The first-in-human study of GFH375 initiated by GenFleet in China has progressed into phase II and the preliminary efficacy & safety data of this study were selected into the rapid oral presentation at the upcoming 2025 American Society of Clinical Oncology (ASCO) Annual Meeting.
The event will take place from Apr. 25th to 30th in Chicago, where the preclinical findings of GenFleet’s multiple large- and small-molecule therapies (GFH276, GFS202A, and GFH375/VS-7375) will be unveiled. With their diverse molecular modalities and broad-spectrum indications, the novel therapies exemplify the robustness and creativity embedded in GenFleet's pipeline composition.
The KROCUS study delivered impressive efficacy across all trial participants and particularly exceptional tumor response among brain-metastatic patients. Additionally, the regimen demonstrated better safety/tolerability over fulzerasib monotherapy in second-line and above NSCLC treatment;
Cachexia is highly prevalent in cancer, and it severely affects patients’ survival rate and tolerance to cancer treatments. Extensive research conducted worldwide has identified the key roles of GDF15 and IL-6 in the progression of cachexia. To date, no therapies targeting both GDF15 and IL-6 have been approved in the world, and GFS202A is the first China-developed GDF15-targeted therapy entering clinical stage.
This multi-center, open-label (~20 sites in China) trial enrolls patients with advanced G12D-mutant solid tumors, including pancreatic ductal adenocarcinoma (PDAC), non-small cell lung cancer (NSCLC) and colorectal cancer (CRC)—three cancer types with high prevalence of G12D mutations
Fulzerasib (GFH925/IBI351) received approval in China on Aug. 21 for the treatment of adult patients with advanced NSCLC harboring KRAS G12C mutation who have received at least one systemic therapy. The first hospital prescription was issued on Aug. 31 and the medications were already shipped to chain pharmacies across the country.
The NDA approval is based on the results from a single-arm registrational study (NCT05005234) intended to evaluate the efficacy and safety of fulzerasib monotherapy in advanced NSCLC patients with KRAS G12C mutation who failed or were intolerant to the standard treatment in China. The updated data from this registration study has been published in full manuscript in the Journal of Thoracic Oncology (JTO) and selected for oral presentation at the 2024 World Conference on Lung Cancer (WCLC) .
GFH375 was selected as Verastem’s lead discovery program from its collaboration with GenFleet established in 2023. GFH375/VS-7375 is an oral, potent and selective KRAS G12D dual inhibitor of ON (GTP) and OFF (GDP) states.
