TKIs like gefitinib, erlotinib, and afatinib block the downstream signaling required for tumor proliferation by binding to the intracellular domain of EGFR. Gefitinib was the first active EGFR-targeting-TKI and has shown moderate response rates during OSCC monotherapy, ranging from 1.4% to 10.6% (187). The gene discussed is EGFR; the disease is neoplasm.