要 旨 光線力学療法 (Photodynamic therapy ; PDT) の抗腫瘍効果は,光感受性物質の腫瘍細胞選択性や腫瘍細胞内での活性 酸素誘導能,光線照射の照射効率などが重要な因子となる.本邦ではこれまで第一世代の Porfimer sodium と第二世代 の Talaporfin sodium が保険で認可され,その適応癌種も近年増えつつある.また研究レベルでは第三世代の光感受性 物質の開発も進んでおり,より低侵襲で切れ味の鋭い PDT の開発が期待される.光感受性物質の特性と今後の開発研 究につき解説する. キーワード:光線力学療法,光線力学診断法,Porfimer sodium, Talaporfin sodium, 5-アミノレブリン酸,Warburg 効果 Abstract Antitumor effects of photodynamic therapy (PDT) depend on the tumor selectivity of photosensitizers, inducibility of reactive oxygen species and radiation efficiency. In Japan, the first generation Porfimer sodium and the second generation Talaporfin sodium have been authorized by insurance and recently, the authorized cancer types targeted by PDT are increasing. In the laboratory, the study of the third generation photosensitizers advances and the development of more effective and lower invasiveness photosensitizers is expected. We summarized the characteristics and future prospects of development research of photosensitizers for PDT.Key words:photodynamic therapy (PDT), photodynamic diagnosis (PDD), porfimer sodium, talaporfin sodium, 5-aminolevulinic acid; 5-ALA, warburg effect 〒 467−8601 愛知県名古屋市瑞穂区瑞穂町字川澄 1 (1 Kawasumi, Mizuho-cho,