评估美国食品药品监督管理局批准的口服药物的理化性质。

IF 6 2区 医学 Q1 PHARMACOLOGY & PHARMACY Expert Opinion on Drug Discovery Pub Date : 2024-02-01 DOI:10.1080/17460441.2023.2275617
Tanner C Reese, Anvita Devineni, Tristan Smith, Ismail Lalami, Jung-Mo Ahn, Ganesh V Raj
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引用次数: 0

摘要

引言:从1990年到1993年,对美国食品药品监督管理局批准的口服药物进行分析,可以确定一组被称为利平斯基五条规则(Ro5)的理化性质。原始Ro5和扩展版本仍然是药物开发计划的参考标准。由于许多生物活性化合物不符合Ro5,我们在美国食品药品监督管理局批准的当代药物队列中验证了这些规则集的相关性和遵守性。涵盖的领域:作者指出,2011年至2022年,美国食品药品监督管理局批准的口服母体化合物中有很大一部分偏离了原始Ro5标准(约38%)或Ro5扩展标准(约53%)。然后,他们评估了是否可以制定当代Ro5标准(cRo5)来更好地预测口服生物利用度。此外,他们讨论了许多案例研究,这些研究表明了增加某些化合物的大小的必要性和益处,并涵盖了提高口服生物利用度的几种不断发展的策略。专家意见:尽管对Ro5进行了多次修订,但作者发现,没有一个单一的物理化学规则与绝对口服生物利用度具有普遍一致性。药物递送和配方的创新极大地扩大了口服给药的理化性质和化学多样性范围。
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Evaluating physiochemical properties of FDA-approved orally administered drugs.

Introduction: Analyses of orally administered FDA-approved drugs from 1990 to 1993 enabled the identification of a set of physiochemical properties known as Lipinski's Rule of Five (Ro5). The original Ro5 and extended versions still remain the reference criteria for drug development programs. Since many bioactive compounds do not conform to the Ro5, we validated the relevance of and adherence to these rulesets in a contemporary cohort of FDA-approved drugs.

Areas covered: The authors noted that a significant proportion of FDA-approved orally administered parent compounds from 2011 to 2022 deviate from the original Ro5 criteria (~38%) or the Ro5 with extensions (~53%). They then evaluated if a contemporary Ro5 criteria (cRo5) could be devised to better predict oral bioavailability. Furthermore, they discuss many case studies showcasing the need for and benefit of increasing the size of certain compounds and cover several evolving strategies for improving oral bioavailability.

Expert opinion: Despite many revisions to the Ro5, the authors find that no single proposed physiochemical rule has universal concordance with absolute oral bioavailability. Innovations in drug delivery and formulation have dramatically expanded the range of physicochemical properties and the chemical diversity for oral administration.

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来源期刊
CiteScore
10.20
自引率
1.60%
发文量
78
审稿时长
6-12 weeks
期刊介绍: Expert Opinion on Drug Discovery (ISSN 1746-0441 [print], 1746-045X [electronic]) is a MEDLINE-indexed, peer-reviewed, international journal publishing review articles on novel technologies involved in the drug discovery process, leading to new leads and reduced attrition rates. Each article is structured to incorporate the author’s own expert opinion on the scope for future development. The Editors welcome: Reviews covering chemoinformatics; bioinformatics; assay development; novel screening technologies; in vitro/in vivo models; structure-based drug design; systems biology Drug Case Histories examining the steps involved in the preclinical and clinical development of a particular drug The audience consists of scientists and managers in the healthcare and pharmaceutical industry, academic pharmaceutical scientists and other closely related professionals looking to enhance the success of their drug candidates through optimisation at the preclinical level.
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