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Therapeutic metallodrugs have gained substantial success in cancer treatment and also motivate the active exploration of metallodrugs for cancer theranostics. However, it remains a challenge to engineer metallodrugs with desired therapy efficacy and safety because of their frequent in vivo limited bioavailability and off‐target delivery. Herein, an efficient strategy to design vanadium nanodrugs (VNDs) with cancer‐specific theranostic capability for visualizing/treating in vivo mice tumors, is developed. The VNDs are controllably constructed via a non‐covalent coordination triggered self‐assembly strategy, which allows the general synthesis of diverse nanoscale metallodrugs. Significantly, the VNDs exert an approximately tenfold enhancement of therapy efficacy in comparison with vanadium compounds and the clinically used cisplatin due to their improved bioavailability and multiple pathways‐mediated tumor‐selective therapy. Moreover, the VNDs feature intense near‐infrared (NIR) absorption and undergo specific disassembly in the tumor microenvironment, thus enabling tumor‐specific molecular imaging by the turn‐on NIR fluorescence of embedded labels upon disassembly. Hence, the vanadium nanoprodrugs propose a new paradigm for in vivo tumor‐selective therapy and imaging and may propel the design of effective anticancer metallodrugs. [ABSTRACT FROM AUTHOR]