Scott L J, Goa K L
Adis International Limited, Mairangi Bay, Auckland, New Zealand.
Drugs Aging. 2000 Feb;16(2):139-46; discussion 147-8. doi: 10.2165/00002512-200016020-00005.
Verteporfin, a benzoporphyrin derivative monoacid ring A, is a photosensitising drug for photodynamic therapy (PDT) activated by low-intensity, nonheat-generating light of 689nm wavelength. Activation generates cytotoxic oxygen free radicals. The specificity and uptake of verteporfin for target cells with a high expression of low density lipoprotein (LDL) receptors, such as tumour and neovascular endothelial cells, is enhanced by the use of a liposomal formulation and its rapid uptake by plasma LDL. Verteporfin therapy (at light doses < 150 J/cm) selectively damages neovascular endothelial cells leading to thrombus formation and specific occlusion of choroidal neovascular vessels in subfoveal lesions in patients with age-related macular degeneration (AMD). Repeated applications of verteporfin therapy 6 mg/m2 improved or maintained visual acuity in the majority of patients with some classic subfoveal choroidal neovascularisation (CNV) secondary to AMD at 1 year's follow-up in 2 large multicentre, placebo-controlled, double-blind trials. Furthermore. in a subgroup of these patients with predominantly classic CNV secondary to AMD, there was a significantly more marked visual acuity (VA) benefit with 67.3% of verteporfin-treated eyes experiencing less than a 15-letter loss of VA versus 39.3% with placebo treatment. Multiple applications of verteporfin therapy were well tolerated in patients with subfoveal CNV secondary to AMD. The most common adverse events were visual disturbances, injection site reactions, photosensitivity reactions and infusion-related back pain.
维替泊芬是一种苯并卟啉衍生物单酸环A,是一种用于光动力疗法(PDT)的光敏药物,由波长689nm的低强度、不产生热量的光激活。激活会产生细胞毒性氧自由基。通过使用脂质体制剂以及其被血浆低密度脂蛋白(LDL)快速摄取,维替泊芬对低密度脂蛋白(LDL)受体高表达的靶细胞(如肿瘤和新生血管内皮细胞)的特异性和摄取得以增强。维替泊芬治疗(光剂量<150 J/cm²)可选择性损伤新生血管内皮细胞,导致血栓形成,并特异性阻塞年龄相关性黄斑变性(AMD)患者黄斑下病变中的脉络膜新生血管。在两项大型多中心、安慰剂对照、双盲试验中,对继发于AMD的一些典型黄斑下脉络膜新生血管(CNV)患者进行1年随访时,重复应用6 mg/m²的维替泊芬治疗可使大多数患者的视力得到改善或维持。此外,在这些主要继发于AMD的典型CNV患者亚组中,维替泊芬治疗组有更显著的视力(VA)获益,67.3%接受维替泊芬治疗的眼睛VA下降少于15个字母,而安慰剂治疗组为39.3%。继发于AMD的黄斑下CNV患者对多次维替泊芬治疗耐受性良好。最常见的不良事件是视觉障碍、注射部位反应、光敏反应和输液相关的背痛。