Small molecule
PubChem CID 176870
Erlotinib
Tarceva
- Mechanism of action
- EGFR tyrosine kinase inhibitor
- In plain language
- Blocks a growth-signal switch on cancer cells that's stuck in the on position, cutting off the signal that tells the tumor to keep growing.
- How it works
- Erlotinib is an orally bioavailable, reversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. It binds the intracellular ATP-binding domain of EGFR, blocking autophosphorylation of tyrosine residues on the receptor and thereby interrupting downstream signal transduction through pathways such as RAS/MAPK and PI3K/AKT. Erlotinib shows greater binding affinity for EGFR harboring exon 19 deletions or the exon 21 L858R substitution than for wild-type EGFR, which is why efficacy is concentrated in tumors carrying these activating mutations. The net effect is suppression of the proliferative and anti-apoptotic signaling that EGFR-driven tumor cells depend on.
- Therapeutic applications
- Indicated for metastatic non-small cell lung cancer (NSCLC) in patients whose tumors harbor EGFR exon 19 deletions or exon 21 (L858R) substitution mutations, as first-line therapy, maintenance therapy, or second-line-or-greater therapy following progression on at least one prior chemotherapy regimen; and, in combination with gemcitabine, as first-line treatment for locally advanced, unresectable, or metastatic pancreatic cancer.
- Class
- Small molecule
- Therapeutic area
- Oncology
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