“五规则”(Rule of five)的提出为小分子药物设计的提供了有效的指导,但时至今日亦有不少上市的药物打破了“五规则”。今天分享一篇来自欧美多国学者联合发表在Drug Discov Today上的文章,题为“Trends in oral small-molecule drug discovery and product develop...
Drugdiscoverybeyondthe‘rule-of-five’——优于“rule-of-five”的药物发现 •生物系：宋彩霞 摘要：•“Rule-of-five”规则是小分子药物设计的有效指导原则，但是在某种程度上被过分强调。“Ruleof-five”规则是针对口服药物总结出的经验性规律，所以存在着一些局限性。本文在此讨论了优于“rule-of-five”...
系统标签: 药物 rule 优于 discovery drug 发现 生物系:宋彩霞„„‟‟———优于优于““rulerule--ofof--fivefive””的药物发的药物发现现••••••••““””•••••”过分地强调过分地强调““rulerule--ofof--fivefive””规则及规则及口服生口服生物利用度物利用...
生物系:宋彩霞„„‟‟———优于优于““rulerule--ofof--fivefive””的药物发的药物发现现1•“Rule-of-five”规则是小分子药物设计的有效指导原则,但是在某种程度上被过分强调。“Rule-of-five”规则是针对口服药物总结出的经验性规律,所以存在着一些局限性。本文在此讨论了优于“rule-of-five...
Synthetic biology for natural product drug discovery(用于天然药物发现的合成生物学) conc| USIOnS(结论) Introduction(引言) 岷Rule-of-ffive”规则,也称为 Lipinski定性规 则,主要用于检验药物的口服生物利用度。 内容 个药物分子中①氢键供体数大于5,②分 ...
Drug discov bond the u 优 1eve的药物发现生物系:宋彩霞 摘要: Rule-of-ffive规则是小分子药物设计的有戏指导原则,但是在某种程度上被过分强调 R 们v规则是针对口服药物总结出的经验性规律, 所以存在着一些局限性。本文在此讨论了优于“ rule-o霄ve罗规则的药物发现的方法:如积极主动地发展与口服药品平行的...
Approximately 6% of orally administered drugs have physicochemical properties that are beyond Lipinski's rule of five (bRo5). However, in the past five years, there have been 22 new oral bRo5 drugs approved by the FDA, which account for 21% of new oral drug approvals. The significant ...
Lipinski's rule of 5 Rule of 5 Rule of fiveLipinski's rule of five is a concept frequently used in drug discovery. This rule helps to predict if a biologically active molecule is likely to have the chemical and physical properties to be orally bioavailable. The Lipinski rule bases pharmacoki...
当然也有个例,如果化合物具有特异性的吸收通道,或者抗菌药,抗生素,维生素,强心配糖体等不适用于Rule of five。同时有个别口服医药品也并不遵循Rule of five。 参考文献 (a) “Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings” Lipinski...