Young S W, Woodburn K W, Wright M, Mody T D, Fan Q, Sessler J L, Dow W C, Miller R A
Pharmacyclics, Inc., Sunnyvale, CA 94086, USA.
Photochem Photobiol. 1996 Jun;63(6):892-7. doi: 10.1111/j.1751-1097.1996.tb09647.x.
Lutetium texaphyrin, PCI-0123, is a pure, water-soluble photosensitizer with a large broad absorption band centered at 732 nm. The compound was tested for photodynamic therapy (PDT) effectiveness in a murine mammary cancer model. The texaphyrin macrocycle as illustrated by magnetic resonance imaging and 14C-radiolabeled texaphyrin studies was shown to be tumor selective; a tumor-to-muscle ratio of 10.55 was seen after 5 h. Lutetium texaphyrin, at a drug dose of 20 mumol/kg with irradiation 5 h postinjection at 150 J/cm2 and 150 mW/cm2, had significant efficacy (P < 0.0001) in treating neoplasms of moderate size (40 +/- 14 mm3) and also had significant efficacy (P < 0.0001) in treating larger neoplasms (147 +/- 68 mm3). The PDT efficacy was correlated with the time interval between PCI-0123 administration and light exposure. A 100% cure rate was achieved when photoirradiation took place 3 h postinjection compared to 50% for 5 h using 10 mumol/kg and 150 J/cm2 at 150 mW/cm2. The PDT efficacy was attributable to the selective uptake/retention of the texaphyrin photosensitizer in addition to the depth of light penetration achievable at the 732 nm laser irradiation.
镥系卟啉（PCI-0123）是一种纯净的水溶性光敏剂，具有以732nm为中心的宽吸收带。该化合物在小鼠乳腺癌模型中进行了光动力疗法（PDT）有效性测试。磁共振成像和14C放射性标记的镥系卟啉研究表明，卟啉大环具有肿瘤选择性；5小时后肿瘤与肌肉的比率为10.55。镥系卟啉在药物剂量为20μmol/kg、注射后5小时以150J/cm2和150mW/cm2进行照射时，对中等大小（40±14mm3）的肿瘤具有显著疗效（P<0.0001），对较大肿瘤（147±68mm3）也具有显著疗效（P<0.0001）。PDT疗效与PCI-0123给药和光照之间的时间间隔相关。注射后3小时进行光照射时治愈率达到100%，而在10μmol/kg、150J/cm2和150mW/cm2条件下，注射后5小时进行光照射时治愈率为50%。PDT疗效除了归因于732nm激光照射可达到的光穿透深度外，还归因于卟啉光敏剂的选择性摄取/保留。
