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.
GFH276 is developed with the novel mechanism by recruiting intracellular cyclophilin A (CypA) protein to target RAS proteins across most wild-type/mutant subtypes, and exerted potent anti-tumor activities in cellular & tumor models harboring RAS mutations or RTK alterations. In preclinical research, GFH276 also demonstrated profound inhibition of MAPK signaling pathway.
The first-in-human study of GFH375 initiated by GenFleet in China has progressed into phase II and the preliminary efficacy & safety data of this study were selected into the rapid oral presentation at the upcoming 2025 American Society of Clinical Oncology (ASCO) Annual Meeting.
The event will take place from Apr. 25th to 30th in Chicago, where the preclinical findings of GenFleet’s multiple large- and small-molecule therapies (GFH276, GFS202A, and GFH375/VS-7375) will be unveiled. With their diverse molecular modalities and broad-spectrum indications, the novel therapies exemplify the robustness and creativity embedded in GenFleet's pipeline composition.
The KROCUS study delivered impressive efficacy across all trial participants and particularly exceptional tumor response among brain-metastatic patients. Additionally, the regimen demonstrated better safety/tolerability over fulzerasib monotherapy in second-line and above NSCLC treatment;
