A sperm-driven micromotor is presented as a targeted drug delivery system, which is appealing to potentially treat diseases in the female reproductive tract. This system is demonstrated to be an efficient drug delivery vehicle by first loading a motile sperm cell with doxorubicin hydrochloride (DOX-HCl, an anticancer drug), then guiding it, using a synthetic magnetic harness, to an in vitro cultured tumor spheroid, and finally delivering the drug locally once the sperm cell is free by an integrated mechanical release mechanism. The sperm release mechanism is designed to liberate the sperm when it hits the tumor walls, allowing the sperm to swim into the tumor and deliver the drug through sperm-cancer cell membrane fusion. In our experiments, sperm cells exhibited a high drug encapsulation capability and drug carrying stability, convenient to minimize the toxic effects and unwanted drug accumulation in healthy tissues. Moreover, sperms are excellent candidates to operate in physiological environments, as they do neither express pathogenic proteins nor proliferate to form undesirable colonies, unlike other cells or microorganisms. Overall, this sperm-hybrid micromotor is a biocompatible platform that can be used in gynecological healthcare, treating or detecting cancer or other diseases in the female reproductive system in the future.