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镥特沙卟啉(Lu-Tex):一种用于眼底血管造影和光动力疗法的潜在新型药物。

Lutetium texaphyrin (Lu-Tex): a potential new agent for ocular fundus angiography and photodynamic therapy.

作者信息

Blumenkranz M S, Woodburn K W, Qing F, Verdooner S, Kessel D, Miller R

机构信息

Pharmacyclics Inc, Sunnyvale, CA, USA.

出版信息

Am J Ophthalmol. 2000 Mar;129(3):353-62. doi: 10.1016/s0002-9394(99)00462-6.

DOI:10.1016/s0002-9394(99)00462-6
PMID:10704552
Abstract

PURPOSE

To investigate the suitability of lutetium texaphyrin (lu-tex) as a fluorescence imaging agent in the delineation of retinal vascular and choroidal vascular diseases. The utilization of an efficient fluorescent molecule that is also a photosensitizer represents a unique opportunity to couple diagnosis and therapy.

METHODS

Fundus fluorescence angiography comparing lu-tex (motexafin lutetium, Optrin, Pharmacyclics Inc, Sunnyvale, California) with the conventional angiographic dyes, sodium fluorescein, and indocynanine green (ICG), was performed on the eyes of normal and laser-injured New Zealand white rabbits. Plasma pharmacokinetic data and plasma protein binding were assessed in addition to light microscopy of the retina in both imaged and laser-injured eyes.

RESULTS

Normal retinal and choroidal vasculature was well delineated by lu-tex angiography. Experimentally induced choroidal and retinal vascular lesions were enhanced by lu-tex and demonstrated different staining patterns than fluorescein or ICG, particularly at the margins of the lesions. Lu-tex cleared rapidly from the plasma, with 39.7% bound to the high-density lipoprotein (HDL) fraction while 15.8% was bound to the low-density lipoprotein (LDL) fraction. No evidence of retinal toxicity after dye administration was observed by either ophthalmoscopy and fundus photography or by light microscopy.

CONCLUSION

Lu-tex angiography is a potentially valuable method for retinal vascular and choroidal vascular evaluation, and it has advantages over fluorescein and ICG angiography. The same agent could conceivably be used for both the identification of abnormal vasculature and subsequent photodynamic treatment.

摘要

目的

研究镥系卟啉(lu-tex)作为荧光成像剂在视网膜血管和脉络膜血管疾病诊断中的适用性。利用一种高效的荧光分子同时也是一种光敏剂,为联合诊断和治疗提供了独特的机会。

方法

在正常和激光损伤的新西兰白兔眼中,进行眼底荧光血管造影,将lu-tex(莫替沙芬镥,Optrin,Pharmacyclics公司,加利福尼亚州桑尼维尔)与传统血管造影染料荧光素钠和吲哚菁绿(ICG)进行比较。除了对成像和激光损伤眼睛的视网膜进行光学显微镜检查外,还评估了血浆药代动力学数据和血浆蛋白结合情况。

结果

lu-tex血管造影能很好地显示正常视网膜和脉络膜血管系统。实验诱导的脉络膜和视网膜血管病变在lu-tex造影下增强,且显示出与荧光素或ICG不同的染色模式,尤其是在病变边缘。lu-tex从血浆中快速清除,39.7%与高密度脂蛋白(HDL)部分结合,15.8%与低密度脂蛋白(LDL)部分结合。通过检眼镜检查、眼底摄影或光学显微镜检查,均未观察到染料给药后视网膜毒性的证据。

结论

lu-tex血管造影是一种潜在有价值的视网膜血管和脉络膜血管评估方法,优于荧光素和ICG血管造影。同一试剂可设想用于识别异常血管并随后进行光动力治疗。

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