Early diagnosis, standardized treatment, and regular monitoring are the clinical treatment principle of rheumatoid arthritis (RA). The overarching principles and recommendations of treat‐to‐target (T2T) in RA advocate remission as the optimum aim, especially for patients with very early disease who are initiating therapy with anti‐RA medications. However, traditional anti‐RA drugs cannot selectively target the inflammatory areas and may cause serious side effects due to its short biological half‐life and poor bioavailability. These limitations have significantly driven the research and application of nanomaterial‐based drugs in theranostics of RA. Nanomedicines have appropriate sizes and easily modified surfaces which can enhance their biological compatibility and prolong circulation time of drug‐loading systems in vivo. Traditional T2T regimens cannot evaluate the efficacy of drugs in real time, while clinical drug nanosizing can realize the integration of diagnosis and treatment of RA. This review bridges clinically proposed T2T concepts and nanomedicine in an integrated system for RA early‐stage diagnosis and treatment. The most advanced progress in various nanodrug delivery systems for theranostics of RA is summarized, establishing a clear path and a new perspective for further optimization of T2T. Finally, the key facing challenges are discussed and prospects are addressed.