Erlotinib
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| Trade names | Tarceva |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a605008 |
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Oral tablets |
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| Pharmacokinetic data | |
| Bioavailability | 59% |
| Protein binding | 95% |
| Metabolism | Hepatic (mainly CYP3A4, less CYP1A2) |
| Biological half-life | 36.2 hrs (median) |
| Excretion | >98% as metabolites, of which >90% via faeces, 9% via urine |
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| ECHA InfoCard | 100.216.020 |
| Chemical and physical data | |
| Formula | C22H23N3O4 |
| Molar mass | 393.436 g/mol |
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Erlotinib hydrochloride (trade name Tarceva) is a drug used to treat non-small cell lung cancer (NSCLC), pancreatic cancer and several other types of cancer. It is a receptor tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR).
It is marketed in the United States by Genentech and OSI Pharmaceuticals and elsewhere by Roche. In the United States as of 2015 one 150 mg pill costs between 200 and 242 USD.
Erlotinib has shown a survival benefit in the treatment of lung cancer in phase III trials. The SATURN (Sequential Tarceva in Unresectable NSCLC) study found that erlotinib added to chemotherapy improved overall survival by 19%, and improved progression-free survival (PFS) by 29%, when compared to chemotherapy alone.
The U.S. Food and Drug Administration (FDA) has approved erlotinib for the treatment of locally advanced or metastatic non-small cell lung cancer that has failed at least one prior chemotherapy regimen.
In November 2005, the FDA approved erlotinib in combination with gemcitabine for treatment of locally advanced, unresectable, or metastatic pancreatic cancer.
In lung cancer, erlotinib has been shown to be effective in patients with or without EGFR mutations, but appears to be more effective in patients with EGFR mutations. Overall survival, progression-free survival and one-year survival are similar to standard second-line therapy (docetaxel or pemetrexed). Overall response rate is about 50% better than standard second-line chemotherapy. Patients who are non-smokers, and light former smokers, with adenocarcinoma or subtypes like BAC are more likely to have EGFR mutations, but mutations can occur in all types of patients. A test for the EGFR mutation in cancer patients has been developed by Genzyme.
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