Gefitinib

Potent and selective EGFR kinase inhibitor (IC50 = 23-79 nM) [1]. Inhibits EGFR autophosphorylation and inhibits tumor growth in vivo [2]. Enhances efficacy of cytotoxic agents [3]. Inhibits growth factor production and angiogenesis [4]. Clinically useful anticancer agent.

References:

1) Baselga et al. (2000), ZD1839 (‘Iressa’) as an anticancer agent;  Drugs, 60 33

2) McKillop et al. (2005), Tumor penetration of gefitinib (Iressa), an epidermal growth factor receptor tyrosine kinase inhibitor;  Mol. Cancer Ther., 4 641

3) Sirotnak et al. (2000), Efficacy of cytotoxic agents against human tumor xenografts is markedly enhanced by coadministration of ZD1839 (Iressa), an inhibitor of EGFR tyrosine kinase; Clin. Cancer Res., 6 4885

4) Ciaradiello et al. (2001), Inhibition of growth factor production and angiogenesis in human cancer cells by ZD1839 (Iressa), a selective epidermal growth factor receptor tyrosine kinase inhibitor;  Clin. Cancer Res., 7 1459