Department of Dermatology, Bispebjerg Hospital, Copenhagen, Denmark.
Exp Dermatol. 2010 Aug;19(8):e166-72. doi: 10.1111/j.1600-0625.2009.01035.x.
Hexyl aminolevulinate (HAL) is a long-chained 5-aminolevulinic acid-ester that has been proposed as a novel photosensitizing agent to methyl aminolevulinate (MAL) in topical photodynamic therapy (PDT). The more lipophilic HAL, may improve treatment outcome for non-melanoma skin cancer.
To compare the prophylactic and therapeutic effects of HAL- and MAL-PDT for ultraviolet-induced squamous cell carcinomas (SCCs) in hairless mice.
Mice (n = 249) were irradiated with solar UV-radiation (UVR) until SCC occurred. Before any skin changes developed, two prophylactic PDT treatments were given, using creams of HAL (2%, 6%, 20%) or MAL (20%) followed by illumination (632 nm, Aktilite, Photocure). Two therapeutic PDT-treatments were given by randomization to the first developed SCC of 1 mm. Primary end-points were time to first SCC of 1 mm and complete SCC clearance. Secondary end-points were time to SCC-recurrence, PpIX fluorescence and skin reactions to PDT.
The median time to first SCC was significantly longer for mice treated with prophylactic HAL-PDT (2%, 6% and 20% HAL, 264 days) and MAL-PDT (20% MAL, 269 days) than mice exposed to UVR (186 days) and UVR + placebo-PDT (199 days) (P < 0.0001). The therapeutic efficacy of HAL- and MAL-PDT showed cure rates of 23-61.5% (P = 0.11). Similar PpIX fluorescence intensity and severity of clinical reactions were seen for HAL- and MAL-groups, although mice developed more intense hyper-pigmentation when treated with 20% MAL-PDT compared with 2% HAL-PDT.
PDT with HAL (2%, 6% and 20%) and MAL (20%) is equally effective to prevent and treat UV-induced SCC in hairless mice.
己基氨基酮酸（HAL）是一种长链 5-氨基酮戊酸酯，已被提议作为一种新型光敏剂，用于局部光动力疗法（PDT）中的甲基氨基酮戊酸（MAL）。更亲脂性的 HAL 可能会改善非黑素瘤皮肤癌的治疗效果。
比较 HAL 和 MAL-PDT 对无毛小鼠紫外线诱导的鳞状细胞癌（SCC）的预防和治疗效果。
将 249 只小鼠用太阳紫外线（UVR）照射，直至发生 SCC。在任何皮肤变化发生之前，用 HAL（2%、6%、20%）或 MAL（20%）乳膏进行两次预防性 PDT 治疗，然后进行光照（632nm，Aktilite，Photocure）。通过随机分配，对第一个 1mm 大小的 SCC 进行两次治疗性 PDT 治疗。主要终点是首次 SCC 为 1mm 的时间和 SCC 完全清除的时间。次要终点是 SCC 复发时间、PpIX 荧光和 PDT 皮肤反应。
与暴露于 UVR（186 天）和 UVR+安慰剂-PDT（199 天）的小鼠相比，用预防性 HAL-PDT（2%、6%和 20%HAL）和 MAL-PDT（20%MAL）治疗的小鼠首次 SCC 的中位时间明显更长（264 天）（P<0.0001）。HAL-和 MAL-PDT 的治疗效果显示治愈率为 23-61.5%（P=0.11）。尽管用 20%MAL-PDT 治疗的小鼠比用 2%HAL-PDT 治疗的小鼠出现更强烈的色素沉着过度，但 HAL-和 MAL-组的 PpIX 荧光强度和临床反应严重程度相似。
HAL（2%、6%和 20%）和 MAL（20%）的 PDT 对预防和治疗无毛小鼠的 UVR 诱导 SCC 同样有效。
