Urethral scar formation after injury remains a clinical challenge due to the adverse urethral microenvironment and the limited tissue specificity of conventional antifibrotic drugs. To address this, the present study introduces a novel approach using a Wnt pathway inhibitor (ICG-001) functionalized with nanomaterials to improve bioavailability and therapeutic efficacy. A polyethylene glycol (PEG) was covalently grafted onto reduced graphene oxide (rGO) in order to develop a biocompatible rGO-PEG carrier, which was subsequently cross-linked with ICG-001, forming ICG-001@rGO-PEG. This nanocomposite exhibited enhanced dispersion stability, hydrophilicity, and bioactivity, which led to more effective inhibition of urethral scar formation. Gene expression analysis showed that ICG-001@rGO-PEG significantly upregulated matrix metalloproteinase-1 (MMP-1) in fibroblasts, promoting blood vessel and epithelial regeneration. These findings suggest that ICG-001@rGO-PEG could be a promising therapeutic strategy for urethral treatment, combining the benefits of nanomedicine with small-molecule inhibitors.