Photodynamic Therapy (PDT) is a minimally invasive treatment that has shown promising results in treating preneoplasticlesions. PDT reckons on the administration of a drug (photosensitizer), which can be used in a topical or systemic form. Photodynamic therapy has been successfully used in the management of a variety of pathologies from different anatomical sites, including the head, neck, brain and lungs, hepatobiliary tree and other gastrointestinal and urological pathologies, skin, gynaecological conditions and in vascular anomalies. Starting from these same considerations, PDT has also been adopted for oral malignant and premalignant lesions treatment, and should be kept under investigation as a promising therapeutic management of leukoplakia and preneoplastic lesions of the oral cavity.