This multicenter phase I trial investigated the safety, tolerability, pharmacokinetics (PK), and efficacy of KN046....In the NSCLC subgroup, all patients were with EGFR mutation. the ORR was 6.3% (95% CI 0.8% to 20.8%), and the median DOR was 17.3 (95% CI 16.6 to NE) months with a 1-year DOR rate of 100.0%. The median PFS was 2.5 (95% CI 1.3 to 2.8) months; the median OS was 7.8 (95% CI 5.3 to 14.8) months with a 1-year OS rate of 41.7% (95% CI 25.6% to 57.0%).