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GenFleet Therapeutics Cleared to Begin Phase I/II Trial in China of KRAS G12D Inhibitor

NEW YORK – GenFleet Therapeutics on Wednesday said China's National Medical Products Administration (NMPA) has cleared the firm's clinical trial application to begin a Phase I/II trial of KRAS G12D inhibitor GFH375 in patients with advanced solid tumors harboring a KRAS G12D mutation.

The Phase I portion of the trial will evaluate safety and tolerability in solid tumors and determine a recommended Phase II dose. The Phase II part of the trial will explore the drug's efficacy in KRAS G12D-mutant solid tumors, including pancreatic, colorectal, and non-small cell lung cancer. Researchers will also explore mechanisms of response and resistance to GFH375.

GenFleet Chief Medical Officer Yu Wang said in a statement that this trial will focus on monotherapy treatment with GFH375, but the firm hopes to evaluate combination approaches in future research. GFH375 inhibits both the "ON" (GTP-bound) and "OFF" (GDP-bound) states of KRAS G12D. In preclinical research published earlier this year, GenFleet found GFH375 could potentially be used to treat patients with brain metastases and that it had favorable combination potential with Verastem Oncology's avutometinib RAF/MEK clamp therapy.

Last year, GenFleet out-licensed GFH375 along with two other programs targeting RAS-driven cancers to Verastem Oncology in countries outside of China in a deal worth up to $625.5 million.

Earlier this year, GenFleet began a Phase III trial of its KRAS G12C inhibitor GFH925 in KRAS G12C-mutant colorectal cancer. The firm is also seeking approval for GFH925 in China as a second-line treatment of KRAS G12C-mutant non-small cell lung cancer.