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Ziqing Huang,1,2,* Guanhui Chen,3,* Feilong Deng,1,2 Yiming Li1,2 1Hospital of Stomatology, Guanghua School of Stomatology, Sun Yat-sen University, Guangzhou, 510055, People’s Republic of China; 2Guangdong Provincial Key Laboratory of Stomatology, Guangzhou, People’s Republic of China; 3Department of Stomatology, Seventh Affiliated Hospital, Sun Yat-sen University, Shenzhen, 518107, People’s Republic of China*These authors contributed equally to this workCorrespondence: Feilong Deng; Yiming Li, Department of Oral Implantology, Guanghua School of Stomatology, Hospital of Stomatology, Sun Yat-sen University, 56 Ling yuan xi Road, Yuexiu District, Guangzhou 510055, People’s Republic of China, Tel +86 20 8386-3002, Fax +86 20-8382-2807, Email dengfl@mail.sysu.edu.cn; liym228@mail.sysu.edu.cnAbstract: Graphdiyne (GDY) is a 2D carbon allotrope that features a one-atom-thick network of sp- and sp2-hybridized carbon atoms with high degrees of π conjugation. Due to its distinct electronic, chemical, mechanical, and magnetic properties, GDY has attracted great attention and shown great potential in various fields, such as catalysis, energy storage, and the environment. Preparation of GDY with various nanostructures, including 0D quantum dots, 1D nanotubes/nanowires/nanoribbons, 2D nanosheets/nanowalls/ordered stripe arrays, and 3D nanospheres, greatly improves its function and has propelled its applications forward. High biocompatibility and stability make GDY a promising candidate for biomedical applications. This review introduces the latest developments in fabrication of GDY-based nanomaterials with various morphologies and summarizes their propective use in the biomedical domain, specifically focusing on their potential advantages and applications for biosensing, cancer diagnosis and therapy, radiation protection, and tissue engineering.Keywords: graphdiyne, nanotechnology, biomedical applications