Yuhan Corporation is set to reveal preliminary results from its phase 1/2 clinical trial of YH42946, an oral HER2-targeted therapy candidate, by year-end.
The company announced on Monday that it presented a poster at the 2026 World Conference on Lung Cancer (WCLC), detailing the design and progress of YH42946’s first-in-human clinical trial.
YH42946, an oral small molecule tyrosine kinase inhibitor (TKI), was licensed from J INTS BIO in 2023. It targets HER2 and is being developed for patients with solid tumors exhibiting HER2 mutations, amplifications, overexpression, or EGFR exon 20 insertion mutations.
This multicenter, open-label study aims to evaluate YH42946’s safety, tolerability, pharmacokinetics (PK), and antitumor efficacy in adult patients with locally advanced or metastatic solid tumors.
In phase 1 part 1, researchers are exploring optimal dosing by gradually increasing from 5 mg to 240 mg. Initially using once-daily (QD) oral administration, they’ve added a twice-daily (BID) cohort based on PK modeling and simulation results. A backfill strategy is being employed to bolster safety, PK, and efficacy data at selected doses.
Phase 2 will compare two doses from part 1 in a 1:1 ratio to determine the recommended dose. The study will then expand to evaluate other solid tumors with HER2 abnormalities.
Primary endpoints include safety and tolerability assessed through treatment-related adverse events. Secondary measures encompass pharmacokinetics and antitumor effects, including objective response rate (ORR), duration of response (DoR), disease control rate (DCR), and progression-free survival (PFS).
Preclinical studies showed YH42946’s antitumor effects in models with HER2 mutations, amplifications, overexpression, and EGFR exon 20 insertion mutations, including intracranial tumors. These findings were published in ‘npj Precision Oncology’ this February.
Yuhan Corporation expects to report initial results on safety, tolerability, pharmacokinetics, and preliminary antitumor effects from the dose escalation phase by year-end. These findings will inform the recommended dose selection, with plans to initiate the dose expansion phase in early 2027.
Dr. Kim Yeol-hong, Chief Executive Officrr (CEO) of Yuhan’s Research and Development (R&D) division, stated that this phase 1/2 trial will allow them to thoroughly assess YH42946’s safety and antitumor efficacy, guiding the dose recommendations and future development strategy.
Yuhan Corporation, founded in 1926 by the late Dr. Yoo Il-han, marks its centennial this year. The company specializes in prescription and over-the-counter medications, with a strong focus on new drug research and development.