The Unique Pharmacometrics of Small Molecule Therapeutic Drug Tracer Imaging for Clinical Oncology

SIMPLE SUMMARY: New clinical radiology scans using trace amounts of therapeutic cancer drugs labeled with radioisotope injected into patients can provide oncologists with fundamentally unique insights about drug delivery to tumors. This new application of radiology aims to improve how cancer drugs are used, towards improving patient outcomes. The article reviews published clinical research in this important new field. ABSTRACT: Translational development of radiolabeled analogues or isotopologues of small molecule therapeutic drugs as clinical imaging biomarkers for optimizing patient outcomes in targeted cancer therapy aims to address an urgent and recurring clinical need in therapeutic cancer drug development: drug- and target-specific biomarker assays that can optimize patient selection, dosing strategy, and response assessment. Imaging the in vivo tumor pharmacokinetics and biomolecular pharmacodynamics of small molecule cancer drugs offers patient- and tumor-specific data which are not available from other pharmacometric modalities. This review article examines clinical research with a growing pharmacopoeia of investigational small molecule cancer drug tracers.