BIBW2992 is an irreversible EGFR/HER2 inhibitor that effectively suppresses kinase activity of both receptors, including erlotinib-resistant variants. It demonstrates potent antitumor activity in preclinical models of lung cancer, including xenograft and transgenic models, with superior efficacy compared to erlotinib. BIBW2992 inhibits EGFR and HER2 phosphorylation, suppresses tumor growth in cell-based assays, and induces tumor regression in lung cancer models. It also shows significant in vivo activity, with dramatic tumor regression in xenograft models of lung cancer. BIBW2992 is effective against both EGFR and HER2 mutations, including those associated with acquired resistance to first-generation EGFR inhibitors. When combined with rapamycin, it further enhances tumor regression. The study highlights BIBW2992 as a promising candidate for targeted therapy in lung cancer patients with EGFR or HER2 mutations. Clinical trials are ongoing to evaluate its efficacy in patients.BIBW2992 is an irreversible EGFR/HER2 inhibitor that effectively suppresses kinase activity of both receptors, including erlotinib-resistant variants. It demonstrates potent antitumor activity in preclinical models of lung cancer, including xenograft and transgenic models, with superior efficacy compared to erlotinib. BIBW2992 inhibits EGFR and HER2 phosphorylation, suppresses tumor growth in cell-based assays, and induces tumor regression in lung cancer models. It also shows significant in vivo activity, with dramatic tumor regression in xenograft models of lung cancer. BIBW2992 is effective against both EGFR and HER2 mutations, including those associated with acquired resistance to first-generation EGFR inhibitors. When combined with rapamycin, it further enhances tumor regression. The study highlights BIBW2992 as a promising candidate for targeted therapy in lung cancer patients with EGFR or HER2 mutations. Clinical trials are ongoing to evaluate its efficacy in patients.