Microdosing in early lead discovery

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.
• 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.