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tunlametinib + fulzerasib
- Development stage
- Unknown
- Lead developer
- GenFleet Therapeutics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Tunlametinib + fulzerasib is a combination therapy being evaluated in Phase 2 clinical trials for the treatment of KRAS G12C-mutated non-small cell lung cancer (NSCLC). Tunlametinib (HL-085) is a small-molecule, allosteric inhibitor of MEK1 and MEK2, which are key kinases in the MAPK/ERK signaling pathway. Fulzerasib (GFH925/IBI351) is a potent and selective covalent inhibitor of the KRAS G12C mutation, which locks the protein in its inactive GDP-bound state. By simultaneously inhibiting the KRAS G12C driver and its downstream effector MEK, the combination aims to achieve more robust suppression of oncogenic signaling and delay the development of resistance. This combination is being studied in trials sponsored by Sun Yat-sen University, following the individual approvals of tunlametinib for NRAS-mutant melanoma and fulzerasib for KRAS G12C-mutant NSCLC in China.
- Other names
- Tunlametinib + GFH925Tunlametinib + IBI351
02
Targets
KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)
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