Bernard B A
Centre International de Recherches Dermatologiques, GALDERMA, Sophia Antipolis, France.
Skin Pharmacol. 1993;6 Suppl 1:61-9. doi: 10.1159/000211165.
Adapalene is a novel chemical entity which, in terms of pharmacology, behaves similar to tretinoin, but is chemically and photochemically stable. It has a particular selectivity profile for the known nuclear retinoic acid receptors with low affinity for RAR alpha and no transactivating potential for RXR alpha. This receptor profile could imply that adapalene, in contrast to tretinoin, affects the terminal differentiation pathway of epidermal cells rather than their proliferation. Furthermore, adapalene does not bind to members of the cellular retinoic acid binding protein family. Adapalene has comedolytic activity in the topical rhino mouse model. It exerts a moderate-to-potent anti-inflammatory effect in a series of in vitro and in vivo models. In comparative clinical studies involving 72 acne patients, the efficacy of adapalene was comparable, if not superior, to tretinoin, but adapalene was better tolerated. The data reviewed in this paper indicate that adapalene should be particularly beneficial in the treatment of acne.
阿达帕林是一种新型化学实体，在药理学方面，其作用与维甲酸相似，但在化学和光化学性质上较为稳定。它对已知的核维甲酸受体具有特定的选择性，对RARα亲和力低，对RXRα无反式激活潜能。这种受体特性可能意味着，与维甲酸不同，阿达帕林影响表皮细胞的终末分化途径而非其增殖。此外，阿达帕林不与细胞维甲酸结合蛋白家族成员结合。在局部应用的犀牛小鼠模型中，阿达帕林具有抗粉刺活性。在一系列体外和体内模型中，它发挥中度至强效的抗炎作用。在涉及72名痤疮患者的比较临床研究中，阿达帕林的疗效即便不优于维甲酸，至少也与之相当，但阿达帕林的耐受性更好。本文综述的数据表明，阿达帕林在痤疮治疗中应具有特别的益处。
