In photochemotherapy, as exemplified by the photodynamic therapy of tumors, a photosensitizing drug is administered to the patient; then, after a period of time to permit the most effective anatomical distribution of the drug, the diseased area is illuminated using an appropriate source of light of wavelengths absorbed by the sensitizer. In the tumor case, this results in the photochemical alteration of critical kinds of biornolecules in the diseased tissue, which interferes with the normal activities of certain cell organelles. This, in turn, leads to the injury or death of diseased cells in the treated area. This paper briefly reviews the reactive chemical species that can be formed in biological systems by illuminated sensitizers (triplet states of sensitizer molecules, free radicals of sensitizers and cellular components, singlet oxygen, superoxide, hydrogen peroxide, hydroxyl radical) and the kinds of biochemical changes they produce in essential cellular molecules (nucleic acids, proteins, unsaturated lipids, etc.). Also reviewed are the effects of these molecular changes on the structure and function of mammalian cell organelles (membranes, mitochondria, nuclear components, etc.) and the mechanisms of the resulting injury or killing of the cells.