MSA-2 / Merck (MSD) - LARVOL DELTA

Discovery of MK-2118, a Small-Molecule Agonist of STING. (PubMed, ACS Med Chem Lett) - "Optimization efforts in this series faced challenges with uniform activity across species, cell shift, and steep structure activity relationships. Herein we report lead optimization efforts guided by structure-based drug design to identify the MSA-2 analog MK-2118."

Journal • Oncology • STING

Merck’s oral cancer drug targeting STING boosts PD-1 immune blockade in mice (FierceBiotech) - "...scientists at Merck & Co. have designed a STING agonist that can be taken by mouth...The drug, dubbed MSA-2, cleared tumors in mice bearing colorectal cancer. In tumor models that were poorly responsive to PD-1 blockade, combining MSA-2 and inhibition of the checkpoint PD-1 outperformed monotherapy at controlling tumor growth and prolonging survival....The drug was well tolerated and induced complete tumor regressions in 80% to 100% of treated animals."

Preclinical • Colorectal Cancer • Gastrointestinal Cancer • Oncology