EGFR TKIs are the standard of care for EGFR mutated, advanced-stage NSCLC. Various mechanisms contribute to their resistance, among which a tertiary point mutation in the C797 residue of EGFR is the most well-known. Currently, there is no approved drug for NSCLC in patients harboring the EGFR C797S resistance mutation. BBT-176, a reversible, ATP-competitive inhibitor was developed to target such complex EGFR mutations and was shown to exhibit low nanomolar IC50 values in cell and animal efficacy models.