The aim of this current review is to summarize the present status of pharmacokinetics in Drug Discovery. The review is structured into four sections. The first section is a general overview of what we understand by pharmacokinetics and the different LADMET aspects: Liberation, Absorption, Distributi
Pharmacokinetics and metabolism in early drug discovery
โ Scribed by Dennis A Smith; Han van de Waterbeemd
- Publisher
- Elsevier Science
- Year
- 1999
- Tongue
- English
- Weight
- 663 KB
- Volume
- 3
- Category
- Article
- ISSN
- 1367-5931
No coin nor oath required. For personal study only.
โฆ Synopsis
The need for high-throughput approaches in absorption, distribution, metabolism and excretion studies is driven by the impact of high-speed chemistry and pharmacological screening. Perhaps an even greater impact is that these studies will, in the future, provide large data sets that can be used to predict biological events related to absorption, bioavailability and metabolism of drugs. Through linking of in silica and in vitro methods, considerable progress has recently been made towards this future perspective. Despite this progress, these approaches do not yet replace in viva methods.
๐ SIMILAR VOLUMES
## Abstract Metabolism by the host organism is one of the most important determinants of the pharmacokinetic profile of a drug. High metabolic lability usually leads to poor bioavailability and high clearance. Formation of active or toxic metabolites will have an impact on the pharmacological and t
With the extensive use of different strains of mice and rats in in vivo efficacy models, lack of relevant metabolic clearance data among strains has been a concern. Metabolic clearance is an important parameter impacting drug discovery, and it is often used as a compound selection filter. Metabolica