HLX97 / Shanghai Henlius Biotech, Fosun Pharma - LARVOL DELTA

Henlius Starts First-in-Human Trial of Novel KAT6A/B Inhibitor HLX97 in Advanced Tumours (TipRanks) - "The trial will test HLX97 as a monotherapy and in combination with fulvestrant in HR-positive, HER2-negative locally advanced or metastatic breast cancer, targeting resistance to endocrine therapy linked to KAT6A amplification."

Trial status • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer

In the field of prospective layout of early-stage pipeline, several new molecules have been approved for the clinical trials (The Manila Times) - "FXS0683, a next-generation Bcl-2 inhibitor, was approved for Phase I clinical trials in hematological malignancies. Innovative molecule including HLX97 (a KAT6A/B small molecule inhibitor) and HLX3901 (tetra specific antibody of DLL3×DLL3×CD3×CD28) were approved for clinical trials, widely covering refractory solid tumors such as breast cancer and small cell lung cancer."

New trial • Breast Cancer • Hematological Malignancies • Neuroendocrine Carcinoma • Small Cell Lung Cancer

Identification of novel KAT6A/B inhibitors with enhanced antitumor activity and reduced hematologic toxicity (AACR 2025) - "Additionally, the inhibition of H3K23 acetylation in ZR-75-1 cells was analyzed by Western blotting. HLX97-069/053 emerged as the top two candidates, exhibiting superior enzymatic inhibition and enhanced selectivity against KAT5/7/8, along with more potent cytotoxic effects in ZR-75-1 cells, in head-to-head comparisons with PF-07248144. In summary, these preclinical data provide compelling evidence that we have identified novel KAT6A/B inhibitors with best-in-class potential. Confirmation of the final candidate will depend on the outcomes of the forthcoming pilot toxicity studies, with an IND application anticipated by the end of 2025."

Breast Cancer • Oncology • Solid Tumor • KAT6A