种族性药物不一定比它们的单个反原体成分更低效和更安全
Israel Agranat1, Ilaria D'Acquarica2
1Organic Chemistry, Institute of Chemistry, The Hebrew University of Jerusalem, Edmond J. Safra Campus, Jerusalem 9190401, Israel.
概括
基隆药物开发应该优先考虑赛马体,除非单个反体显示出明显的优势. 最近支持单个反体而不是种族体的说法受到质疑,主张逐案评估.
科学领域:
- 药用化学 医学化学
- 药理学 药理学 是一个学科.
- 药物开发 药物开发
背景情况:
- 奇拉类药物存在一个发展困境:种族化合物与单个反体.
- 最近的出版物 (2024) 声称单个反体提供优越的临床效力,疗效和安全性,与racemates相比.
- 这些说法需要对当前的合药物开发策略进行批判性重新评估.
研究的目的:
- 为了反驳最近的指控,青单反体药物而不是种族药物.
- 提供关于单反体药物的发展的历史视角.
- 分析种族化合物或二聚体混合物比单个反体更受欢迎的情况.
主要方法:
- 单反体药物开发的动机的历史调查.
- 对种族化合物/二聚体混合物偏好于单个反体的案例研究分析.
- 检查从奇拉切换中"教导"的情况 (例如,体内互转换,反化).
主要成果:
- 拉塞马特/二聚合物混合物药物本质上并非比单个反聚合物成分更低效或更安全.
- 存在一些特殊的情景,在这些情景中,人们更喜欢racemates,包括快速的体内相互转换或反化.
- 详细介绍了racemic和单反体药物的优缺点.
结论:
- 拉塞马特/二聚合物混合物药物仍然是手性开关的可行候选者.
- 奇拉药物的开发应该默认地继续使用racemate.
- 只有在确定了相关的,差异化的性质时,才应该追求单个反体.
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