De Camp W H
Division of Anti-Infective Drug Products, Food and Drug Administration, Rockville, Maryland 20857.
Chirality. 1989;1(1):2-6. doi: 10.1002/chir.530010103.
The current regulatory position of the Food and Drug Administration is discussed with regard to the approval of racemates and pure stereoisomers. Circumstances in which stereochemically sensitive analytical methods are necessary to ensure the safety and efficacy of a drug are described. Regulatory guidelines are interpreted for applications for the approval of a pure enantiomer in which the racemate is marketed, for the approval of either a racemate or a pure enantiomer in which neither is marketed, and for clinical investigations to compare the safety and efficacy of a racemate and its enantiomers. Examples of the basis for such regulation are drawn from historical situations (thalidomide, benoxaprofen) as well as currently marketed drugs (arylpropionic acids, disopyramide, indacrinone).
讨论了美国食品药品监督管理局（FDA）目前在消旋体和纯立体异构体批准方面的监管立场。描述了需要立体化学敏感分析方法以确保药物安全性和有效性的情况。对以下几种申请的监管指南进行了解读：已上市消旋体情况下纯对映体的批准申请；消旋体和纯对映体均未上市时消旋体或纯对映体的批准申请；以及比较消旋体及其对映体安全性和有效性的临床研究。此类监管依据的例子取自历史案例（沙利度胺、苯恶洛芬）以及目前上市的药物（芳基丙酸类、丙吡胺、茚达立酮）。
