Screening for human ADME/Tox drug properties in drug discovery.

Li AP

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Screening for human ADME/Tox drug properties in drug discovery.

机译：筛选药物发现中的人类Adme / Tox药物性质。

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There is no doubt that ADME/Tox drug properties, absorption, distribution, metabolism, elimination and toxicity, are properties crucial to the final clinical success of a drug candidate. It has been estimated that nearly 50% of drugs fail because of unacceptable efficacy, which includes poor bioavailability as a result of ineffective intestinal absorption and undesirable metabolic stability(1). It has also been estimated that up to 40% of drug candidates have failed in the past because of safety issues(2). In this review, the methodologies that are available for use in drug development as in vitro human-based screens for ADME/Tox drug properties are discussed.

机译：毫无疑问，Adme / Tox药物性质，吸收，分布，代谢，消除和毒性是对药物候选者的最终临床成功至关重要的性质。据估计，由于不可接受的功效，近50％的药物失效，这包括由于肠道吸收和不希望的代谢稳定性而导致的生物利用度差（1）。据估计，由于安全问题（2），过去的毒品候选人高达40％的候选人失败了。在本文中，讨论了作为ADME / TOX药物性质的体外人基筛选可用于药物开发的方法。

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《Drug discovery today》 |2001年第7期|共10页
作者
Li AP;
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In Vitro Technologies 1450 S. Rolling Rd 21227 Baltimore MD USA;

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原文格式 PDF
正文语种 eng
中图分类药学;
关键词
Human; Pharmaceutical Preparations;

机译：人类;药品制剂;

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专利

1. Screening for human ADME/Tox drug properties in drug discovery. [J] . Li AP Drug discovery today . 2001,第7期

机译：筛选药物发现中的人类Adme / Tox药物性质。
2. ADME Evaluation in Drug Discovery. 9. Prediction of Oral Bioavailability in Humans Based on Molecular Properties and Structural Fingerprints. [J] . Tian S, Li Y, Wang J, Molecular pharmaceutics . 2011,第3期

机译：药物发现中的ADME评估。 9.基于分子特性和结构指纹图谱预测人类口服生物利用度。
3. ADME evaluation in drug discovery. 6. Can oral bioavailability in humans be effectively predicted by simple molecular property-based rules? [J] . Hou TJ, Wang JM, Zhang W, Journal of chemical information and modeling . 2007,第2期

机译：药物发现中的ADME评估。 6.是否可以通过基于简单分子特性的规则有效预测人类的口服生物利用度？
4. ADME Evaluation in Drug Discovery. 5. Correlation of Caco-2 Permeation with Simple Molecular Properties [C] . T. J. Hou, W. Zhang, K. Xia, Collection of Academic Papers(2004) . -1

机译：药物发现中的ADME评估。 5. Caco-2渗透与简单分子性质的相关性
5. Modulation of the redox status of isolated mitochondria by energy-linked substrates: Quantification by high performance liquid chromatography and "Splicing up" Drug discovery. Cell-based expression and screening of genetically-encoded libraries of backbone cyclized polypeptides. [D] . Sancheti, Harshkumar. 2010

机译：通过能量连接的底物调节分离的线粒体的氧化还原状态：通过高效液相色谱法和“拼接”药物发现进行定量。基于细胞的骨架骨架多肽的遗传编码文库的表达和筛选。
6. Virtual screening ADME/Tox predictions and the drug repurposing concept for future use of old drugs against the COVID-19 [O] . Lorane Izabel da Silva Hage-Melim, Leonardo Bruno Federico, Nayana Keyla Seabra de Oliveira, -1

机译：虚拟筛选ADME / Tox预测以及针对将来针对COVID-19的旧药物使用的药物重用概念
7. ADME evaluation in drug discovery. 6. Can oral bioavailability in humans be effectively predicted by simple molecular property-based rules [O] . Tingjun Hou, Junmei Wang, Wei Zhang, 2015

机译：aDmE药物发现评估。 6.通过简单的基于分子属性的规则可以有效地预测人类口服生物利用度

Screening for human ADME/Tox drug properties in drug discovery.

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