Name: | erlotinib |
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PubChem Compound ID: | 11954378 |
Molecular formula: | C22H24ClN3O4 |
Molecular weight: | 429.896 g/mol |
Synonyms: |
Erlotinib hydrochloride; 183319-69-9; Tarceva; Erlotinib hydrochloride (JAN/USAN); Tarceva (TN); D04023
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Name: | erlotinib |
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Name (isomeric): | DB00530 |
Drug Type: | small molecule |
Synonyms: |
OSI-774
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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. |
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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: |
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