GENFLEET-B (02595): The world's first oral KRAS G12D inhibitor for the treatment of non-small cell lung cancer has entered Phase III trials, and the second registrational clinical study of GFH375 has completed the enrollment of its first patient.

GENFLEET-B (02595) announced that GFH375 (an oral KRAS G12D inhibitor) has entered a registrational phase III clinical study for monotherapy in non-small cell lung cancer (NSCLC) in China (Qilin-Fei 01). Qilin-Fei 01 is a multicenter, open-label, randomized controlled phase III study assessing the efficacy of GFH375 compared to docetaxel in KRAS G12D mutant, locally advanced unresectable or metastatic NSCLC patients whose standard treatments have failed. The study will be conducted at over 40 research centers nationwide, with the first patient recently enrolled at Nanjing Gulou Hospital. Previously, GFH375 entered the worlds first registrational phase III clinical study for oral KRAS G12D inhibitor treatment in pancreatic cancer (Qilin-Yi 01) last year; this year, GFH375 has been recognized as a breakthrough therapy (BTD) for monotherapy in KRAS G12D mutant NSCLC and pancreatic cancer in China. Currently, there are no targeted therapies available on the global market for patients with KRAS G12D mutations, and the first-line standard treatment for these patients references treatment regimens for driver gene-negative NSCLC. However, previous studies have indicated that patients with KRAS mutant NSCLC have a lower sensitivity to chemotherapy and are prone to quickly develop resistance to chemotherapy due to the effects of epigenetic regulatory mechanisms. Furthermore, KRAS G12D patients exhibit low PD-L1 expression, resulting in lower response rates to PD-1/L1 inhibitors among various KRAS mutant subtypes. The objective response rates and overall survival benefits from second-line and beyond immunotherapy, chemotherapy anti-angiogenic agents are also limited. GFH375 has demonstrated potential best-in-class efficacy for treating NSCLC among global KRAS G12D inhibitors, and the latest data on monotherapy for late-line NSCLC treatment will be presented as an oral report at this years World Congress on Lung Cancer (WCLC).