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 downregulation of the number of receptors is required.
Keywords: PET, SPECT, receptor imaging, targeted therapie
Current Pharmaceutical Design
Title: Growth Factor/Peptide Receptor Imaging for the Development of Targeted Therapy in Oncology
Volume: 14 Issue: 31
Author(s): Christophe Van de Wiele, Hendricus Boersma, Rudi A. Dierckx, Bart De Spiegeleer, Aren Van Waarde and Philip H. Elsinga
Affiliation:
Keywords: PET, SPECT, receptor imaging, targeted therapie
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 downregulation of the number of receptors is required.
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de Wiele Van Christophe, Boersma Hendricus, Dierckx A. Rudi, De Spiegeleer Bart, Waarde Van Aren and Elsinga H. Philip, Growth Factor/Peptide Receptor Imaging for the Development of Targeted Therapy in Oncology, Current Pharmaceutical Design 2008; 14 (31) . https://dx.doi.org/10.2174/138161208786549434
DOI https://dx.doi.org/10.2174/138161208786549434 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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