+ Site Statistics
References:
54,258,434
Abstracts:
29,560,870
PMIDs:
28,072,757
+ Search Articles
+ Subscribe to Site Feeds
Most Shared
PDF Full Text
+ PDF Full Text
Request PDF Full Text
+ Follow Us
Follow on Facebook
Follow on Twitter
Follow on LinkedIn
+ Translate
+ Recently Requested

Recent advances in physicochemical and ADMET profiling in drug discovery



Recent advances in physicochemical and ADMET profiling in drug discovery



Chemistry and Biodiversity 6(11): 1887-1899



The drastic increase in the cost for discovering and developing a new drug along with the high attrition rate of development candidates led to shifting drug-discovery strategy to parallel assessment of comprehensive drug physicochemical, and absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties alongside efficacy. With the proposal of a profiling paradigm and utilization of integrated risk assessment, one can exponentially enhance the predictive power of in vitro tools by taking into consideration the interplay among profiling parameters. In particular, this article will review recent advances in accurate assessment of solubility and other physicochemical parameters. The proper interpretation of these experimental data is crucial for rapid and meaningful risk assessment and rational optimization of drug candidates in drug discovery. The impact of these tools on assisting drug-discovery teams in establishing in vitro-in vivo correlation (IVIVC) as well as structure-property relationship (SPR) will be presented.

(PDF emailed within 0-6 h: $19.90)

Accession: 055398405

Download citation: RISBibTeXText

PMID: 19937823

DOI: 10.1002/cbdv.200900117


Related references

Physicochemical profiling and drug absorption at the drug discovery stage. Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica 133(5): 270-273, 2009

High throughput physicochemical profiling for drug discovery. Journal of Pharmaceutical Sciences 90(11): 1838-1858, 2001

Physicochemical profiling and preformulation studies at the drug discovery stage. Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica 127(3): 213-216, 2006

Impact of physicochemical profiling for rational approach on drug discovery. Chemical and Pharmaceutical Bulletin 61(12): 1228-1238, 2014

Impact of Physicochemical Profiling for Rational Approach on Drug Discovery. Chemical & Pharmaceutical Bulletin 61(12): 1228-1238, 2013

High throughput screening of physicochemical properties and in vitro ADME profiling in drug discovery. Combinatorial Chemistry and High Throughput Screening 12(3): 315-329, 2009

Recent Advances in Drug Design and Drug Discovery for Androgen- Dependent Diseases. Current Medicinal Chemistry 23(8): 792-815, 2016

Recent advances in computational prediction of drug absorption and permeability in drug discovery. Current Medicinal Chemistry 13(22): 2653-2667, 2006

Recent advances in computer-aided drug design as applied to anti-influenza drug discovery. Current Topics in Medicinal Chemistry 14(16): 1875-1889, 2015

Recent advances in malaria drug discovery. Recent Patents on Anti-Infective Drug Discovery 2(2): 95-114, 2008

Targeting C5a: recent advances in drug discovery. Current Medicinal Chemistry 12(2): 217-236, 2005

Recent advances in malaria drug discovery. Bioorganic and Medicinal Chemistry Letters 23(10): 2829-2843, 2013

Recent development in high-throughput bioanalytical support for in vitro ADMET profiling. Expert Opinion on Drug Metabolism and Toxicology 6(3): 321-336, 2010

Recent Advances Toward the Discovery of Drug-Like Peptides De novo. Frontiers in Chemistry 3: 69, 2016

Recent advances in combinatorial biosynthesis for drug discovery. Drug Design, Development and Therapy 9: 823-833, 2016