GenFleet Starts First-in-human Phase I Trial of Highly Selective CDK9 Inhibitor

May 10, 2021

May 10,2021 (Tianjin, China) -- GenFleet Therapeutics, a clinical-stage biotechnology company focusing on cutting-edge therapies in oncology and immunology, today announced that the first patient has been dosed in its first-in-human trial of GFH009. As the first highly selective CDK9 inhibitor entering clinical stage in China, GFH009 has been granted with IND approvals by both Chinese and US authorities for the treatment of recurrent/refractory hematological malignancies. 

The primary objective of this study is to evaluate the safety and tolerability of GFH009 among patients with recurrent/refractory hematological malignancies including acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL) and other lymphomas. In addition to characterizing the pharmacokinetic profile of GFH009, the study will also assess the preliminary anti-tumor activities of compound and test specific biomarkers in peripheral blood among patients. 

Preclinical studies have demonstrated that GFH009 is a potent and highly selective small-molecule inhibitor of CDK9 with more than 100 times selectivity over other CDK subtypes.

“We target at recurrent/refractory hematological malignancies in phase I trial based on the properties of CDK9 and data of biomarkers from preclinical studies, expecting to expand the clinical application of CDK inhibitors. Building on the FIH results, we will continuously refine and optimize our clinical development plan of GFH009. As GenFleet's first global multi-center trial, study of GFH009 will remarkably promote our global development of innovative drugs. " said Yu Wang, M.D./Ph.D., Chief Medical Officer of GenFleet Therapeutics.

“GenFleet has been conducting clinical trials of TGF-β R1 inhibitor and RIPK1 inhibitor in China and Australia respectively. It marks another major milestone as we proceed with synchronous enrollment of patients in China and US in the FIH trial of highly selective CDK9 inhibitor. There was no clinical proof of concept for the target of CDK9 when we started the project, which is typical of GenFleet's innovative pipeline that focuses on novel mechanisms.” said Jiong Lan, Ph.D., Chief Executive Officer of GenFleet Therapeutics. 

About GFH009 and CDK9

As a potent and highly selective small molecule CDK9 inhibitor, GFH009 exhibits strong apoptosis-inducing and anti-proliferation activities in a variety of human cell lines and animal models of diseases. It effectively inhibits the growth of tumor in various xenograft models and significantly improves survival of tumor bearing animals. Preclinical data have also suggested the potential anti-tumor effects of GFH009 in combination with BCL-2 inhibitors.

As a family of serine & threonine kinases, cyclin-dependent kinase (CDK) plays an important role in cell cycle regulation and transcription. CDK9 is one of the most potential targets for cancer therapeutics in the CDK family. Compared with non-selective CDK inhibitors, highly selective CDK9 inhibitors are advantageous in avoiding off-target toxicity against other CDK subtypes and reducing the risk of dose-limiting toxicity. Currently, no highly selective CDK9 inhibitors have been authorized with New Drug Application (NDA) approvals on the global market.