Verastem Oncology Doses First Patient with KRAS G12D Inhibitor in Phase 1/2 Trial in China

Verastem Oncology, a biopharmaceutical company dedicated to developing new cancer treatments, has announced the dosing of the first patient in a Phase 1/2 trial in China. This trial, conducted by GenFleet Therapeutics, is evaluating GFH375/VS-7375, a KRAS G12D inhibitor.

GFH375/VS-7375 was chosen as the leading discovery program from Verastem’s collaboration with GenFleet in 2023. It is an oral, potent, and selective inhibitor targeting both ON (GTP) and OFF (GDP) states of the KRAS G12D mutation. Preclinical data presented at the American Association for Cancer Research (AACR) Annual Meeting in April 2024 showed promising results, including strong anti-tumor activity and the potential to treat brain metastases due to its oral bioavailability and efficacy in intracranial tumor models.

"We quickly identified GFH375/VS-7375 as our lead discovery program last year," said Dan Paterson, president and CEO of Verastem Oncology. "Now that the first patient has been dosed in the Phase 1/2 study by GenFleet, we look forward to using the initial clinical dose escalation data to accelerate our development path in the U.S. Given the lack of FDA-approved treatments targeting KRAS G12D, this is a significant step forward for patients with cancers such as pancreatic, colorectal, lung, and uterine."

The Phase 1 study, currently being conducted in approximately 20 hospitals in China, will assess the safety and efficacy of GFH375/VS-7375 in patients with advanced KRAS G12D mutant solid tumors. The goal is to determine the recommended Phase 2 dose (RP2D) and then evaluate its efficacy and safety further in Phase 2, focusing on advanced solid tumors like pancreatic ductal adenocarcinoma, colorectal cancer, and non-small cell lung cancer.

About GFH375/VS-7375:
GFH375/VS-7375 is a potential best-in-class, orally administered dual inhibitor for KRAS G12D mutations. It emerged as the lead discovery program from the collaboration between Verastem Oncology and GenFleet Therapeutics. GenFleet's Investigational New Drug (IND) application for GFH375/VS-7375 was approved in China in June 2024, leading to the initiation of the Phase 1/2 trial for KRAS G12D-mutant solid tumors and the dosing of the first patient in July 2024. This collaboration includes three discovery programs, with the first being the KRAS G12D inhibitor. It also provides Verastem Oncology with exclusive options to license three compounds selected for collaboration after meeting specific milestones in Phase 1 trials, giving them development and commercialization rights outside mainland China, Hong Kong, Macau, and Taiwan.

About Verastem Oncology:
Verastem Oncology is a late-stage biopharmaceutical company focused on developing and commercializing new cancer treatments. Their pipeline emphasizes RAS/MAPK-driven cancers, particularly through novel small molecule drugs that inhibit critical signaling pathways for cancer cell survival and tumor growth, including RAF/MEK and FAK inhibition.