Application of pharmaceutical profiling assays for optimization of drug-like properties

被引：0

作者：

Di, L ^{[1
]}

Kerns, EH ^{[1
]}

机构：

[1] Wyeth Inc, Monmouth Jct, NJ 08852 USA

来源：

CURRENT OPINION IN DRUG DISCOVERY & DEVELOPMENT | 2005年 / 8卷 / 04期

关键词：

ADME/toxicity; blood-brain barrier; cytochrome P450 inhibition; metabolism; solubility; stability; permeability; prodrugs;

D O I：

暂无

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Pharmaceutical profiling assays provide an early assessment of drug-like properties, such as solubility, permeability, metabolism, stability and drug-drug interactions. This information can be used to alert project teams to potential property issues, predict and diagnose in vivo assay results, guide structure-property relationships, provide insight into structure modification, and help drug discovery teams to make informed decisions. Successful drugs can be developed when biological activities of interest and pharmaceutical properties are optimized in parallel.

引用

页码：495 / 504

页数：10

共 50 条

[21] Endogenous drug-like factors
Mrozikiewicz, A
POLISH JOURNAL OF PHARMACOLOGY, 1998, 50 (06): : 393 - 397
[22] Drug-like Properties and Fraction Lipophilicity Index as a combined metric
Tsantili-Kakoulidou, Anna
Demopoulos, Vassilis J.
ADMET AND DMPK, 2021, 9 (03): : 177 - 190
[23] The impact of physical organic chemistry on the control of drug-like properties
Davis, AM
Riley, R
DRUG DESIGN: CUTTING EDGE APPROACHES, 2002, (279): : 106 - 123
[24] An Overview on the Anticancer Potential of Punarnavine: Prediction of Drug-Like Properties
Ahmad, Imad
Khan, Haroon
Amin, Muhammad Usman
Khalid, Shah
Behl, Tapan
Rahman, Najeeb Ur
ONCOLOGIE, 2021, 23 (03) : 321 - 333
[25] Drug-like properties and topical delivery of rapalogs and tacrolimus in ophthalmology
Sigurdsson, Hakon H.
Jansook, Phatsawee
Loftsson, Thorsteinn
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY, 2024, 101
[26] Improved drug-like properties of therapeutic proteins by directed evolution
Buchanan, Andrew
Ferraro, Franco
Rust, Steven
Sridharan, Sudharsan
Franks, Ruth
Dean, Greg
McCourt, Matthew
Jermutus, Lutz
Minter, Ralph
PROTEIN ENGINEERING DESIGN & SELECTION, 2012, 25 (10): : 631 - 638
[27] Drug-like properties and the causes of poor solubility and poor permeability
Lipinski, CA
JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS, 2000, 44 (01) : 235 - 249
[28] Considering the impact drug-like properties have on the chance of success
Yusof, Iskander
Segall, Matthew D.
DRUG DISCOVERY TODAY, 2013, 18 (13-14) : 659 - 666
[29] Antimalarial Trioxolanes with Superior Drug-Like Properties and In Vivo Efficacy
Blank, Brian R.
Gonciarz, Ryan L.
Talukder, Poulami
Gut, Jiri
Legac, Jennifer
Rosenthal, Philip J.
Renslo, Adam R.
ACS INFECTIOUS DISEASES, 2020, 6 (07): : 1827 - 1835
[30] Physicochemical properties of drug-like fluids using thermodynamic models
Akbari, Falamarz
Farhadi, Mitra
PHYSICS AND CHEMISTRY OF LIQUIDS, 2022, 60 (01) : 95 - 110

← 1 2 3 4 5 →