derazantinib + atezolizumab

Derazantinib + atezolizumab is an investigational combination therapy evaluated primarily for advanced or metastatic urothelial cancer with FGFR1–3 genetic aberrations. Derazantinib is an orally available, spectrum-selective small molecule inhibitor of the fibroblast growth factor receptor (FGFR) family, with potent activity against FGFR1, FGFR2, and FGFR3 kinases and additional inhibitory effects on colony-stimulating factor 1 receptor (CSF1R) and vascular endothelial growth factor receptor 2 (VEGFR2). Atezolizumab is a monoclonal antibody immune checkpoint inhibitor targeting programmed death-ligand 1 (PD-L1), restoring antitumor T-cell activity. The rationale for combining these agents lies in the potential immunomodulatory effect of CSF1R inhibition by derazantinib to enhance the efficacy of PD-L1 blockade by atezolizumab. The combination has been studied in phase 1b/2 trials but did not demonstrate sufficient efficacy to warrant further development in metastatic urothelial cancer[1][3][5][8].

Other names

derazantinib + Tecentriq