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Published on: January 7, 2019
Growth factor/peptide receptor imaging for the development of targeted therapy in oncology
Christophe Van de Wiele1, Hendricus Boersma, Rudi A Dierckx
1Department of Nuclear Medicine, De Pintelaan 185B, 9000 Ghent, Belgium. christophe.vandewiele@ugent.be
Abstract:
Receptor imaging by means of positron emission tomography (PET) and single photon emission computerized tomography (SPECT) may non-invasively address questions that are essential to the development and the clinical application of drugs targeting receptors expressed on human malignancies : is the receptor targeting drug getting to the tumor in the required concentration, is there a heterogeneity in tumor uptake, how fast is the drug cleared from the tumor and how is the receptor targeting drug metabolized. Such information may be used to assess the efficacy of strategies that aim to improve drug penetration through tumor tissue or to select compounds based on their ability to penetrate tumor tissue, thereby increasing the therapeutic index. In addition, imaging by means of PET and SPECT with receptor targeting radiopharmaceuticals may allow for the selection of patients that may benefit from receptor targeting therapies either ab initio, in the situation where the levels of receptor expression are proportional to the level of signaling via the receptor, or through sequential imaging in the situation where the level of receptor expression is not proportional to the level of signaling via the receptor and proof of down-regulation of the number of receptors is required.
Insights
Positron emission tomography (PET) and single photon emission computerized tomography (SPECT) enable non-invasive receptor imaging for cancer drug development. This technique assesses drug delivery, tumor uptake, and metabolism, aiding patient selection for targeted therapies.
Area of Science:
- Nuclear medicine
- Radiopharmacology
- Oncology
Background:
- Receptor imaging is crucial for developing and applying drugs targeting human malignancy receptors.
- Positron emission tomography (PET) and single photon emission computerized tomography (SPECT) offer non-invasive assessment of drug behavior in tumors.
Purpose of the Study:
- To highlight the essential role of PET and SPECT in evaluating receptor-targeting drugs for cancer.
- To demonstrate how imaging can optimize drug development, assess therapeutic strategies, and guide patient selection for targeted therapies.
Main Methods:
- Utilizing receptor targeting radiopharmaceuticals with PET and SPECT.
- Analyzing drug concentration, tumor uptake heterogeneity, clearance rates, and metabolism.
- Assessing strategies to improve drug penetration and selecting compounds with optimal tumor penetration.
Main Results:
- Imaging provides critical data on drug-tumor interactions, including concentration and heterogeneity.
- PET and SPECT facilitate evaluation of drug clearance and metabolism within tumors.
- These imaging modalities aid in selecting patients likely to benefit from receptor-targeting therapies.
Conclusions:
- PET and SPECT imaging are indispensable tools for advancing receptor-targeting cancer drug development and clinical application.
- Imaging enables personalized medicine approaches by identifying suitable candidates for targeted therapies.
- The data derived from receptor imaging supports optimizing treatment strategies and improving therapeutic outcomes.
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