Bollag W
J Am Acad Dermatol. 1983 Nov;9(5):797-805. doi: 10.1016/s0190-9622(83)80143-1.
The retinoids are a class of compounds consisting of vitamin A and its natural and synthetic analogues. Vitamin A has a marked influence on the differentiation of epithelial tissues, such as skin and mucous membranes. Vitamin A deficiency leads to hyperkeratosis of the skin and squamous metaplasia of mucous membranes, histologic features common to various dermatologic and precancerous diseases. The beneficial effect of vitamin A in these diseases was, however, unsatisfactory. Therefore, a retinoid program was set up in order to find new synthetic retinoids with the highest possible therapeutic activity and the least possible side effects. It was discovered that the chemically induced skin papilloma of the mouse responded to retinoids with a marked regression. This therapeutic activity in combination with the determination of a therapeutic index (relation between therapeutic action and hypervitaminosis A syndrome) served as criteria in choosing retinoids for clinical trials in dermatologic and oncologic diseases. Until now three particular compounds have achieved remarkable usefulness in dermatology: 13-cis-retinoic acid (isotretinoin; Accutane) in the treatment of cystic acne, the aromatic retinoid etretinate in the therapy of severe forms of psoriasis, and an arotinoid. Much less spectacular success has been achieved with these compounds in the prevention and therapy of premalignant and malignant diseases. It is hoped that newer retinoids with a still better therapeutic index or a more selective therapeutic activity will further enrich our therapeutic armamentarium in the fields of dermatology, oncology, and other disciplines of medicine.
类视黄醇是一类由维生素A及其天然和合成类似物组成的化合物。维生素A对上皮组织（如皮肤和黏膜）的分化有显著影响。维生素A缺乏会导致皮肤角化过度和黏膜鳞状化生，这些是各种皮肤病和癌前疾病常见的组织学特征。然而，维生素A在这些疾病中的有益效果并不理想。因此，开展了一项类视黄醇研究计划，以寻找具有尽可能高的治疗活性和尽可能少的副作用的新型合成类视黄醇。人们发现，化学诱导的小鼠皮肤乳头瘤对类视黄醇有明显的消退反应。这种治疗活性与治疗指数（治疗作用与维生素A过多综合征之间的关系）的确定一起，作为选择用于皮肤病和肿瘤疾病临床试验的类视黄醇的标准。到目前为止，有三种特定的化合物在皮肤科取得了显著成效：13 - 顺式维甲酸（异维甲酸；泰尔丝）用于治疗囊肿性痤疮，芳香族类视黄醇阿维A酯用于治疗严重形式的银屑病，以及一种芳香维甲酸。这些化合物在癌前和恶性疾病的预防和治疗方面取得的成功则要小得多。人们希望具有更好治疗指数或更具选择性治疗活性的新型类视黄醇将进一步丰富我们在皮肤科、肿瘤学和其他医学学科领域的治疗手段。
