GenFleet receives EMA approval for phase Ib/II study of GFH925 (KRAS G12C inhibitor) in combination with ERBITUX® (cetuximab) treating patients with advanced NSCLC in first-line setting

SHANGHAI,March 1,2023 -- GenFleet Therapeutics,a clinical-stage biotechnology company focusing on cutting-edge therapies in oncology and immunology,announced today that European Medicine Agency (EMA) approved the phase Ib/II study of GFH925 (KRASG12C inhibitor) in combination with ERBITUX® (cetuximab). This is the first therapy combining a KRASG12C inhibitor and cetuximab granted with CTA approval to treat advanced patients with KRASG12C-mutant NSCLC (non-small cell lung cancer) in the first-line setting.

With study concept proposed by GenFleet,the trial is led by Professor Rafael Rosell,a world-renowned expert in particular in the field of lung cancer,with scores of clinical research centers participating in the study across Europe. GenFleet will firstly initiate the overseas study,followed by domestic trials conducted by its partner Innovent Biologics,to accelerate the clinical development of the combination therapy treating NSCLC in first-line setting.

"GFH925 is an investigational product with promising efficacy and good safety profile as monotherapy developed by Chinese biotech. This product has been granted breakthrough therapy designation (BTD) by NMPA in China. The innovative and thoughtful idea of combining GFH925 with Erbitux will potentially pave the way for bringing KRAS inhibitors to treat NSCLC in the first-line setting. The study is among the few combination trials that target the frontline treatment and is in leading position when compared with other pharmaceutical companies. We look forward to seeing data from this study." said Professor Rafael Rosell,Quiron-Dexeus University Institute and Catalan Institute of Oncology.

"As GenFleet's first multi-center study in Europe,it highlights our ability for novel design and our efficiency executing cross-border combination trials. Currently,GenFleet and our partner are conducting a number of trials in different regions across the globe,demonstrating the broad prospects of GFH925 in clinical development. Through collaboration with our industry-leading partners,we hope innovative therapies can be delivered fast to benefit patients worldwide. " said by Yu Wang,M.D.,Ph.D.,Chief Medical Officer of GenFleet.

About GFH925X0201 and GFH925

The multi-center study of GFH925 in combination with cetuximab is to kick off in scores of clinical rsearch centers worldwide and sets its objectives to evaluate the safety/tolerance,efficacy and the pharmacokinetic characteristics of the combination in advanced NSCLC patients harboring KRASG12C mutation.

The phase I data of GFH925 monotherapy were presented at ASCO and CSCO annual meetings in 2022. Of 21 patients with NSCLC treated at 600mg BID (the recommended phase 2 dose),better efficacy signal was observed,with investigator assessed ORR 61.9% and DCR 100%. GFH925 monotherapy has been granted with breakthrough therapy designation by CDE,to treat advanced NSCLC patients with KRASG12C mutation that have received at least one prior line of systemic therapy.

By covalently and irreversibly modifying the cysteine residue of KRASG12C protein,GFH925 inhibits the GTP/GDP exchange,an essential step in pathway activation. Preclinical cysteine selectivity studies demonstrated high selectivity of GFH925 towards G12C. Subsequently,GFH925 inhibits the downstream signal pathway to induce tumor cells' apoptosis and cell cycle arrest.

About ERBITUX® (cetuximab)

ERBITUX is an IgG1 monoclonal antibody targeting the epidermal growth factor receptor (EGFR). As a monoclonal antibody,the mode of action of ERBITUX is distinct from standard non-selective chemotherapy treatments in that it specifically targets and binds to the EGFR. This binding inhibits the activation of the receptor and the subsequent signal-transduction pathway,which results in reducing both the invasion of normal tissues by tumor cells and the spread of tumors to new sites.

About GenFleet Therapeutics

GenFleet Therapeutics,a clinical-stage biotechnology company focusing on cutting-edge therapies,is dedicated to serving significant global unmet medical needs in oncology and immunology. Based on the deep understanding of disease biology and translational medicine,GenFleet's proprietary and fully integrated R&D platform highlights multiple cutting-edge products with novel mechanisms and global IP.

Since its inception in 2017,GenFleet has built up industry-leading capabilities and expertise in developing novel drug candidates - both small molecules and biologics. Its pipeline includes over 10 programs,many of which have entered multi-regional clinical trials across China (including Taiwan),the United States,Europe and Australia. To date,GenFleet has over 5 clinical studies encompassing IND stage to phase II studies and completed co-development partnerships with a number of publicly listed companies worldwide.

GenFleet is expected to progress additional programs into the clinic,as well as transition from a clinical stage biotech company into a commercial stage biopharmaceutical company in the next 3-5 years.

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