Abstract: Positron emission tomography (PET) is the most advanced molecular imaging technology with the advantage of high sensitivity and quantity analysis. Molecule probe is the key factor for PET. ⁸⁹Zr is a novel imaging nuclide and suitable for labeling macromolecular bioactive substances such as antibody due to its favorably long half-life and energy. This review outlined the recent development of the production of ⁸⁹Zr, labeling methods and application of ⁸⁹Zr labelled radiopharmaceuticals.