The road map to oral bioavailability: an industrial perspective

Area of Science:

• Pharmaceutical Sciences
• Drug Discovery
• Biotechnology

Background:

• Optimizing oral bioavailability presents a significant challenge in pharmaceutical and biotechnology industries.
• Increased drug candidate numbers from combinatorial chemistry and a trend towards lipophilic compounds exacerbate solubility issues.
• There is a growing need for efficient in vitro and in silico tools to reduce reliance on in vivo studies.

Purpose of the Study:

• To propose a team-based discussion tool, a 'road map,' to guide the selection of profiling assays for optimizing oral bioavailability.
• To provide a systematic approach for drug discovery teams to address challenges in oral drug delivery.
• To facilitate cross-disciplinary discussions and streamline experimental strategies.

Main Methods:

• Development of a 'road map' framework categorizing factors affecting oral bioavailability into absorption and metabolism.
• Integration of in vitro and in silico tools into the drug discovery workflow.
• Facilitation of team-based discussions to guide assay selection.

Main Results:

• The proposed road map systematically addresses absorption and metabolism factors influencing oral bioavailability.
• It provides a structured approach for selecting appropriate profiling assays.
• The tool aims to improve efficiency and reduce resource utilization in drug discovery.

Conclusions:

• The developed road map serves as a valuable interface for cross-disciplinary collaboration in drug discovery.
• It offers a systematic strategy to achieve acceptable oral bioavailability with minimal resources and time.
• This approach supports the efficient progression of drug candidates through the discovery pipeline.