Verastem selects GFH375/VS-7375 as lead program of pact with GenFleet

Verastem announced a potential KRAS G12D oral inhibitor as the lead program of its discovery and development collaboration with GenFleet Therapeutics. GFH375/VS-7375 is an orally bioavailable and selective small molecule KRAS G12D inhibitor. Preclinical models demonstrate strong tumor regression as a single agent and support approaches in combination with Verastem Oncology’s RAF/MEK clamp avutometinib as well as other rational combinations across KRAS G12D-driven cancers. KRAS G12D represents 26% of all KRAS mutations, making it the most prevalent KRAS mutation in human cancer. KRAS G12D mutation occurs most commonly in pancreatic, colorectal, endometrial and non-small cell lung cancers. As previously announced, the discovery and development collaboration between Verastem Oncology and GenFleet aims to advance three oncology discovery programs related to RAS pathway-driven cancers. The collaboration builds on the strengths of both companies in oncology small molecule drug development, enabling Verastem Oncology to partner its clinical development and regulatory expertise with GenFleet’s accomplished discovery capabilities. This synergistic collaboration includes Verastem Oncology’s experience and established network of collaborators, including scientific and clinical experts in RAS biology and RAS pathway-driven cancers and GenFleet’s accomplishments with its KRAS G12C inhibitor program. The IND filing and initial Phase 1 studies will be led and funded by GenFleet in China. The collaboration provides Verastem Oncology with an exclusive option to obtain a license to each of the three compounds in the collaboration after successful completion of pre-determined milestones in a Phase 1 trial. The licenses would give Verastem Oncology development and commercialization rights outside of China while GenFleet would retain development and commercialization rights inside of China.