GenFleet Therapeutics (Shanghai) Inc. (GenFleet, stock code: 2595) announced that the first patient has been dosed in a Phase Ib/II trial of GFH375, an oral KRAS G12D (ON/OFF) inhibitor, combined with cetuximab or chemotherapy for advanced solid tumors, including first-line pancreatic ductal adenocarcinoma (PDAC). The trial is being conducted at Peking University Cancer Hospital and other investigational sites.

According to the announcement, China’s National Medical Products Administration approved the clinical trial application of GFH375 in combination with cetuximab or chemotherapy in an open-label, multi-center Phase Ib/II study (GFH375X1202). The chemotherapy arm will be administered to previously untreated patients with advanced PDAC to assess efficacy, safety, tolerability, and pharmacokinetic profile.

The plan includes approximately 15 investigational sites, evaluating GFH375 plus albumin-bound paclitaxel and gemcitabine in first-line PDAC patients, and GFH375 combined with cetuximab for advanced PDAC or colorectal cancer. GFH375 has also been granted Fast Track Designation by the U.S. Food and Drug Administration for KRAS G12D-mutant locally advanced or metastatic PDAC across all lines of therapy.

GenFleet indicated that GFH375 is an orally active, potent, and highly selective small-molecule inhibitor designed to target KRAS G12D in both GTP- and GDP-bound states. Preclinical data demonstrated dose-dependent efficacy, along with a low off-target risk in relevant assays. The company has entered a development collaboration with Verastem, under which Verastem may license GFH375 (also designated VS-7375) for development and commercialization rights outside of China, while GenFleet retains the rights within China.

The announcement included forward-looking statements cautioning that actual outcomes may differ due to market, policy, and research and development uncertainties. A further statement reminded shareholders and potential investors to exercise caution, as there is no guarantee of successful development or ultimate marketing of GFH375.