Abstract: Photodynamic therapy has been widely used in the treatment of tumors and has broad application prospect. Recent studies have shown that padeliporfin, a water-soluble vascular-targeting photosensitizer can selectively accumulate in tumor cells after intravenous administration and release a large amount of reactive oxygen species upon photoactivation, thereby exerting anti-tumor effect. This drug has been approved in Europe as a treatment for prostate cancer. This review mainly introduced the discovery process, synthetic route, pharmacological action and clinical research progress of padeliporfin, so as to provide reference for further exploration of tumor photodynamic therapy.