Preclinical data demonstrated that ORM‐5029 exhibited 10‐ to 1000‐fold enhanced efficacy in HER2‐expressing cell lines compared to treatment with SMol006, ADC targeting HER2 (Kadcyla and Enhertu).[151, 152] Cytotoxic activity of ORM‐5029 in tumor xenograft models significantly surpassed SMol006, CC‐885, as well as Kadcyla and Enhertu.[153] Phase I trial of ORM‐5029 for treating HER2‐expressing solid tumors was started on 3 October 2022 (NCT05511844).[152]. The gene discussed is ERBB2; the disease is neoplasm.