Chandraratna R A
Allergan, Inc., Irvine CA 92713, USA.
J Am Acad Dermatol. 1997 Aug;37(2 Pt 3):S12-7.
Tazarotene belongs to a novel, nonisomerizable class of retinoic acid receptor (RAR)-specific retinoids, the acetylenic retinoids, and is the first topical retinoid developed for the treatment of psoriasis. Tazarotene targets the keratinocyte and modulates the major causes of psoriasis. Tazarotene is rapidly metabolized by esterase to the active free acid tazarotenic acid, which is rapidly eliminated in animal species. Tazarotene selectively transactivates RAR beta and RAR gamma subtypes and is inactive at retinoid X receptors (RXRs). This receptor selectivity could contribute to an optimized therapeutic index. Tazarotene has low systemic absorption after topical administration. In preclinical toxicity studies, high topical doses produced reversible topical irritation, and lower doses were well tolerated. Topical doses were neither teratogenic nor carcinogenic and were not sensitizing, phototoxic, or photosensitizing. The topical delivery of tazarotene and limited systemic exposure apparently result in a very low potential for systemic effects.
他扎罗汀属于一类新型的、不可异构化的视黄酸受体（RAR）特异性维甲酸，即炔类维甲酸，是首个开发用于治疗银屑病的外用维甲酸。他扎罗汀作用于角质形成细胞，调节银屑病的主要病因。他扎罗汀经酯酶迅速代谢为活性游离酸他扎罗汀酸，在动物物种中迅速消除。他扎罗汀选择性地反式激活RARβ和RARγ亚型，对视黄酸X受体（RXR）无活性。这种受体选择性可能有助于优化治疗指数。局部给药后，他扎罗汀的全身吸收较低。在临床前毒性研究中，高局部剂量产生可逆的局部刺激，较低剂量耐受性良好。局部剂量既无致畸性也无致癌性，且无致敏、光毒性或光敏性。他扎罗汀的局部给药和有限的全身暴露显然导致全身效应的可能性非常低。
