gemcitabine, as the first-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer.
Pharmacology: Erlotinib is a Human Epidermal Growth Factor Receptor Type 1/Epidermal Growth Factor Receptor (HER1/EGFR) tyrosine kinase inhibitor.
Mechanism of Action:
The mechanism of clinical antitumor action of erlotinib is not fully characterized. Erlotinib inhibits the intracellular phosphorylation of tyrosine kinase associated with the epidermal growth factor receptor (EGFR). Specificity of inhibition with regard to other tyrosine kinase receptors has not been fully characterized. EGFR is expressed on the c...
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Absorption: Erlotinib is about 60% absorbed after oral administration and its bioavailability is substantially increased by food to almost 100%.
Protein binding: 93% protein bound to albumin and alpha-1 acid glycoprotein (AAG)
Biotransformation: In vitro assays of cytochrome P450 metabolism showed that erlotinib is metabolized primarily by CYP3A4 and to a lesser extent by CYP1A2, and the extrahepatic isoform CYP1A1.
Half Life: Median half-life of 36.2 hours.
Toxicity: Symptoms of overdose include diarrhea, rash, and liver transaminase elevation.
Affected organisms: Humans and other mammals
Food interaction:
Take with a glass of water.
Take at least 1 hour before or 2 hours after any food.
Drug interaction:
St. John's WortDecreased levels/effect of erlotinib
KetoconazoleThis CYP3A4 inhibitor increases levels/toxicity of erlotinib
RifampinDecreased levels/effect of erlotinib
TroleandomycinThis CYP3A4 inhibitor increases levels/toxicity of erlotinib
TrastuzumabTrastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
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