BeiGene's KAT6 inhibitor initiates Phase I clinical trial in the U.S.

On October 29, 2025, BeiGene registered a Phase I clinical trial for its KAT6 inhibitor BG-75202 targeting advanced solid tumors on ClinicalTrials.gov.

This Phase I clinical trial plans to enroll 86 patients with advanced solid tumors to evaluate the therapeutic efficacy of the KAT6 inhibitor both as a monotherapy and in combination with other agents, such as CDK4 inhibitors.

On May 2025, updated Phase I clinical data for Pfizer's KAT6 inhibitor PF-07248144 in treating ER+/HER2- metastatic breast cancer were released in an ASCO meeting abstract. The recommended dose expansion (RDE) cohort enrolled 107 patients, all of whom had previously received CDK4/6 inhibitor and endocrine therapy. Among them, 35 patients received 5mg PF-07248144 monotherapy, 43 received 5mg PF-07248144 plus fulvestrant, and 29 received 1mg PF-07248144 plus fulvestrant.

In the 1mg and 5mg PF-07248144 plus fulvestrant groups, the objective response rates (ORR) were 24.1% and 37.2%, clinical benefit rates (CBR) were 37.9% and 55.8%, median duration of response (mDOR) were 4.6 months and 15.8 months, and median progression-free survival (mPFS) were 3.6 months and 10.7 months, respectively.

Regarding safety, the most common grade 3 or higher adverse event was neutropenia. The incidence of grade 3 neutropenia was 20.7% and 39.5%, while grade 4 incidence was 0% and 7.0%, respectively. This side effect was reversible and manageable through dose adjustment. No cases of pneumonitis were reported.

In July of this year, Pfizer registered a Phase III clinical trial on ClinicalTrials.gov for its KAT6 inhibitor PF-07248144 in combination with fulvestrant to treat HR+/HER2- breast cancer.

Among Chinese companies, Insilico Medicine out-licensed its KAT6 inhibitor ISM5043 to Menarini in January 2024, with an upfront payment of $12 million and a total potential deal value exceeding $500 million. Several Chinese pharmaceutical companies have advanced KAT6 inhibitors into the clinical stage, including Qilu Pharmaceutical, Konruns Pharmaceutical, and BeiGene. At this year's AACR conference, preclinical data for additional KAT6 inhibitors were presented, including QLS1034 (Qilu Pharmaceutical), HW321005 (Humanwell Healthcare), HLX97 (Henlius), and compounds from Innogate Pharma.