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Photodynamic therapy relies on the action of a photosensitising drug in order to generate reactive oxygen species that cause damage to biological cells and tissues. The key aspects for the success of this therapy are the optical and photosensitising properties of the drug, as well as its pharmacological properties. This chapter provides an overview of the drugs already approved for clinical use for cancer, antimicrobial or other applications, as well as a list of those in clinical trials and at the preclinical stage. Emerging strategies for controlling the production of reactive oxygen species and novel photosensitising modalities brought about by the bio- and nano-revolutions are discussed.

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