Antengene Corporation has announced receiving approval from the US Food and Drug Administration (FDA) to initiate a Phase I clinical study for its ATG-017, an extracellular regulated protein kinase 1/2 (ERK1/2) inhibitor. The Shanghai-based biotech company will commence the joint part of the Phase I ETASER study, assessing the safety, pharmacokinetics, and preliminary efficacy of the drug in advanced solid tumors when combined with nivolumab.
ATG-017: Mechanism and Target Pathway
ATG-017 is an oral, selective small-molecule inhibitor of ERK1/2 signaling, which plays a crucial role in cell proliferation by regulating cell growth and cell cycle progression. ERK1/2 is a serine/threonine protein kinase involved in the regulation of the RAS-MAPK pathway, thereby affecting cell proliferation and other biological processes. More than 30% of cancer patients have disorders in the RAS-MAPK pathway, with the most common changes being mutations in the RAS or BRAF genes. ERK inhibitors can target both RAS and BRAF mutation-related diseases simultaneously.
Pre-Clinical Results and Global Approvals
Pre-clinical data demonstrated that ATG-017, when combined with an anti-PD-L1 monoclonal antibody (mAb), can transform cold tumors into hot tumors in a mouse model, which are typically resistant to immunosuppressants at immune checkpoints. The drug has already obtained multiple clinical trial approvals in Australia and the US for the treatment of advanced solid tumors and hematologic malignancies.-Fineline Info & Tech
