Photodynamic therapy (PDT) is a therapeutic modality that uses light to treat malignant or benign diseases. A photosensitizer, light, and oxygen are the three main components needed to generate a cytotoxic effect. Pyrrole-based photosensitizers have been widely used for PDT. Many of the photosensitizers within this class are macrocyclic. This is particularly true for systems that have received regulatory approval or been the subject of clinical trials. However, in recent years, a number of boron dipyrromethanes (BODIPY) have been studied as photosensitizers. Herein, we review examples of some of the most relevant pyrrole-based photosensitizers.