GenFleet Therapeutics (2595.HK) announced today that preclinical data of three novel drug candidates have been selected for the poster presentation at the 2026 Annual Meeting of the American Association for Cancer Research (AACR), which is scheduled to take place in San Diego, US from April 17 to 22, 2026. GenFleet’s RAS-targeted matrix encompasses multiple selective and Pan RAS inhibitors, as well as targeted therapies for potential co-mutations associated with the RAS pathway. This matrix includes small and large molecules with diversified modalities and mechanisms; preclinical research data of three compounds - GFH276 (non-degrading molecular glue), GFS784 (novel ADC linking functional antibody with synergistic targeted payload) and GFH603 (molecular glue-like covalent allosteric activator) - will be featured at this upcoming conference.
Title: Preclinical evaluation of GFH276 monotherapy and combination therapy for RAS-mutant tumors
Session Category: Experimental and Molecular Therapeutics
Session Start: 4/21/2026 9:00:00 AM
Session End: 4/21/2026 12:00:00 PM
Poster Number: 4565
GFH276, a molecular glue Pan (ON) RAS inhibitor with favorable oral bioavailability, showed potent suppression of most activated wild-type and mutant RAS subtypes. Preclinical research conducted across multiple KRAS-mutant models demonstrated GFH276's significant and dose-dependent anti-tumor efficacy in tumor types including non-small cell lung cancer, colorectal cancer, pancreatic cancer, cholangiocarcinoma and endometrial carcinoma. Furthermore, GFH276 also exhibited notable synergistic effects when administered in combination with cetuximab or anti-PD-1 monoclonal antibody, highlighting broad therapeutic potential of both monotherapy and combinational treatments.
Title: GFS784, a next-generation ADC with a novel Pan RAS (ON) inhibitor payload
Session Category: Experimental and Molecular Therapeutics
Session Start: 4/21/2026 9:00:00 AM
Session End: 4/21/2026 12:00:00 PM
Poster Number: 4536
GFS784, linking a Pan RAS inhibitor payload to cetuximab, was the first candidate developed from GenFleet's globally innovative FAScon™ ADC platform combining functional antibodies with synergistic targeted payloads. Preclinical studies showed GFS784’s potent activity in both DXd-sensitive and Dxd-resistant RAS-mutant tumor models, while also exerting anti-tumor activity in EGFR-mutant and osimertinib-resistant models, bringing a potential next-generation ADC therapeutic regimen to patients.
Title：GFH603: A molecular glue-like allosteric activator of the KEAP1-CUL3 E3 ligase complex for targeting NRF2-activated tumors
Session Category: Experimental and Molecular Therapeutics
Session Start: 4/19/2026 2:00:00 PM
Session End: 4/19/2026 5:00:00 PM
Poster Number: 348
KEAP1 is a frequently co-mutated gene in RAS-mutant tumors. Dysfunction of the KEAP1 protein can lead to aberrant activation of its downstream NRF2, causing resistance to various cancer treatments. Designed to restore the KEAP1-CUL3 E3 ligase activity and promote the NRF2 degradation, GFH603 demonstrated potent anti-tumor efficacy across multiple preclinical models in single-agent research and in combination with Pan RAS inhibitors. The molecular glue-like allosteric activator holds the potential to provide a novel targeted therapy for NRF2-driven malignancies.
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