rbs2418

RBS2418 is a potent and selective small molecule inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase I (ENPP1). It is designed as an immune modulator to promote anti-tumor immunity by inhibiting ENPP1, which leads to increased levels of endogenous 2'-3'-cyclic guanosine monophosphate–adenosine monophosphate (cGAMP) and adenosine triphosphate (ATP), while reducing adenosine production in tumors. By protecting cGAMP from hydrolysis, RBS2418 enhances activation of antigen-presenting cells and subsequent T cell activation. The drug has demonstrated excellent oral bioavailability, full ENPP1 inhibition at all tested dose levels, and favorable safety in early clinical trials. It is being developed for use both as monotherapy and in combination with checkpoint inhibitors such as pembrolizumab for advanced unresectable, recurrent or metastatic solid tumors, including colorectal cancer[2][3][4][5][6][7][8].