Abstract: Positron-emitting radionuclide ⁸⁹Zr is just emerging in recent years. It has a half-life of 78.4 h, and is especially suitable for labelling antibodies, or nanoparticles, and other carriers of long time observation. ⁸⁹Zr is cheap to produce, stable in vivo, and residualizes in tumors, and importantly has high resolution of PET images, therefore it will have wide application prospect in the field of PET imaging. This paper provides a comprehensive research progress of ⁸⁹Zr medicinal chemistry and in vivo biological behavior evaluation, including the production and purification of ⁸⁹Zr, the solution coordination chemistry of ⁸⁹Zr, new bioconjugation strategies, the preclinical imaging studies of ⁸⁹Zr based agents, and the clinical applications of ⁸⁹Zr labeled radiopharmaceuticals.