zipalertinib + quemliclustat

TAS6417 + AB680 is a combination therapy being developed by Taiho Pharmaceutical in collaboration with Arcus Biosciences for the treatment of non-small cell lung cancer (NSCLC). The combination consists of TAS6417 (zipalertinib), an orally available, irreversible small molecule tyrosine kinase inhibitor that selectively targets EGFR exon 20 insertion mutations, and AB680 (quemliclustat), a potent small molecule inhibitor of CD73 (ecto-5'-nucleotidase). CD73 is an enzyme responsible for the production of immunosuppressive adenosine in the tumor microenvironment; by inhibiting it, AB680 aims to enhance anti-tumor immune responses. This combination approach seeks to provide synergistic efficacy by directly blocking oncogenic EGFR signaling while simultaneously alleviating immune suppression. It is currently being evaluated in Phase 1 clinical trials, often in further combination with the anti-PD-1 monoclonal antibody zimberelimab.

Other names

TAS6417 + AB680zipalertinib + quemliclustatCLN-081 + AB680