GENFLEET-B (02595) has unveiled updated efficacy data from its Phase II trial evaluating GFH375 as a monotherapy for patients with pretreated KRAS G12D-mutant non-small cell lung cancer (NSCLC). The findings were presented as an oral presentation at the World Conference on Lung Cancer (WCLC), held in Seoul, on September 14.

At the 600mg QD dose, GFH375 demonstrated robust antitumor activity in a heavily pretreated population, with nearly 100% of enrolled patients presenting with distant metastases and over 40% having received two or more prior lines of therapy. As of the data cutoff, 71 patients were evaluable for response, yielding an objective response rate (ORR) of 59.2%, a confirmed ORR (cORR) of 52.1%, and a disease control rate (DCR) of 93%. Notably, the median progression-free survival (mPFS) for patients who had not previously received taxane-based therapy reached 9.6 months at a median follow-up of 11 months. The 12-month overall survival (OS) rate across the entire cohort was 77%, observed at a median follow-up of 11.2 months.

Dr. Yu Wang, Chief Medical Officer of GENFLEET-B, commented, "This is the second time GFH375's clinical data in NSCLC has been selected for presentation at WCLC, and this larger dataset continues to showcase its impressive efficacy in treating pretreated NSCLC. Based on the Phase I/II results, GFH375 received Breakthrough Therapy Designation (BTD) in China for pretreated KRAS G12D-mutant NSCLC and has entered the world's first Phase III study of an oral KRAS G12D inhibitor in this setting (the 'Qilin-Fei 01' trial). Our RAS-targeted therapeutic matrix encompasses multiple targets, molecular formats, and diversified clinical strategies, including both monotherapy and frontline combination approaches for NSCLC. We are confident in advancing the 'Qilin-Fei 01' study and anticipate further positive developments across the product's clinical programs."

As of September 4, 2026, a total of 75 patients with KRAS G12D-mutant NSCLC had received oral GFH375 at the 600mg QD dose. Among these, 98.7% had distant metastases, including bone (37.3%), brain (16%), and liver (13.3%) involvement. All patients had received prior platinum-based chemotherapy and immune checkpoint inhibitors (90.7% had received both concurrently), with 42.7% having undergone two or more prior lines of therapy. Additionally, 38.7% had prior taxane exposure (including docetaxel), and 64% had received an immune checkpoint inhibitor within 90 days before their first dose of GFH375.

The mPFS for all patients was 8.3 months, with taxane-pretreated patients showing an mPFS of 8.1 months. The median overall survival (mOS) had not yet been reached. As of June 17, 2026, safety and tolerability data from the 75 patients receiving single-agent GFH375 indicated a manageable profile. The majority of treatment-related adverse events (TRAEs) were grade 1-2, with the most common being diarrhea, vomiting, and nausea, most of which resolved with supportive care. Grade 3 or higher TRAEs were primarily diarrhea and elevated ALT, and overall, TRAEs were well-controlled with no treatment-related deaths reported. No new safety signals emerged compared to earlier reported data. Notably, patients who had received an ICI within the 90 days prior to initiating GFH375 exhibited a less favorable safety/tolerability profile than those with a longer interval, particularly showing a higher incidence of grade 3 or higher hepatotoxicity (16.7% versus 0%).