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类固醇与“避孕药”:先灵葆雅早期的类固醇研究

Steroids and "the pill": early steroid research at Searle.

作者信息

Colton F B

机构信息

G. D. Searle & Co., Chicago, Illinois.

出版信息

Steroids. 1992 Dec;57(12):624-30. doi: 10.1016/0039-128x(92)90015-2.

Abstract

The announcement from the Mayo Clinic in 1949 of the dramatic effectiveness of cortisone in the treatment of rheumatoid arthritis stimulated tremendous interest in steroid chemistry, endocrinology, and related areas of medicine. Shortly thereafter, G. D. Searle & Co. initiated a major effort in steroid research, the objective of which was to discover better steroid drugs than those available at that time or steroids that could be used for conditions for which no compounds were previously available. This effort was remarkably successful and resulted in the introduction of several important pioneering drugs. These included norethandrolone, marketed in 1956 as Nilevar, the first anabolic agent with a favorable separation between protein building and virilization, and spironolactone, introduced in 1959 as Aldactone, the first steroid antialdosterone antihypertensive agent. Of special importance was the research that culminated in the discovery of Enovid. This substance, a combination of the progestin norethynodrel and the estrogen mestranol was first approved in 1957 for the treatment of a variety of disorders associated with the menstrual cycle. The era of oral contraception began in May 1960, when Enovid was approved by the Food and Drug Administration for ovulation inhibition, and was immediately thereafter introduced for such use.

摘要

1949年,梅奥诊所宣布可的松在治疗类风湿性关节炎方面具有显著疗效,这激发了人们对类固醇化学、内分泌学及相关医学领域的极大兴趣。此后不久,G.D.塞尔公司在类固醇研究方面展开了重大努力,其目标是研发出比当时现有药物更好的类固醇药物,或者找到可用于此前尚无化合物可用病症的类固醇。这项努力取得了显著成功,催生了几种重要的开创性药物。其中包括1956年作为尼罗瓦上市的诺乙雄龙,它是第一种在蛋白质合成与男性化作用之间具有良好区分度的合成代谢剂;还有1959年作为安体舒通推出的螺内酯,它是第一种类固醇抗醛固酮类降压药。特别重要的是最终促成发现异炔诺酮的研究。这种物质是炔诺酮和炔雌醇甲醚的组合,1957年首次获批用于治疗与月经周期相关的多种病症。口服避孕药时代始于1960年5月,当时异炔诺酮被美国食品药品监督管理局批准用于抑制排卵,并随即被用于此用途。

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