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Title: Receptor Occupancy Imaging Studies in Oncology Drug Development.
Austin Authors: Burvenich, Ingrid J G;Parakh, Sagun ;Parslow, Adam C;Lee, Sze Ting ;Gan, Hui K ;Scott, Andrew M 
Affiliation: Tumour Targeting Laboratory, Olivia Newton-John Cancer Research Institute, Heidelberg, Victoria, Australia
School of Cancer Medicine, La Trobe University, Melbourne, Australia
Department of Medical Oncology, Austin Health, Heidelberg, Victoria, Australia
Department of Molecular Imaging and Therapy, Austin Health, Heidelberg, Victoria, Australia
Department of Medicine, University of Melbourne, Melbourne, Australia
Issue Date: 8-Mar-2018 2018-03-08
Publication information: The AAPS journal 2018; 20(2): 43
Abstract: 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.
DOI: 10.1208/s12248-018-0203-z
ORCID: 0000-0001-8641-456X
PubMed URL: 29520671
Type: Journal Article
Subjects: drug development
positron emission tomography (PET)
receptor imaging
receptor occupancy
single–photon emission tomography (SPECT)
Appears in Collections:Journal articles

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