SR-8541A + pembrolizumab

SR-8541A + pembrolizumab is a combination therapy under clinical development for solid tumors and metastatic colorectal cancer. SR-8541A is an orally administered small molecule inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase family member 1 (ENPP1), designed to block ENPP1 activity. This action is thought to enhance anti-tumor immunity by activating the STING pathway, increasing immune cell infiltration, and promoting interferon response, thereby making tumors more responsive to immune checkpoint blockade. Pembrolizumab is a well-established monoclonal antibody targeting the programmed cell death protein 1 (PD-1), acting as an immune checkpoint inhibitor to augment T-cell mediated anti-tumor immunity. The combination has demonstrated preclinical and early clinical evidence of synergistic activity, supporting its ongoing clinical evaluation as an anti-cancer immunotherapy.

Other names

SR 8541ASR8541ASR-8541AENPP1 inhibitor (SR-8541A)Keytruda (brand name for pembrolizumab)