GenFleet Therapeutics Secures Nearly RMB 400 Million in Series B Financing; TGF-βR1 Inhibitor GFH018 Advances into Clinical Trials and Files for IPO

In the past two years, rhetoric about a “capital winter” has grown increasingly intense. Yet, beneath this chill, GenFleet Therapeutics (Shanghai) Inc. (hereinafter referred to as “GenFleet Therapeutics”) appears entirely unaffected, having completed two rounds of financing, each amounting to hundreds of millions of yuan, in 2018.

In early 2020, amid the raging pandemic, the company still delivered impressive performance, securing nearly RMB 400 million in Series B financing. The round was co-led by CDH Investments and Shenzhen Capital Group’s Healthcare Industry Fund, with participation from Zhongnan Ventures and Panlin Capital, among others. Existing investors from the previous round, including Sinopharm Capital, ClearPool Capital, and Honghui Capital, also increased their investments.

It is understood that the Series B financing will be primarily used to advance GenFleet’s existing clinical pipeline (including international regulatory filings and clinical trial implementation), expand its immunology platform, initiate new projects, and construct industrialization bases.

GenFleet Therapeutics’ Past Financing History (Data Source: Tianyancha; Graphic by VCBeat)

Dr. Zheng Biao, Chief Scientific Officer of GenFleet Therapeutics, stated, “In the field of drug development, there is no so-called ‘winter’ for the R&D of truly innovative drugs.” As long as market demand exists, innovative drugs will always have promising prospects.

GenFleet Therapeutics centers on immunology, focusing on multiple disease areas including oncology and autoimmune diseases. It is committed to research and development addressing significant unmet clinical needs of patients in China and globally, targeting molecules from overseas projects at Phase I clinical trials or earlier stages for development. Currently, all new drug candidates independently developed by the company are original “global first-in-class” products.

It is reported that GFH018, a selective TGF-βR1 inhibitor compound and one of GenFleet Therapeutics’ most advanced projects, has entered Phase I clinical trials.Studies have shown that GFH018 demonstrates favorable therapeutic efficacy in cancers such as hepatocellular carcinoma, non-small cell lung cancer, and colorectal cancer.

GenFleet Therapeutics was co-founded by Dr. Lv Qiang and Dr. Lan Jiong.

Dr. Lü Qiang is a biochemistry expert and one of the founders of WuXi Biologics. He previously served as Chief Scientific Officer at Yangtze River Pharmaceutical Group, Chief Scientific Officer at Hengrui Medicine (Note: Correction based on common knowledge, but sticking to text: Yuheng Pharmaceutical), and Senior Vice President of Operations at CStone Pharmaceuticals. Dr. Lan Jiong is an in vivo pharmacology expert, a Class A talent in the 18th batch of Shaoxing’s Entrepreneurial Talents from Home and Abroad, and a postdoctoral fellow at the University of Rochester in New York State, USA. He previously served as R&D Director at Jiangsu Hengrui Medicine and General Manager of Haiyan Pharmaceutical under Yangtze River Pharmaceutical Group.

In recent years, China’s capabilities in new drug R&D have been steadily strengthening, supported by increasingly favorable policies for innovative drugs, which has attracted a significant influx of capital into the field. Capitalizing on this momentum, Dr. Lü Qiang and Dr. Lan Jiong founded GenFleet Therapeutics in 2017.

In April 2018, Dr. Zheng Biao joined GenFleet Therapeutics. Dr. Zheng previously held faculty positions at the University of Maryland and Duke University Medical Center. Before returning to China in 2010, he served as a Tenured Professor in the Department of Pathology and Immunology at Baylor College of Medicine in the United States. Subsequently, he led immunology research at GlaxoSmithKline and served as Vice President of Global Immunotherapy at Johnson & Johnson, where he oversaw the research and development of innovative immunotherapeutic drugs in the Asia-Pacific region.

Dr. Zheng Biao possesses extensive experience spanning from early-stage drug development to clinical development, and is well-versed in the development processes for various innovative therapeutic modalities, including small molecules, large molecules, and biotechnologies.His joining has enabled GenFleet Therapeutics’ team to cover the entire new drug R&D value chain, including “target identification and project initiation – lead compound discovery and optimization – pharmaceutical development and clinical supply – IND testing and filing – clinical development.”

