4-methyl erlotinib is an analog of erlotinib by the addition of a methyl group at the four position of the phenyl group. erlotinib is a tyrosine kinase inhibitor which acts on the epidermal growth factor receptor (egfr) [1].the epidermal growth factor receptor (egfr) autocrine pathway has been important for cancer development and progression, including cell proliferation, apoptosis, angiogenesis, and metastatic spread [2].erlotinib inhibits egfr-associated kinase activity by binding to the egf-activated receptor, with the phenyl group at one end sequestered in a hydrophobic pocket of the kinase domain and the ether linkages at the opposite end projecting into solvent [1].erlotinib can prolong survival in patients with non–small-cell lung cancer after first-line or second-line chemotherapy [3].
[1] stamos, j. ,sliwkowski, m.x. and eigenbrot, c. structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor. the journal of biological chemisty 277(48), 46265-46272 (2002).
[2] ciardiello f, tortora g. a novel approach in the treatment of cancer: targeting the epidermal growth factor receptor[j]. clinical cancer research, 2001, 7(10): 2958-2970.
[3] shepherd f a, rodrigues pereira j, ciuleanu t, et al. erlotinib in previously treated non–small-cell lung cancer[j]. new england journal of medicine, 2005, 353(2): 123-132.
