Tackling Poor Bioavailability With Early Formulation Strategies

Low oral bioavailability is a major hurdle in drug development, contributing significantly to the high failure rate in clinical trials. Many promising drug candidates, particularly new chemical entities (NCEs), are highly lipophilic and have low aqueous solubility, which limits absorption and systemic exposure in the body. These poorly soluble compounds often fall into the Biopharmaceutics Classification System (BCS) Class II or IV, where solubility, not permeability, is the rate-limiting factor.

Addressing poor solubility early in development is critical to mitigate challenges like unpredictable pharmacokinetics and delayed timelines. Enabling formulation strategies—such as amorphous solid dispersions, lipid-based systems, or micronization—can often resolve solubility issues, turning a poorly soluble candidate into a viable clinical product. However, choosing the most effective strategy requires a data-driven approach that leverages minimal active pharmaceutical ingredient (API). Learn about a comprehensive, eight-week platform designed to identify the optimal formulation path for your challenging compound.