CVD series DDR1 inhibitors

CVD series DDR1 inhibitors are a novel class of highly selective, orally available small-molecule inhibitors targeting Discoidin Domain Receptor 1 (DDR1). Developed by Curere using a non-kinase scaffold-hopping approach combined with fragment-based drug discovery, these compounds act as Type II, DFG-out state-specific binders that occupy a previously unexploited pocket in the DDR1 kinase domain. DDR1 is a collagen-activated receptor tyrosine kinase that orchestrates extracellular matrix (ECM) remodeling, pro-survival signaling, and immune exclusion in the tumor microenvironment. By inhibiting DDR1, these compounds reprogram the collagen-rich matrix, disrupt tumor-stroma interactions, and enhance T-cell infiltration, thereby potentially improving the efficacy of PD-1/PD-L1 blockade. They are primarily being investigated for the treatment of ECM-abundant malignancies, including pancreatic ductal adenocarcinoma (PDAC), triple-negative breast cancer (TNBC), and non-small cell lung cancer (NSCLC).

Other names

CVD-series DDR1 inhibitors