Epidermal growth factor receptor (EGFR) inhibitor, Icotinib

Epidermal growth factor receptor (EGFR) inhibitor, Icotinib:

Epidermal growth factor receptor (EGFR):

HER/ErbB family of transmembrane receptors

Dimerizes on ligand binding

Intracellular tyrosine kinase (TK) domain

Activation leads to downstream effector pathways, cellular proliferation, etc.

NSCLC: Activating mutations in TK domain -

in-frame deletions in exon 19

single amino acid substitutions in exon 21

EGFR TK mutations present in ~10% of NSCLC

Potential Benefits

Clinical Status

Phase I completed in healthy volunteers and Chinese NSCLC patients:

Icotinib was well-tolerated.
In a dose-dependent manner, Icotinib has a disease control rate of 56%-90% in Chinese NSCLC patients.

A Phase II and III (a fast track) trial in Chinese NSCLC patients has begun. Middle analysis from this trial are expected in the second half of 2009.