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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
PubMed
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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.

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.