Water-insoluble fullerene (C-60) was chemically modified with poly(eth
ylene glycol) (PEG) to solubilize it in water. The C-60-PEG conjugates
, upon injecting intravenously, were accumulated in the tumor to a gre
ater extent than in the normal tissue and exhibited prolonged C-60 ret
ention at the tumor tissue. Conjugate injection followed by light irra
diation significantly suppressed the volume increase of tumor. We conc
lude that the PEG-modified C-60 has a high potentiality as a drug of p
hotodynamic tumor therapy.