Drug intelligence / Profile preview

erlotinib

Development stage
Approved
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

Erlotinib is a small molecule tyrosine kinase inhibitor that selectively targets the epidermal growth factor receptor (EGFR) tyrosine kinase. By reversibly binding to the ATP-binding site of EGFR, erlotinib blocks downstream signaling pathways involved in cell proliferation and survival. This inhibition slows or stops the growth of cancer cells with abnormal EGFR activity. Erlotinib is primarily used for the treatment of metastatic non-small cell lung cancer (NSCLC) with specific EGFR mutations (exon 19 deletions or exon 21 L858R substitution mutations), and in combination with gemcitabine for advanced pancreatic cancer that cannot be surgically removed. It was first approved by regulatory agencies in 2004 and is marketed under the brand name Tarceva[1][2][3][4][5][6].

Brand names
Tarceva
Other names
erlotinib hydrochloride
02

Targets

EGFR (Epidermal growth factor receptor)JAK2 V617F (Janus kinase 2 V617F mutant)

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