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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].

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