tunlametinib + cetuximab

Tunlametinib + cetuximab is a combination therapy consisting of tunlametinib (HL-085), a potent and selective small molecule inhibitor of mitogen-activated protein kinase kinase 1 and 2 (MEK1/2), and cetuximab, a chimeric monoclonal antibody targeting the epidermal growth factor receptor (EGFR). This combination is being evaluated in Phase 2 clinical trials, notably sponsored by the Chinese PLA General Hospital, for the treatment of RAS-mutated advanced gastrointestinal malignancies, including colorectal cancer and pancreatic cancer. The therapeutic rationale involves the dual blockade of the MAPK/ERK signaling pathway; while RAS mutations typically confer resistance to EGFR inhibitors like cetuximab, the addition of a MEK inhibitor like tunlametinib aims to overcome this resistance by inhibiting the pathway downstream of RAS, thereby restoring anti-tumor activity.

Other names

HL-085 + cetuximabtunlametinib + cetuximab betatunlametinib + cetuximab β