Nano/micromotors are artificial robots at the nano/microscale that are capable of transforming energy into mechanical movement. In cancer diagnosis or therapy, such “tiny robots” show great promise for targeted drug delivery, cell removal/killing, and even related biomarker sensing. Yet biocompatibility is still the most critical challenge that restricts such techniques from transitioning from the laboratory to clinical applications. In this review, we emphasize the biocompatibility aspect of nano/micromotors to show the great efforts made by researchers to promote their clinical application, mainly including non-toxic fuel propulsion (inorganic catalysts, enzyme, etc.), bio-hybrid designs, ultrasound propulsion, light-triggered propulsion, magnetic propulsion, dual propulsion, and, in particular, the cooperative swarm-based strategy for increasing therapeutic effects. Future challenges in translating nano/micromotors into real applications and the potential directions for increasing biocompatibility are also described.