HIGHLIGHTS• Recent advances of micro/nanomotors in the field of cancer-targeted delivery, diagnosis, and imaging-guided therapy are summarized.• Challenges and outlook for the future development of micro/nanomotors toward clinical applications are discussed.ABSTRACT Micro/nanomotors have been extensively explored for efficient cancer diagnosis and therapy, as evidenced by significant breakthroughs in the design of micro/nanomotors-based intelligent and comprehensive biomedical platforms. Here, we demonstrate the recent advances of micro/nanomotors in the field of cancer-targeted delivery, diagnosis, and imaging-guided therapy, as well as the challenges and problems faced by micro/nanomotors in clinical applications. The outlook for the future development of micro/nanomotors toward clinical applications is also discussed. We hope to highlight these new advances in micro/nanomotors in the field of cancer diagnosis and therapy, with the ultimate goal of stimulating the successful exploration of intelligent micro/nanomotors for future clinical applications.