Understanding the Absorption, Metabolism and Excretion of Masitinib in Healthy Male Subjects

Masitinib is a treatment under development for neurology, inflammatory diseases, oncology, and viral infections.

In collaboration with AB Science, TNO, and Pharmaron, Quotient Sciences presented a scientific poster at ISSX 2022 detailing a human ADME study of Masitinib, an oral tyrosine kinase inhibitor targeting mast cells and macrophages. 

The open-label, radiolabeled study involved six healthy male volunteers who received a single oral dose of 14C-masitinib. Using accelerator mass spectrometry (AMS) and UPLC-HRMS, researchers assessed mass balance, routes of elimination, and metabolite profiling. 

Results showed 69% recovery of the radioactive dose, primarily through fecal excretion. Several metabolites were identified, and findings suggested possible covalent binding of masitinib metabolites to plasma proteins.

This study provides critical insights into Masitinib’s pharmacokinetics, supporting its regulatory strategy and further clinical development.

Download the poster to see detailed findings from the ADME program.