PROTAC Enabling Formulation <i>In Vivo</i>: Implications of the Polymeric Carrier Eudragit E PO.

ABSTRACT: Proteolysis targeting chimeras (PROTACs) are heterobifunctional degraders with a unique mode of action that permits access to "undruggable" targets. These molecules pose challenges in terms of solubility and bioavailability due to their physicochemical properties. So far, very little information is available on the potential of enabling formulations of PROTACs in pharmacokinetic studies. In a previous work of our group, amorphous spray-dried formulations (SDDs) of the model PROTAC MS4078 were developed. However, the potential of the amorphous solid dispersions of the PROTAC MS4078 has not yet been examined in vivo. The present study reports on the evaluation of an SDD containing MS4078 and E PO in comparison to a solution vehicle in a pharmacokinetic study in mice. Unexpectedly, ver

SUBMITTER: Hofmann N 

PROVIDER: S-EPMC12505254 | biostudies-literature | 2025 Oct

REPOSITORIES: biostudies-literature