Lung cancer is the uncontrolled proliferation of cells lining the air passages and tissues of the lungs. It is the second most  common  cancer in  both men  and women.   It is estimated that lung cancer accounts  for  about 14%  of all  new cancer  cases.

Based on the morphology  of  cells,  lung  cancer  can be classified into two  subtypes: small  cell  lung  cancer (SCLC) and non-small cell lung cancer (NSCLC).   On one hand, SCLC is more aggressive and fast growing cancer type  that  starts  in  the lung tissue and migrates  to  other  parts  of  the body. On  the  other  hand,  NSCLC is less aggressive and accounts for about 80% to 85% of all lung cancer cases.  

Icotinib is an orally available selective EGFR TKI.

Icotinib is a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that is used for the treatment of non-small cell lung cancer (NSCLC).

Mechanism of Action:

  • Icotinib selectively binds to the ATP binding site of the EGFR, inhibiting the dimerization and phosphorylation of the receptor.
  • This inhibition prevents the activation of oncogenic cell signaling pathways that promote cell survival, proliferation, tumorigenesis, and anti-apoptosis.
  • Icotinib specifically targets EGFR and its mutants, showing meaningful inhibitory activity only towards these targets.

In vitro studies have shown that icotinib inhibits EGFR activity in a dose-dependent manner, with complete inhibition at higher concentrations. Firstly, icotinib blocks EGFR-mediated intracellular tyrosine phosphorylation in cancer cells. Secondly, it exhibits a broad spectrum of antitumor activity and is especially effective against tumors expressing higher levels of EGFR. Besides, in vivo studies in mice carrying human tumor-derived xenografts have demonstrated potent dose-dependent antitumor effects of icotinib.

References:

[1] Pranav Gupta, et al. February 2018Translational Cancer Research 7(S1):S26-S30.

[2] Tan F, et al.Lung Cancer. 2012 May;76(2):177-82.