In this study, we utilized Ac‐Gly‐BoroPro, a highly selective FAP inhibitor with a selectivity ninefold greater for FAP than for its homolog DppIV.[45] Systemically administering Ac‐Gly‐BoroPro in mice significantly increased the trabecular bone volume and density at the metaphysis of the femur in a dose‐dependent manner without observable side effects.[8] Furthermore, we successfully alleviated inflammation and alveolar bone resorption in the mouse model of periodontitis through localized injections of Ac‐Gly‐BoroPro into the periodontal tissues. The gene discussed is DPP4; the disease is periodontitis.