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Drug Discovery: Overview

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Updated: Jun 21, 2026

High-throughput Screening for Chemical Modulators of Post-transcriptionally Regulated Genes

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Published on: March 3, 2015

High-throughput screening for lead optimization: a rational approach.

M Bajpai¹, K K Adkison

¹Department of Pharmacokinetics and Drug Metabolism, Amgen Inc, CA 91320, USA. mbajpai@amgen.com

Current Opinion in Drug Discovery & Development

|August 4, 2009

Summary

This summary is machine-generated.

Advancements in drug discovery require faster methods to assess how new molecular entities (NMEs) are absorbed, distributed, metabolized, and eliminated (ADME). Improved in vitro and in vivo assays enable earlier prediction of human pharmacokinetics for drug development.

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Area of Science:

Pharmacology
Drug Discovery
Analytical Chemistry

Background:

The pharmaceutical industry faces an increasing number of new molecular entities (NMEs) due to advances in genetics, combinatorial chemistry, and automation.
This surge necessitates improved methods for evaluating compound characteristics early in the drug discovery process.

Purpose of the Study:

To highlight the need for earlier determination of absorption, distribution, and elimination (ADME) properties of NMEs.
To discuss the development of higher-throughput in vitro and in vivo methods for assessing ADME characteristics.

Main Methods:

Development of high-throughput in vitro screens utilizing advancements in analytical technology and molecular biology, often employing human or 'humanized' tissues.
Advancement of in vivo pharmacokinetic throughput using techniques such as mixture dosing and sample pooling.

Main Results:

Refined in vitro and in vivo ADME methods allow for the evaluation of a larger number of molecules.
These improved methods facilitate the prediction of human pharmacokinetics at earlier stages of drug development.

Conclusions:

Continued refinement of ADME assays is crucial for efficient drug discovery and development.
Earlier prediction of human pharmacokinetics using advanced in vitro and in vivo methods will streamline the selection of drug candidates.