HLX97-053 / Fosun Pharma, Shanghai Henlius Biotech - LARVOL DELTA

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

Shanghai Henlius Biotech…announced that the NMPA has approved the IND application for HLX97, a novel oral small molecule inhibitor targeting Lysine Acetyltransferase 6A/B (KAT6A/B) independently developed by the company, for the treatment of advanced or metastatic solid tumors (Henlius Press Release) - "It is expected to provide a new therapeutic option for patients with breast cancer and other solid tumors who have progressed on standard therapies."

New trial • Breast Cancer

Henlius to Present Three Preclinical Studies at AACR 2025 (Henlius Press Release) - "The American Association for Cancer Research 2025 Annual Meeting (AACR 2025) is set to take place from April 25 to April 30 in Chicago, the United States. Henlius will share three latest preclinical research results from its pipeline programs. The results to be presented include the novel anti-PD-L1/VEGF bispecific antibody HLX37, a novel KAT6A/B inhibitors with best-in-class potential, and a first-in-class ADC linker-payload featuring a highly differentiated killing mechanism."

Preclinical • Oncology