Other name


International/Other brands





Prescription products

PMS-erlotinibTablet150 mgOralPharmascience Inc
PMS-erlotinibTablet100 mgOralPharmascience Inc
TarcevaTablet25 mg/1OralPhysicians Total Care, Inc.
TarcevaTablet100 mg/1OralGenentech, Inc.
TarcevaTablet100 mgOralHoffmann La Roche
TarcevaTablet100 mg/1OralPhysicians Total Care, Inc.
TarcevaTablet, film coated100 mgOralRoche Registration Limited
TarcevaTablet25 mgOralHoffmann La Roche
TarcevaTablet25 mg/1OralGenentech, Inc.
TarcevaTablet150 mg/1OralPhysicians Total Care, Inc.




Erlotinib hydrochloride (trade name Tarceva, Genentech/OSIP, originally coded as OSI-774) is a drug used to treat non-small cell lung cancer, pancreatic cancer and several other types of cancer. Similar to gefitinib, erlotinib specifically targets the epidermal growth factor receptor (EGFR) tyrosine kinase. It binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. Erlotinib has recently been shown to be a potent inhibitor of JAK2V617F activity. JAK2V617F is a mutant of tyrosine kinase JAK2, is found in most patients with polycythemia vera (PV) and a substantial proportion of patients with idiopathic myelofibrosis or essential thrombocythemia. The study suggests that erlotinib may be used for treatment of JAK2V617F-positive PV and other myeloproliferative disorders.


Locally Advanced Non-Small Cell Lung Cancer, Locally Advanced Pancreatic Cancer, Lung Cancer Non-Small Cell Cancer (NSCLC), Metastatic Non-Small Cell Lung Cancer, Pancreatic Cancer Metastatic

Other indications


Mechaism of action



Erlotinib is about 60% absorbed after oral administration and its bioavailability is substantially increased by food to almost 100%. Peak plasma levels occur 4 hours after dosing. The solubility of erlotinib is pH dependent. Solubility decreases pH increases. Smoking also decrease the exposure of erlotinib.


Metabolism occurs in the liver. 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.


Symptoms of overdose include diarrhea, rash, and liver transaminase elevation. The most common adverse reactions (>50%) in NSCLC are rash, diarrhea, anorexia and fatigue. The most common adverse reactions (>50%) in pancreatic cancer are fatigue, rash, nausea and anorexia.