Pharmacodynamic characterization of a STAT3 inhibitor

Important results from the project

STAT3 is a protein that is frequently activated in different types of cancer, leading to uncontrolled growth of tumor cells, treatment resistance and tumor induced immunosuppression. However, it has been a great challenge dug like molecules that can specifically block STAT3 and that display a clear correlation between effect and exposure. The purpose of the project was to demonstrate a correlation between dose, exposure and effect for Glactone’s STAT3 inhibitor and generate knowledge and data that support the continued development.

Expected long term effects

The results from the project showed that Glactone’s compound had very good pharmacokinetic properties. The development of a pharmacodynamic model demonstrated that it is possible to have a relevant and specific model for STAT3 inhibition in vivo. The positive outcome of the project motivates continued work focused on establishing a marker for efficacy and shows a clear differentiation between Glactone’s compound and other STAT3 inhibitors.

Approach and implementation

The project and its work packages were designed in collaboration with leading experts in pharmacokinetics and pharmacodynamics. The different parts of the project were executed using contract research laboratories. The original plan was modified through the development and utilization of a more relevant model of STAT3 inhibition. This new model will find continued use, following slight optimization, throughout the project’s development. The other studies were performed as planned and data from the studies were analyzed in cooperation with the project participants.