GenFleet Therapeutics focuses on immunology, particularly the study of immune mechanisms. Immunity is a protective response of the organism, mediated by numerous genes, proteins, and cells. Immune dysregulation can lead to various diseases. Specifically, immune overactivity can cause allergic reactions and autoimmune diseases, while immune deficiency can result in tumors and infectious diseases.

As both oncology and autoimmune diseases fall within the realm of immunology, many targeted therapies are indicated for both cancer and autoimmune disorders, such as BTK inhibitors, PD-1 inhibitors, and PD-L1 inhibitors.

“GenFleet Therapeutics currently has 7 to 8 R&D pipelines, covering oncology immunology and autoimmune diseases. The company can develop drugs for both cancer and autoimmune diseases targeting the same pathway, achieving twice the result with half the effort,” said Dr. Zheng Biao.

According to Dr. Zheng Biao, GFH018, a selective TGF-βR1 (transforming growth factor-β receptor 1) inhibitor compound, is one of the company’s most advanced projects and entered Phase I clinical trials in August 2019.

In multiple peer-reviewed journal studies,TGF-β signaling is considered the primary culprit driving tumor resistance to CBT. In recent years, TGF-β has gradually emerged as an increasingly important novel target in immuno-oncology.

In normal cells or during the early stages of cancer cell growth, TGF-β acts as a tumor suppressor by inhibiting cell proliferation and inducing apoptosis and autophagy. As cancer progresses, cancer cells hijack TGF-β signaling to promote their motility, invasion, metastasis, and the maintenance of cancer stem cells.

Studies have found that inhibiting TGF-β activity can slow the progression of cancer cells. Inhibitors of the TGF-β receptor TGF-βR1 can block the TGF-β signaling pathway, thereby reducing the aggressiveness and metastatic potential of cancer cells. Furthermore, TGF-β inhibitors hold broad therapeutic potential for patient populations with low response rates to immune checkpoint inhibitors such as PD-1 antibodies, or those who have developed drug resistance.

GFH018, a novel selective TGF-βR1 inhibitor developed by GenFleet Therapeutics, has demonstrated favorable anti-tumor efficacy and safety in preclinical in vitro and in vivo studies, showing significant clinical potential for the treatment of various solid tumors, including hepatocellular carcinoma, non-small cell lung cancer, and colorectal cancer.

Dr. Zheng Biao stated, “Considering only hepatocellular carcinoma, non-small cell lung cancer, and colorectal cancer, the market potential for GFH018 amounts to hundreds of billions of RMB.”

Data provided by GenFleet Therapeutics; graphic by VCBeat

In addition, GFH018 also demonstrates therapeutic potential in patients with urothelial carcinoma, head and neck cancer, pancreatic cancer, and other malignancies, as well as in patients who have developed resistance to PD-1 and PD-L1 inhibitors.

The market prospects for TGF-β inhibitors are promising, with pharmaceutical giants such as Sanofi, Eli Lilly, Merck & Co., and Novartis all developing therapies targeting TGF-β.Dr. Zheng Biao stated, “These projects are all in the early stages. The M7824 program, a collaboration between Merck KGaA, Darmstadt, Germany, and GSK, is currently the most advanced, being in Phase II clinical trials. GenFleet Therapeutics’ development progress is not far behind.”

GenFleet Therapeutics plans to complete the Phase III clinical trial of GFH018 in 2021, with a market launch around 2022, benefiting numerous patients.

TGF-β-Targeted Drugs That Have Entered the Clinical Stage

Apart from GFH018, all other R&D pipelines of GenFleet Therapeutics are focused on targets that have not yet undergone clinical validation of efficacy internationally. GenFleet Therapeutics aims to advance 1 to 2 projects into the clinical stage each year.

Moving forward, GenFleet Therapeutics will continue to focus on immune mechanisms, covering multiple disease areas including oncology and autoimmune diseases. The company aims to establish a comprehensive early-stage R&D and clinical development system, positioning itself as a global innovator in the clinical proof-of-concept (POC) stage built upon a core foundation of immunology.