The AAPS Journal

, 20:43 | Cite as

Receptor Occupancy Imaging Studies in Oncology Drug Development

  • Ingrid J. G. Burvenich
  • Sagun Parakh
  • Adam C. Parslow
  • Sze Ting Lee
  • Hui K. Gan
  • Andrew M. Scott
Review Article Theme: Advances and Applications of In Vivo Medical Imaging in Drug Development and Regulation
Part of the following topical collections:
  1. Theme: Advances and Applications of In Vivo Medical Imaging in Drug Development and Regulation


The selection of therapeutic dose for the most effective treatment of tumours is an intricate interplay of factors. Molecular imaging with positron emission tomography (PET) or single–photon emission computed tomography (SPECT) can address questions central to this selection: Does the drug reach its target? Does the drug engage with the target of interest? Is the drug dose sufficient to elicit the desired pharmacological effect? Does the dose saturate available target sites? Combining functional PET and SPECT imaging with anatomical imaging technologies such as magnetic resonance imaging (MRI) or computed tomography (CT) allows drug occupancy at the target to be related directly to anatomical or physiological changes in a tissue resulting from therapy. In vivo competition studies, using a tracer amount of radioligand that binds to the tumour receptor with high specificity, enable direct assessment of the relationship between drug plasma concentration and target occupancy. Including imaging studies in early drug development can aid with dose selection and suggest improvements for patient stratification to obtain higher effective utility from a drug after approval. In this review, the potential value of including translational receptor occupancy studies and molecular imaging strategies early on in drug development is addressed.


drug development positron emission tomography (PET) receptor imaging receptor occupancy single–photon emission tomography (SPECT) 


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Copyright information

© American Association of Pharmaceutical Scientists 2018

Authors and Affiliations

  • Ingrid J. G. Burvenich
    • 1
    • 2
  • Sagun Parakh
    • 1
    • 2
    • 3
  • Adam C. Parslow
    • 1
    • 2
  • Sze Ting Lee
    • 2
    • 4
  • Hui K. Gan
    • 1
    • 2
    • 3
  • Andrew M. Scott
    • 1
    • 2
    • 3
    • 4
    • 5
    • 6
  1. 1.Tumour Targeting LaboratoryOlivia Newton-John Cancer Research InstituteMelbourneAustralia
  2. 2.School of Cancer MedicineLa Trobe UniversityMelbourneAustralia
  3. 3.Department of Medical OncologyAustin HealthMelbourneAustralia
  4. 4.Department of Molecular Imaging and TherapyAustin HealthMelbourneAustralia
  5. 5.Department of MedicineUniversity of MelbourneMelbourneAustralia
  6. 6.Tumour Targeting LaboratoryOlivia Newton-John Cancer Research InstituteHeidelbergAustralia

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