GENFLEET-B (02595.HK): Phase III study of world's first oral KRAS G12D inhibitor for NSCLC initiated; second registrational clinical study of GFH375 completes first patient enrolment

NewTimeSpace News: On 10 August 2026, GenFleet Therapeutics (Shanghai) Inc. (stock code: 02595) published a voluntary announcement, announcing that GFH375 (an oral KRAS G12D inhibitor) has entered a registrational Phase III clinical study (the "Qilin-Fei 01") in China as monotherapy for the treatment of non-small cell lung cancer (NSCLC). The study is a multicentre, open-label, randomised controlled Phase III study evaluating GFH375 versus docetaxel in patients with KRAS G12D-mutated, locally advanced unresectable or metastatic NSCLC who have failed standard therapy; the study will be conducted at more than 40 study sites nationwide, with the first patient enrolled at Nanjing Drum Tower Hospital recently.

According to the announcement, GFH375 had entered the world's first registrational Phase III clinical study of an oral KRAS G12D inhibitor for pancreatic cancer last year (the "Qilin-Yi 01"), and this year it has obtained two breakthrough therapy designations (BTDs) in China for monotherapy treatment of KRAS G12D-mutated NSCLC and pancreatic cancer. Currently, no targeted therapy for patients with KRAS G12D mutations has been launched globally; previous studies have shown that NSCLC patients with KRAS mutations are less sensitive to chemotherapy and more prone to drug resistance, and KRAS G12D patients have lower PD-L1 expression with lower response rates to PD-1/L1 inhibitor monotherapy among various KRAS mutation subtypes, while second-line and later-line immunotherapy and chemotherapy with or without anti-angiogenic agents also offer limited objective response rates and overall survival benefits. GFH375 has demonstrated potential best-in-class efficacy in treating NSCLC among global KRAS G12D inhibitors, with the latest monotherapy later-line NSCLC data to be presented as an oral presentation at this year's World Conference on Lung Cancer (WCLC).

GFH375 is an oral, highly active, highly selective small-molecule KRAS G12D (ON/OFF) inhibitor that binds non-covalently to the KRAS G12D protein and inhibits its binding to downstream effector proteins, thereby disrupting the sustained activation of downstream pathways by KRAS G12D in cells and ultimately potently inhibiting tumour cell proliferation; preclinical studies have shown that the tumour growth inhibition of GFH375 monotherapy increases with dosage and treatment duration, with low off-target risk in kinase selectivity and safety target assays. The Company has entered into a licence and early co-development agreement with Verastem Oncology for three products with RAS/MAPK-driven cancers; Verastem selected GFH375/VS-7375 as the lead programme of the collaboration in December 2023 and obtained a licence for GFH375 in January 2025, with the licence granting Verastem development and commercialisation rights outside China while GenFleet retains such rights within China.

Professor Lu Shun of Shanghai Chest Hospital commented that targeted therapy for lung cancer has developed rapidly over the past 20 years, but there remains a huge unmet need in the treatment of KRAS G12D-mutated NSCLC, with no related targeted drug approved globally, and that GFH375's clinical exploration in this indication is at the forefront globally, with the preliminary data presented as oral presentations at last year's ASCO and WCLC being encouraging. Dr. Wang Yu, Chief Medical Officer of GenFleet, stated that GFH375 has demonstrated excellent efficacy in treating NSCLC since entering clinical development in 2024, with related study data continuously entering oral presentations or late-breaking abstracts (LBAs) at multiple international academic conferences, and that based on the Phase I/II monotherapy efficacy and the current NSCLC treatment landscape, the Company is confident in rapidly advancing the various therapeutic trials of GFH375 for NSCLC. The announcement also noted that, pursuant to Rule 18A.05 of the Listing Rules, the Company cannot guarantee the successful development or eventual commercialisation of GFH375, and shareholders and potential investors should exercise caution when dealing in the shares of the Company.

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