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Updated: Feb 13, 2026

A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development
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A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development

Published on: February 11, 2019

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Receptor Occupancy Imaging Studies in Oncology Drug Development

Ingrid J G Burvenich1,2, Sagun Parakh1,2,3, Adam C Parslow1,2

  • 1Tumour Targeting Laboratory, Olivia Newton-John Cancer Research Institute, Melbourne, Australia.

The AAPS Journal
|March 10, 2018
PubMed

Insights

Molecular imaging, including PET and SPECT, helps determine optimal therapeutic doses by assessing drug delivery and target engagement. Early imaging studies improve drug development, dose selection, and patient stratification for better treatment outcomes.

Area of Science:

  • Oncology
  • Radiology
  • Pharmacology

Background:

  • Therapeutic dose selection for tumors is complex.
  • Molecular imaging techniques like PET and SPECT can answer key questions about drug efficacy.
  • Combining functional and anatomical imaging aids in understanding treatment effects.

Purpose of the Study:

  • To review the value of translational receptor occupancy studies and molecular imaging in early drug development.
  • To highlight how imaging can optimize therapeutic dose selection.
  • To explore improvements in patient stratification for enhanced drug utility.

Main Methods:

  • Utilizing positron emission tomography (PET) and single-photon emission computed tomography (SPECT) for molecular imaging.
  • Integrating functional imaging (PET/SPECT) with anatomical imaging (MRI/CT).
  • Conducting in vivo competition studies with specific radioligands to assess drug-target interactions.

Main Results:

  • Molecular imaging assesses drug reach, target engagement, dose sufficiency, and target saturation.
  • Combined imaging modalities allow correlation of drug occupancy with anatomical/physiological changes.
  • In vivo studies directly link drug plasma concentration to target occupancy.

Conclusions:

  • Early integration of molecular imaging and receptor occupancy studies is crucial for effective drug development.
  • Imaging aids in precise therapeutic dose selection and refinement.
  • Improved patient stratification through imaging can maximize drug effectiveness post-approval.
Keywords:
drug developmentpositron emission tomography (PET)receptor imagingreceptor occupancysingle–photon emission tomography (SPECT)

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