GFH276 is the third candidate in GenFleet’s RAS-targeted matrix to enter clinical research, following successful development of a marketed KRAS G12C inhibitor (fulzerasib) and a phase-II KRAS G12D inhibitor (GFH375).
"Over the past eight years, we've built a powerful pipeline that includes the first China-developed KRAS inhibitor. Anchored by a leading-edge RAS-targeted matrix, the pipeline tackles critical unmet needs globally in cancers such as pancreatic, lung, and colorectal cancer. Riding the waves of innovation, we've kept moving forward and delivered novel therapeutics and solid out-licensing milestones, for the benefit of patients and the value creation of shareholders."
The conference will take place in Barcelona, Spain from Sept. 6-9, with a mini oral presentation scheduled for Sept. 7 to highlight the efficacy and safety data of GFH375 in patients with advanced non-small cell lung cancer (NSCLC).
Fast Track is a process designed by the FDA to facilitate the development and expedite the review of drugs to treat serious conditions and fill an unmet medical need. Programs with FTD are eligible for more frequent interactions with FDA to discuss the candidate’s development plan, as well as a rolling review of NDA or BLA to facilitate Accelerated Approval and Priority Review if relevant criteria are met.
Fulzerasib was the first China-developed KRAS G12C inhibitor that had its NDA approved with Priority Review Designation in Aug 2024 by NMPA. Fulzerasib has also earned Class 1 recommendation in treatment for KRAS G12C-mutant NSCLC in the 2025 CSCO guidelines, offering patients a new option of targeted therapy with durable efficacy and good tolerability.
Among 49 patients orally administered at daily dosages of 400 or 600 mg: 43 patients who received at least one post-treatment tumor assessment achieved an objective response rate (ORR) of 42% and a disease control rate (DCR) of 91%; the ORR was 52% and DCR was 100% among 23 efficacy-evaluable PDAC patients, and the ORR was 42% and DCR was 83% among 12 efficacy-evaluable NSCLC patients.
Through extensive preclinical research, the poster highlights the anti-tumor activity of GFH375, as well as its mechanistic advantage in dual ON/OFF inhibition of KRAS G12D. Specifically, cell-based assays demonstrated GFH375’s superior selective inhibition of the target protein; in the comparative studies of animal models, GFH375 induced significant tumor responses that outperformed the efficacy of multiple other RAS-inhibiting therapeutics and chemotherapy.
GFS202A is the world’s first clinical-stage GDF15/IL-6 bispecific antibody for cachexia, as well as the first China-developed GDF15-targeted therapy entering clinical development.
