Tarceva

Erlotinib

Clinical data
Trade names	Tarceva
AHFS/Drugs.com	Monograph
MedlinePlus	a605008
License data	EU EMA: Tarceva US FDA: Erlotinib
Pregnancy category	US: D (Evidence of risk)
Routes of administration	Oral tablets
ATC code	L01XE03 (WHO)
Legal status
Legal status	UK: POM (Prescription only) US: ℞-only
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
Identifiers
IUPAC name N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy) quinazolin-4-amine
CAS Number	183321-74-6 Y
PubChem CID	176870
IUPHAR/BPS	4920
DrugBank	DB00530 Y
ChemSpider	154044 Y
UNII	J4T82NDH7E
KEGG	D07907 Y
ChEBI	CHEBI:114785 Y
ChEMBL	CHEMBL553 Y
ECHA InfoCard	100.216.020
Chemical and physical data
Formula	C22H23N3O4
Molar mass	393.436 g/mol
3D model (Jmol)	Interactive image
SMILES COCCOc1cc2c(cc1OCCOC)ncnc2Nc3cccc(c3)C#C
InChI InChI=1S/C22H23N3O4/c1-4-16-6-5-7-17(12-16)25-22-18-13-20(28-10-8-26-2)21(29-11-9-27-3)14-19(18)23-15-24-22/h1,5-7,12-15H,8-11H2,2-3H3,(H,23,24,25) Y Key:AAKJLRGGTJKAMG-UHFFFAOYSA-N Y

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.