HLX97

HLX97 is a novel oral small-molecule inhibitor targeting the lysine acetyltransferases KAT6A and KAT6B (KAT6A/B), developed by Shanghai Henlius Biotech. Designed as a potential best-in-class epigenetic modulator, HLX97 is being developed for the treatment of advanced or metastatic solid tumors, including endocrine-resistant breast cancer, castration-resistant prostate cancer, and non-small cell lung cancer (NSCLC). The drug features a fast-on/fast-off pharmacokinetic profile and high selectivity against other KAT enzymes (such as KAT5, KAT7, and KAT8) to minimize hematologic toxicities like neutropenia. By precisely inhibiting KAT6A/B activity, HLX97 modulates the expression of genes critical for tumor cell proliferation, differentiation, and apoptosis. In early 2026, HLX97 received Investigational New Drug (IND) approval from China's NMPA for a Phase 1 clinical trial evaluating its safety, tolerability, and preliminary efficacy as a monotherapy or in combination with fulvestrant.