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Related Concept Videos

Drug Discovery: Overview01:26

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
Preclinical Development: Overview01:28

Preclinical Development: Overview

Preclinical development consists of a series of tests that ensure the safety and efficacy of a new therapeutic compound before it is tested in humans. There are four main phases to this process. First, safety pharmacology tests are conducted to ensure the drug does not produce any acutely harmful effects. These tests examine parameters such as bronchoconstriction, cardiac dysrhythmias, blood pressure changes, and ataxia. Next, preliminary toxicological testing is performed to determine the...

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Related Experiment Video

Updated: Jun 6, 2026

Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
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Microdosing in early lead discovery.

A P Jekunen1, E K J Pauwels, K J A Kairemo

  • 1Oncology Unit, Kokkola Central Hospital, 67200 Kokkola, Finland. antti.jekunen@ksshp.fi

Bioanalysis
|November 19, 2010
PubMed
Summary

Microdosing accelerates drug development by enabling early human studies, aiding go/no-go decisions and reducing costs. This approach helps identify effective drug candidates sooner, optimizing the pipeline.

Area of Science:

  • Pharmacology
  • Drug Development
  • Clinical Trials

Background:

  • Early-stage drug development faces challenges in identifying effective compounds.
  • Preclinical studies can be time-consuming and costly.
  • A need exists for efficient methods to assess drug viability before extensive trials.

Purpose of the Study:

  • To evaluate microdosing as a tool for enhancing early drug development.
  • To assess microdosing's utility in go/no-go decision-making for drug candidates.
  • To explore microdosing's role in selecting potential leads at the clinical stage.

Main Methods:

  • Utilizing microdosing to initiate human studies before Phase I trials.
  • Applying microdosing to molecularly targeted compounds with known mechanisms of action.

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  • Gathering data on drug accessibility and biodistribution.

    • Main Results:

    • Microdosing facilitates early assessment of drug candidates, aiding go/no-go decisions.
    • It allows for selection of potential leads at the clinical stage, bypassing some preclinical hurdles.
    • Data on accessibility and biodistribution are obtainable, benefiting molecular development.
    • Steady-state and genetic investigations are becoming feasible.

    Conclusions:

    • Microdosing offers a valuable tool for efficient drug development, saving time and costs.
    • Its application in early human studies enhances decision-making and pipeline optimization.
    • Further original reports are needed to fully establish the significance of microdosing.