SR-8541A + immune checkpoint inhibitor

SR-8541A + immune checkpoint inhibitor is a combination therapy under investigation by Stingray Therapeutics for the treatment of advanced or metastatic solid tumors. SR-8541A is an orally bioavailable, highly selective small molecule inhibitor of Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1). ENPP1 is the primary enzyme responsible for the degradation of cyclic GMP-AMP (cGAMP), which is the endogenous ligand for the Stimulator of Interferon Genes (STING) receptor. By inhibiting ENPP1, SR-8541A prevents cGAMP degradation, thereby activating the STING pathway and promoting an inflamed tumor microenvironment characterized by increased interferon production and innate immune activation. In clinical trials, SR-8541A is administered in combination with immune checkpoint inhibitors (ICIs) such as nivolumab or pembrolizumab, which are monoclonal antibodies that block the Programmed cell death protein 1 (PD-1) receptor. This combination strategy is designed to synergistically enhance T-cell mediated anti-tumor responses and potentially overcome resistance to standard immunotherapy in various cancers, including colorectal and breast cancer.

Other names

SR-8541A in combination with nivolumabSR8541A in combination with nivolumabSR 8541A in combination with nivolumabSR-8541A in combination with pembrolizumabSR8541A in combination with pembrolizumabSR 8541A in combination with pembrolizumabENPP1 inhibitor plus ICIENPP-1 inhibitor plus ICIENPP 1 inhibitor plus ICI