Simotinib is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities[1].
Simotinib inhibits in a dose-dependent manner EGFR and the growth of human A431 tumor cells with high expression of EGFR, with no significant activity on other investigated kinases[1].
Simotinib has been shown to exert its antitumor activity by inhibiting EGFR phosphorylation in nude xenograft model[1].
[1]. Hu XS, et al. Safety, tolerability, and pharmacokinetics of simotinib, a novel specific EGFR tyrosine kinase inhibitor, in patients with advanced non-small cell lung cancer: results of a phase Ib trial. Cancer Manag Res. 2019;11:4449-4459. Published 2019 May 13.