Tumour phototherapy involves the preferential destruction of tumour ce
lls by a combination of photosensitizer, light, and oxygen (photodynam
ic therapy). The origins of this topic are considered, as are mechanis
tic aspects. The review then concentrates on current efforts to discov
er photosensitizers which are more potent and more selective than the
first generation materials (Haematoporphyrin Derivative and its commer
cial variants). Design features are summarized, and recent work on sen
sitizers of the porphyrin, chlorin, phthalocyanine, naphthalocyanine,
porphycene, and texaphyrin classes are discussed in relation to our ow
n work on m-THPC (Temoporfin).