GFH375

GFH375 is an orally bioavailable, highly selective and potent small molecule inhibitor targeting the KRAS G12D mutation in both its active ("ON", GTP-bound) and inactive ("OFF", GDP-bound) states. It is designed to disrupt the GTP/GDP exchange cycle of KRAS G12D, thereby inhibiting downstream signaling pathways such as RAF/MEK/ERK that drive tumor cell proliferation. Preclinical studies have demonstrated strong anti-tumor efficacy as a single agent in multiple KRAS G12D mutant cancer models, including pancreatic ductal adenocarcinoma (PDAC), colorectal cancer, and non-small cell lung cancer (NSCLC). GFH375 also shows potential for treating brain metastases due to its ability to cross the blood-brain barrier. The drug candidate has shown good oral bioavailability and safety in early clinical trials[2][3][6].

Other names

GFH375GFH-375GFH 375VS-7375VS7375VS 7375