China-based GenFleet Therapeutics Inc. has announced a European multi-center clinical study and drug supply agreement with Germany’s Merck KGaA. The collaboration will conduct an open, multi-center, Phase Ib/II clinical study to assess the efficacy of combining GenFleet’s KRAS G12C inhibitor, GFH925, with Merck’s Erbitux (cetuximab) in treatment-naïve advanced non-small cell lung cancer (NSCLC) with KRAS G12C mutation. Under the agreement, GenFleet will initiate the study, and Merck will provide Erbitux for the trial. Financial details were not disclosed.
GFH925: An Innovative KRAS G12C Inhibitor
GFH925 is an in-house developed drug candidate targeting the oncogenic driver gene KRAS G12C, commonly found in lung cancer and other solid tumors. Pre-clinical data indicate that GFH925 has potential best-in-class activities, effectively inhibiting the growth of various tumor cell lines carrying KRAS G12C mutations. A Phase I dosage ascending study preliminarily found that GFH925 as a monotherapy demonstrated good safety, tolerability, and anti-tumor activities in KRAS G12C mutant advanced NSCLC with previous standard treatment failure or intolerance.
Erbitux: A Leading EGFR Targeted Therapy
Erbitux (cetuximab), the world’s first epidermal growth factor receptor (EGFR) targeted IgG1 monoclonal antibody (mAb), was originally developed by ImClone (now wholly owned by Eli Lilly) and licensed to Merck for markets outside the US and Canada in 1998. Cetuximab targets EGFR, inhibits its receptor activation, and subsequent signal transduction, reducing tumor cells’ invasion of normal tissues and spread to new sites. It also inhibits tumor cells’ ability to repair damage caused by chemotherapy and radiotherapy and inhibits the formation of new blood vessels in tumors. In vitro studies have shown that cetuximab exhibits antibody-dependent cytotoxicity (ADCC) against EGFR-positive tumor cells.-Fineline Info & Tech
