Photodynamic therapy (PDT), defined as ''the light-induced inactivation of cells, microorganisms, or molecules,'' combines the use of a photosensitive agent or photosensitizer (PS) activated by irradiation with a light source to produce reactive oxygen species and highly reactive singlet oxygen. PDT has been used for the treatment of different oral diseases with promising results. This review describes the basic principles of PDT, including the nature of PS and the light sources, and focuses on evaluating the efficacy of this method, according to the existing data, for the treatment of different oral diseases. PubMed was used as the source of the relevant literature, about the clinical application of PDT in actinic cheilitis (AC), leukoplakia, oral lichen planus, oral lichenoid lesions, and oral cancer. Complete response to PDT as high as 100% has been reported not only in cases of AC but also in dysplasias/carcinomas in situ, T1N0, and T2N0. According to the available data, PDT appears to be a safe, well-tolerated therapy with limited adverse effects and excellent cosmetic outcome. Although PDT is a very promising therapy, further research is needed in order to investigate the cases that fail to respond, to examine the long-term prognosis for cases of reported complete response and thus avoid the future recurrence of diseases.