Across different dose levels (100-900 mg QD) in the early-stage clincal development, GFH375 had demonstrated encouraging antitumor activity with a manageable safety and tolerability profile in heavily pretreated patients across tumor types including pancreatic cancer and non-small cell lung cancer (NSCLC).
he presentation demonstrated encouraing efficacy of GFH375 at the 600 mg QD dose level in NSCLC patients, with nearly 100% of enrolled patients having distant metastases and over 40% having received at least two prior lines of therapy.
GenFleet Therapeutics (2595.HK) announced that GFH375 has entered a phase II study for first-line treatment of patients with advanced, KRAS G12D-mutant non-small cell lung cancer (NSCLC). The multicenter, open-label, randomized trial features three arms including GFH375 monotherapy and two combination regimens pairing GFH375 with the EGFR antibody (cetuximab) or with chemotherapy (pemetrexed).
The two combination therapies include GFH375 plus GFS202A, the world’s first cachexia-targeted bispecific antibody (GDF15/IL-6 bispecific antibody), and GFH375 plus GFH276, a Pan RAS (ON) inhibitor. GFH375/VS-7375 received China’s first Breakthrough Therapy Designation for monotherapy in KRAS G12D-mutant metastatic pancreatic cancer in February 2026, following Fast Track designation from the U.S. FDA for KRAS G12D-mutant metastatic pancreatic ductal adenocarcinoma (PDAC) granted in 2025.
The updated data of GFH375 for KRAS G12D-mutant non-small cell lung cancer (NSCLC) will be presented in an oral presentation at the IASLC 2026 World Conference on Lung Cancer (WCLC); the event will take place from September 12 to 15 in Seoul, with accepted abstracts to be released on the official WCLC website by late August.
TARGET-D 201 is an open-label, multi-center study in the U.S. to evaluate both the monotherapy and in combination with full-dose cetuximab in patients with second-line metastatic PDAC. The study also evaluates the combination with cetuximab in the first-line PDAC setting.
The oral KRAS G12D (ON/OFF) inhibitor was previously granted with FDA’s FTD for the treatment of KRAS G12D-mutant pancreatic ductal adenocarcinoma (PDAC) in 2025. Besides, GFH375 received the first two Breakthrough Therapy Designations in China for monotherapy treating G12D-mutant pancreatic cancer and NSCLC respectively.
GenFleet Therapeutics（2595.HK） announced the updated clinical data of GFH375 monotherapy treating KRAS G12D-mutant solid tumors were presented in the oral abstract session at the 2026 American Society of Clinical Oncology (ASCO) annual meeting on June 1 local time.
