[7] Discovering and Developing Molecules with Optimal Drug-Like Properties, Chapter 2 Discovery Formulations: Approaches and Practices in Early Preclinical Development, P65-72 [8] A F D , A N F , B S G ,et al. Preparation, characterization and in-vivo evaluation of microemulsions containing t...
常用的人体药动学预测方法包括虚拟方法(In silico computational approach)(太简单、准确度太差),异速增长法(Allometric scaling approach),体外/体内外推法(In vitro/in vivo extrapolation,IVIVE)和生理药动学模型(Physiologically based pharmacokinetic approach)(需收集较多数据、需专门软件、操作性差) 七、临床研究中...
DMPK in CNS drug discovery_Ziqiang Cheng_final PRIVILEGED&STRICTLYCONFIDENTIAL CurrentDMPKTechnologiesandStrategiesforCNSDrugDiscovery Ziqiang(Zack)ChengDrugMetabolismandPharmacokinetics GlaxoSmithKlineR&DChina Drugcandidate(候选药物)failingduetoDMPKdropsfrom40%in1991to10%in2002 DrugcompaniesbeganscreeningforDMPK...
This is particularly true in the early stage of drug discovery, where a large number of NCEs needs to be evaluated so that the selected few can proceed to drug development. In vitro models for the assessment of the biopharmaceutical properties such as metabolic stability, permeability across the...
(DMPK) studies investigated the absorption, distribution, metabolism and excretion (ADME) character of a drug with variety of technologies, which provides data for optimization of the potential drug to acquire desirable in vivo performance, as well as predicting the ADME of the potential drug when ...
可惜以前不是学这个的，有些素语不是很理解呢，比如FTiH是什么呢？是不是first in human呢 ...
E. Cooper, "The influence of DMPK as an integrated partner in modern drug discovery," Current Drug Metabolism, vol. 3, no. 5, pp. 527-550, 2002.Riley, R.J.; Martin, I.J.; Cooper, A.E. The influence of DMPK as an integrated partner in modern drug discovery. Curr. Drug Metab....
药物代谢及药代动力学(Drug metabolism & pharmacokinetics,DMPK)是研究药物分子在生物体内吸收、分布、代谢和排泄(Absorption, Distribution, Metabolism & Elimination,ADME)的学科,在药物早期筛选以及后期临床开发阶段都有着重要的作用。因此,笔者想...
[2] Churcher, I., 2018. Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones? Journal of Medicinal Chemistry 61, 444–452. [3] Békés M, Langley DR, Crews CM. PROTAC targeted protein degraders: the past is prologue[J]. Nat Rev Drug Discov...
[10] CaldwellGW1, Ritchie DM, Masucci JA, etc. The new pre-preclinical paradigm: compoundoptimization in early and late phase drug discovery. Curr Top Med Chem. 2001Nov;1(5):353-66. [11] Ballard P, Brassil P, Bui KH, etc. The right compound in the right assay at theright time:...