Solubility Enhancement Strategies For Targeted Oral Therapies

Next-generation targeted oral therapies, such as targeted protein degraders (TPDs) — including proteolysis-targeting chimeras (PROTACs) and molecular glues — offer significant promise for therapeutic areas where conventional protein inhibitors have proven ineffective or limited. These innovative modalities can unlock new treatment opportunities by selectively degrading disease-causing proteins rather than merely inhibiting them. However, the development of such complex molecules presents notable challenges, including optimizing solubility, permeability, metabolic stability, and overall bioavailability to ensure safe and effective delivery.

To address these hurdles, novel enabling technologies, along with strategic collaborations between drug developers and specialized contract development and manufacturing organizations (CDMOs), are playing an increasingly critical role in accelerating the advancement of targeted oral therapies from early discovery through clinical and commercial stages.