2023 ASCO | Multi-center Data for Combination Study of GenFleet's GFH018 (TGF-β R1 inhibitor) with Anti-PD-1 Antibody Demonstrates Significant Potential to Enhance Efficacy of Immune Checkpoint Inhibitors among ICI-naïve Patients

SHANGHAI and CHICAGO,June 6,2023 -- GenFleet Therapeutics,a clinical-stage biotechnology company focusing on cutting-edge therapies in oncology and immunology,today published the latest results from the phase Ib/II study of GFH018 (TGF-β R1 inhibitor) with toripalimab（anti-PD-1 antibody）at the 2023 American Society of Clinical Oncology Meeting in Chicago.

The data demonstrated promising anti-tumor activity and tolerability among patients with recurrent/metastatic nasopharyngeal carcinoma (R/M NPC). Over 40% patients enrolled have received ≥3 lines of prior therapies and This combination therapy demonstrated significant potential to enhance efficacy of immune checkpoint inhibitors (ICIs) among ICI-naïve patients and subjects in late-line setting.

A phase Ib/II study of GFH018 in combination with toripalimab in recurrent/metastatic nasopharyngeal carcinoma（R/M NPC）.

Abstract #: 6026

This trial (NCT04914286) is the first global multi-center study of a TGF-β R1 inhibitor combined with an anti-PD-1 antibody conducted by a Chinese biotech. As of 20 April 2023,41 patients with R/M NPC were enrolled in China (including the Chinese mainland and Taiwan) and Australia.

As of 20 April 2023,among the 32 patients with post-baseline tumor assessments,the overall response rate (ORR) was 31.3%,and disease control rate (DCR) was 50%; 10 pts achieved partial response (PR),and 6 pts with stable disease (SD).

Among 17 ICI-naïve patients (without prior treatment of ICIs),the ORR was 47.1%,and DCR was 64.7%,8 pts achieved PR,and 3 pts SD; a total of 4 pts that achieved PR have their target lesion decreased by over 50% from baseline.

The majority of patients experienced treatment-related adverse events (TRAEs) of 1/2 grades,and 11 patients (26.8%) had ≥ Grade 3. The most common TRAEs were anaemia,hyponatraemia,rash,fatigue,etc. No adverse events were observed that affected subjects' vital health conditions,and there were no bleeding events that have been reported in clinical trials of large molecules targeting TGF-β pathway.

The team of Professor Mai Haiqiang,Director of the Department of Nasopharyngeal Carcinoma，Sun Yat-sen University Cancer Center visited the ASCO site together with GenFleet's clinical executives. As the principal investigator of the study （NCT04914286）,Professor Mai stated,"we are pleased to collaborate with GenFleet and present our latest results to the global audience at ASCO. The study suggested a potential immunomodulation effect of GFH018 enhancing efficacy of anti-PD-1 antibodies among ICI-naïve patients. Currently no innovative therapies targeting TGF-β pathway has been approved for the market and we look forward to further advances in this therapy."

Yu Wang,M.D./Ph.D.,Chief Medical Officer of GenFleet expressed his expectations about the product's clinical potential in future,"GFH018 as GenFleet's first product entering clinical trial is expected to alleviate the suppressed tumor immune microenvironment and reduce the incidence of severe chemoradiation-induced pneumonitis accompanying TGF-β-induced fibrosis. Thus,GFH018 combined with anti-PD-1 inhibitor will provide novel options for virus-related cancer patients. Currently,GenFleet is at the forefront in the development of the small-molecule immunotherapies targeting TGF-β pathway. More positive results from this combination therapy of GFH018 applying to multiple solid tumors will be disclosed in future academic conferences."

About GFH018 and TGF-β R1

Developed by GenFleet Therapeutics,GFH018 is an orally administered TGF-β R1 inhibitor pand entered into phase I clinical trial in 2019. The phase Ib/II trial of GFH018 with PD-1 inhibitor treating patients with advanced solid tumors is underway in China (including the Chinese mainland and Taiwan) and Australia; the other study is a phase II trial of GFH018,PD-1 inhibitor with concurrent chemoradiotherapy treating patients with locally advanced & unresectable NSCLC in China.

In the microenvironment of advanced solid tumors,TGF-β signaling pathway can promote epithelial mesenchymal transition (EMT) & metastasis,induce the formation of cancer stem cells and their functional maintenance,inhibit anti-tumor immunity,enhance vasculature and fibrosis,and ultimately result in tumor progression.

Among patients of hepatocellular carcinoma,glioma,colorectal cancer,lung cancer,pancreatic cancer,urothelial cancer and other solid tumors,high expression of genes related to TGF-β signaling pathway is frequently discovered in their blood and tumor tissues. The expression level is positively correlated to the malignancy & poor differentiation of tumor and unfavorable prognosis in patients. TGF-β pathway also plays a crucial role especially for non-oncology diseases such as fibroblast-associated fibrosis with inflammation and tissue injury. Therefore,diseases could be treated with GFH018 such as idiopathic pulmonary fibrosis,interstitial pneumonia,primary biliary cirrhosis and others.

About GenFleet

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.

CONTACT: Yun Zeng,Phone: +86-13482182145