regorafenib eye drops

Regorafenib is a multi-kinase inhibitor developed by Bayer that targets several pathways involved in angiogenesis, oncogenesis, and the tumor microenvironment. While the oral tablet formulation (Stivarga) is approved for the treatment of metastatic colorectal cancer, gastrointestinal stromal tumors, and hepatocellular carcinoma, Bayer also explored a topical ophthalmic formulation for neovascular age-related macular degeneration (nAMD). This formulation was designed to inhibit vascular endothelial growth factor receptors (VEGFR1, -2, -3), TIE2, and platelet-derived growth factor receptor (PDGFR), which are critical drivers of pathological neovascularization and vascular leakage in the retina. The Phase IIa/IIb DREAM study evaluated the efficacy of regorafenib eye drops compared to intravitreal ranibizumab in treatment-naïve patients. However, the study failed to demonstrate sufficient efficacy to support further development, leading to the termination of the ophthalmic program for nAMD.

Other names

regorafenib ophthalmic solutionregorafenib