April 27, 2021 (Melbourne, Australia) -- GenFleet Therapeutics, a clinical-stage biotechnology company focusing on cutting-edge therapies in oncology and immunology, today announced its first-in-human phase I trial of GFH312 has achieved dosing of subjects in the first cohort. GenFleet is the first Chinese company that moves RIPK1 inhibitor development into clinical stage.
RIPK1 modulations are correlated with cell survival and necroptosis in response to a variety of stimuli in human diseases. So far no drugs have been approved and marketed for this target in the world. The clinical development of GFH312 is expected to focus on the treatment of autoimmune and neurodegenerative diseases.
The primary objective of this study is to evaluate the safety and tolerability, and to characterize the pharmacokinetics of GFH312 through single- and multiple-ascending dose studies in healthy subjects. Preclinical data of GFH312 have demonstrated its effects in suppressing inflammation (peripheral and neuronal), reducing pathological as well as behavioral deficits, and improving survival in animal models with acute systemic inflammation resulting from multiple tissue injury.
“Indications of molecules targeting RIPK1 span across a variety of diseases and the biological mechanism of RIPK1 was confirmed through studies over a decade. Preclinical data suggest GFH312 effectively inhibit the activity of RIPK1, and the phase I trial will explore its safe dose range and tolerability in healthy subjects providing basis for further clinical development. Granted with GenFleet's first IND approval in Australia, the program will greatly accelerate the company's global multi-center clinical development.” said Dr. Yu Wang, Chief Medical Officer of GenFleet Therapeutics.
“This is GenFleet's first non-oncology clinical program, which will expand the depth and diversity of our balanced pipeline and reinforce our grand platform developing small molecules and biological therapeutics. Probing exploratory as well as mature targets, GenFleet will continue to broaden our own pipeline while seeking co-development opportunities globe-wise. We are looking forward to persistent growth of the platform and hope to deliver more innovative therapies for patients worldwide.” said Dr. Jiong Lan, Co-founder and Chief Executive Officer of GenFleet Therapeutics.
RIPK1（receptor-interacting protein kinase）is a central regulator of multiple signaling pathways modulating cell survival and death in response to a variety of stimuli. Widely expressed in human cells, the serine/threonine kinase of RIPK1 is most abundant in tissues including immune cell clusters (dendritic cells, macrophages and T cells). RIPK1 activation correlates with inflammatory, autoimmune and neurodegenerative conditions. Small-molecule RIPK1 inhibitors are currently in clinical development treating auto-inflammatory and autoimmune diseases (including psoriasis, rheumatoid arthritis, ulcerative colitis, etc.) and have the potential to tackle neurodegenerative diseases.