Definition

An orally bioavailable radioconjugate composed of ibcasertib, an orally bioavailable inhibitor of select serine-threonine kinases including aurora kinase B (aurora B), vascular endothelial growth factor receptors (VEGFRs), stem cell factor receptor (c-KIT) and platelet-derived growth factor receptors (PDGFRs), radiolabeled with the radioisotope carbon C 14, with potential use for evaluating the pharmacokinetic profile of chiauranib. Upon oral administration of carbon C 14 ibcasertib, ibcasertib targets, binds to and inhibits the activity of aurora B, VEGFRs, c-kit and PDGFRs, which may result in a decrease in the proliferation of tumor cells that overexpress these kinases. Labeling of ibcasertib with the radioactive tracer carbon C 14 allows for the evaluation of chiauranib’s pharmacokinetic profile, including its absorption, distribution, metabolism and excretion (ADME).