The development of therapies which are selective for tumor tissues is one o
f the most important goals in anticancer research. Within this framework ph
otochemotherapy can be considered a very promising approach. Its therapeuti
c effectiveness depends on two connected factors: drug and light. The drug
(photosensitizer) is able to exert an antiproliferative effect only after i
nteraction with suitable light. Both the photosensitizing drug and light al
one are ineffective at doses used for these treatments. Nowadays, photochem
otherapy is used in the treatment of cutaneous T-cell lymphoma and cavitary
tumors. In the first case the photosensitizer is a psoralen derivative (P)
and long-wavelength ultraviolet radiation (UVA) is used (PUVA therapy). In
the second case, the treatment with porphyrins, porphyrin-based and non po
rphyrin-based photosensitizers is followed by irradiation with 600-1000 nm
light (photodynamic therapy, PDT). This review is concerned with PUVA and P
DT treatments of cancer, The molecular mechanisms considered accountable fo
r the photochemotherapeutic effects are discussed, the development of new c
hemical structures aimed at improving the effectiveness and/or overcoming s
ome undesired side effects will also be reported. Moreover, some clinical a
pplications will be described.