By Fineline Cube 
GenFleet Therapeutics (Shanghai) Inc. (HKG: 2595) today announced that the first patient has been enrolled in a Phase Ib/II study of its oral KRAS G12D inhibitor, GFH375, at Peking University Cancer Hospital. The trial evaluates two combination regimens—GFH375 with cetuximab and GFH375 with chemotherapy—targeting advanced solid tumors harboring the KRAS G12D mutation. The chemotherapy‑based arm is slated to become a first‑line treatment for pancreatic ductal adenocarcinoma (PDAC).
Key Highlights
- First‑in‑class Oral KRAS G12D Inhibitor – GFH375 is a highly selective, non‑covalent inhibitor that blocks KRAS G12D‑mediated effector signaling.
- Dual‑Regimen Design – Combines GFH375 with either the EGFR blocker cetuximab or standard chemotherapy.
- Strategic Licensing – GenFleet’s partnership with Verastem grants exclusive outside‑China rights to GFH375, while GenFleet retains mainland China rights.
Clinical Development Pathway
| Phase | Status | Milestones |
|---|---|---|
| Phase Ib/II | Enrollment launched | Primary endpoint: objective response rate (ORR) in KRAS G12D+ solid tumors |
| Chemotherapy Arm | Planned first‑line PDAC therapy | Expected to progress to Phase III if ORR ≥ 35 % |
| Cetuximab Arm | Evaluating synergy with EGFR inhibition | Secondary endpoints: progression‑free survival (PFS), overall survival (OS) |
Pre‑clinical data demonstrate a robust, dose‑dependent antitumor effect and a favorable kinase‑selectivity profile, underscoring GFH375’s potential to transform KRAS‑driven oncology.
Strategic Collaboration with Verastem
- Three‑Product RAS/MAPK Portfolio – GenFleet and Verastem have signed a licensing and early‑stage collaboration for three RAS‑driven agents.
- Exclusive License Option – Verastem holds an exclusive option to license each product upon meeting predefined Phase I milestones.
- Geographic Rights – Verastem gains development and commercialization rights outside Greater China; GenFleet retains rights within mainland China.
- GFH375 Lead Program – Selected as the partnership’s flagship in December 2023, GFH375’s license marks the first product to materialize from the collaboration.
Forward‑Looking Statements
This release contains forward‑looking statements that involve risks and uncertainties. Actual results may differ materially.-Fineline Info & Tech