Prediction of pharmacokinetic properties using experimental approaches during early drug discovery.

Abstract:

:There has been a significant increase in the number of compounds synthesized in early drug-discovery programs with the advances in combinatorial chemistry and high-throughput biological screening efforts. Various in silico, in vitro and in situ approaches have been described in literature that achieve higher throughput pharmacokinetic screening. In silico methodologies have mainly attempted to quantify the prospects of oral absorption of compounds based upon their physico-chemical properties. There is a greater availability of in vitro and in situ approaches to screen compounds for intestinal permeability (as a surrogate for absorption) and metabolic stability (as a surrogate for clearance). More recent modifications of the in vitro and in situ approaches to assess the potential of absorption and metabolism have enabled a higher throughput and an ability to correlate better with in vivo pharmacokinetics of compounds.

journal_name

Curr Opin Chem Biol

authors

Chaturvedi PR,Decker CJ,Odinecs A

doi

10.1016/s1367-5931(00)00228-3

subject

Has Abstract

pub_date

2001-08-01 00:00:00

pages

452-63

issue

4

eissn

1367-5931

issn

1879-0402

pii

S1367-5931(00)00228-3

journal_volume

5

pub_type

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