Photodynamic therapy (PDT) is a noninvasive, highly selective method for the treatment of diseases characterized by uncontrolled cell proliferation. It was clinically approved more than 30 years ago. PDT involves the selective uptake of a photosensitizer (PS) by neoplastic tissue, which is able to produce reactive oxygen species (ROS) upon irradiation with visible or near-infrared (NIR) light. ROS induce destruction of target cells and damage of tumor-associated vasculature and activate an antitumor immune response, leading to tumor regression. The execution of this process is attained by different mechanisms, including host immune responses and activation of cell death pathways: apoptosis and necrosis.