Search research articles

ABOUT JoVE

Overview Leadership Blog JoVE Help Center

AUTHORS

Publishing Process Editorial Board Scope & Policies Peer Review FAQ Submit

LIBRARIANS

Testimonials Subscriptions Access Resources Library Advisory Board FAQ

RESEARCH

JoVE Journal Methods Collections JoVE Encyclopedia of Experiments Archive

EDUCATION

JoVE Core JoVE Business JoVE Science Education JoVE Lab Manual Faculty Resource Center Faculty Site

Terms & Conditions of Use

Search research articles

Related Experiment Videos

In vitro preclinical lead optimisation technologies (PLOTs) in pharmaceutical development.

C K Atterwill¹, M G Wing

¹Biosciences Division, Huntingdon Life Sciences, Woolley Road, Alconbury, Huntingdon, Cambridgeshire PE28 4HS, UK.

Alternatives to Laboratory Animals : ATLA

|December 6, 2000

Summary

High-throughput screening generates many drug candidates. Medium-throughput screening optimizes these leads by assessing absorption, distribution, metabolism, excretion (ADME), and toxicity, improving drug development efficiency.

Related Concept Videos

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by

Same author

Experimental strategies to discover and develop the next generation of psychedelics and entactogens as medicines.

Neuropharmacology·2022

Same author

Effects of the neurotoxin ethylcholine mustard aziridinium in rat brain reaggregate cultures.

Toxicology in vitro : an international journal published in association with BIBRA·2010

Same author

Aluminium and iron induced metabolic changes in neuroblastoma cell lines and rat primary neural cultures.

Toxicology in vitro : an international journal published in association with BIBRA·2010

Same author

New models for the In vitro assessment of neurotoxicity in the nervous system and the preliminary validation stages of a 'tiered-test' model.

Toxicology in vitro : an international journal published in association with BIBRA·2010

Same author

Hyperplastic and hypertrophic responses in toxicity and carcinogenesis.

Toxicology in vitro : an international journal published in association with BIBRA·2010

Same author

Neurotoxicity in vitro: Model systems and practical applications. Comparative studies with the cholinergic neurotoxin in primary brain cultures and in rabbit retina in vivo.

Toxicology in vitro : an international journal published in association with BIBRA·2010

Area of Science:

Drug discovery and development
Pharmacology
Toxicology

Background:

High-throughput screening (HTS) generates vast numbers of potential drug candidates.
Selecting promising leads from HTS presents a significant bottleneck in drug development.
Traditional Contract Research Organization (CRO) roles focused on late-stage regulatory support.

Purpose of the Study:

To address the lead candidate selection bottleneck in drug discovery.
To introduce preclinical lead optimization technologies.
To bridge the gap between HTS and safety assessment.

Main Methods:

Employing medium-throughput screening (MTS) for lead optimization.
Ranking compounds based on absorption, distribution, metabolism, excretion (ADME) properties.

Related Experiment Videos

Evaluating toxicological profiles of potential drug candidates.

Main Results:

MTS allows for efficient ranking of compounds identified from HTS.
Preclinical optimization technologies facilitate earlier selection of leading candidates.
The role of CROs is evolving towards supporting early-stage lead optimization.

Conclusions:

Advancements in preclinical lead optimization are crucial for efficient drug development.
Integrating MTS into the early stages streamlines the selection of viable drug candidates.
CROs are increasingly involved in preclinical optimization, enhancing the drug discovery pipeline.