Driver mutations and epigenetic alterations are crucial in the progression of lung cancer. Many highly selective mutant targeting inhibitors, such as EGFR tyrosine kinase inhibitors, have been applied in clinical treatments with good efficacy. Drugs targeting epigenetic regulators, including inhibitors against HDAC, DNMT and non-coding RNA, show encouraging anti-tumour effects in preclinical studies, and some have entered clinical trials. Moreover, combination therapies show value in improving therapeutic efficacy and overcoming drug resistance. Overall, targeted drugs against driver mutations and epigenetic alterations, as novel anti-tumour drugs or combination therapies, will open up a new era for treating patients with lung cancer.
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