The main steps of development of fluorescence diagnosis and photodynamic therapy were overviewed. Brief historical data were presented about Photohem, Photosens, Alasens, Radachlorin, and Photoditazine photosensitizers, along with their corresponding pharmacokinetic properties, mechanisms of action, and specific features of use. Key aspects of development of fluorescence diagnosis and photodynamic therapy in Gertsen Moscow Research Oncological Institute were described. The main indications for photodynamic therapy and its efficiency in patients with oral, tongue, stomach, esophageal, skin, cervical, and central lung cancer and vulval lesions were demonstrated. It was shown that photodynamic therapy is effective for adjuvant or intraoperative treatment in patients with high risk of local recurrence after surgical treatment, and palliative photodynamic therapy increases the quality of life and survival rates in the most challenging group of cancer patients. The results of photodynamic therapy for cervical pre-cancer and cancer associated with human papillomavirus were reported. The main trends of intraoperative "fluorescence guidance" with Alasens were covered. Clinical experience allows rating photodynamic therapy among the most encouraging methods for the current medicine.