Abstract Conjugated polymers exhibit unique structural and optoelectronic properties, enabling precise modulation of chemical reactions within cellular microenvironments. This review highlights recent advances in CP‐directed biomedical strategies, focusing on their roles in light‐driven biophotocatalysis, photodynamic and photothermal therapies, and precision cellular regulation. By facilitating targeted redox transformations, gas generation, and supramolecular interactions, CPs provide spatiotemporal control over complex biological processes. The integration of CPs into dynamic assemblies and biointerfaces enables responsive, minimally invasive interventions for cancer, inflammation, and metabolic dysfunctions. Furthermore, emerging approaches that combine artificial intelligence with molecular design are accelerating the development of CP‐based platforms for personalized medicine. These interdisciplinary innovations underscore the transformative potential of CPs in therapeutic modulation, diagnostic enhancement, and the development of next‐generation biomedical devices.