PET in neurotherapeutic discovery and development
Positron emission tomography (PET) is a highly sensitive, quantitative imaging technique that can track sub-nanomolar quantities of positron-emitting radionuclides throughout the body. By incorporating such radionuclides into molecules of interest, we can directly assess their pharmacokinetic and ph...
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| Format: | Article |
| Language: | English |
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Elsevier
2025-01-01
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| Series: | Neurotherapeutics |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S1878747924001855 |
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| author | Melissa Chassé Neil Vasdev |
| author_facet | Melissa Chassé Neil Vasdev |
| author_sort | Melissa Chassé |
| collection | DOAJ |
| description | Positron emission tomography (PET) is a highly sensitive, quantitative imaging technique that can track sub-nanomolar quantities of positron-emitting radionuclides throughout the body. By incorporating such radionuclides into molecules of interest, we can directly assess their pharmacokinetic and pharmacodynamic (PK/PD) characteristics in vivo without changing their physicochemical characteristics or eliciting a pharmacological response. As such, PET imaging has long been used as a tool to aid drug discovery programs from preclinical biomarker validation all the way through to clinical trials. In this perspective we discuss the use of PET radioligands in central nervous system (CNS) drug discovery and development, with a focus on recent applications in psychiatry (e.g. 5-HT2A, 11β-HSD1), neuro-oncology (e.g. KRASG12C, ATM, ALK2), and neurodegeneration (e.g. amyloid beta plaques, MAPK p38), while exploring the intricacies associated with developing novel radiotracers for CNS targets. Examples highlight the preclinical and clinical uses of PET for studying biomarker function, drug candidate PK/PD, target occupancy/engagement, dosing regimen determination, clinical trial patient selection, and quantifying biomarker changes in response to treatments. |
| format | Article |
| id | doaj-art-38241035d421484a89f7523f5164c3ee |
| institution | Kabale University |
| issn | 1878-7479 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Neurotherapeutics |
| spelling | doaj-art-38241035d421484a89f7523f5164c3ee2025-02-01T04:11:53ZengElsevierNeurotherapeutics1878-74792025-01-01221e00498PET in neurotherapeutic discovery and developmentMelissa Chassé0Neil Vasdev1Azrieli Centre for Neuro-Radiochemistry, Brain Health Imaging Centre, Centre for Addiction and Mental Health, Campbell Family Mental Health Research Institute, Toronto, Canada; Institute of Medical Science, Temerty Faculty of Medicine, University of Toronto, CanadaAzrieli Centre for Neuro-Radiochemistry, Brain Health Imaging Centre, Centre for Addiction and Mental Health, Campbell Family Mental Health Research Institute, Toronto, Canada; Institute of Medical Science, Temerty Faculty of Medicine, University of Toronto, Canada; Corresponding author.Positron emission tomography (PET) is a highly sensitive, quantitative imaging technique that can track sub-nanomolar quantities of positron-emitting radionuclides throughout the body. By incorporating such radionuclides into molecules of interest, we can directly assess their pharmacokinetic and pharmacodynamic (PK/PD) characteristics in vivo without changing their physicochemical characteristics or eliciting a pharmacological response. As such, PET imaging has long been used as a tool to aid drug discovery programs from preclinical biomarker validation all the way through to clinical trials. In this perspective we discuss the use of PET radioligands in central nervous system (CNS) drug discovery and development, with a focus on recent applications in psychiatry (e.g. 5-HT2A, 11β-HSD1), neuro-oncology (e.g. KRASG12C, ATM, ALK2), and neurodegeneration (e.g. amyloid beta plaques, MAPK p38), while exploring the intricacies associated with developing novel radiotracers for CNS targets. Examples highlight the preclinical and clinical uses of PET for studying biomarker function, drug candidate PK/PD, target occupancy/engagement, dosing regimen determination, clinical trial patient selection, and quantifying biomarker changes in response to treatments.http://www.sciencedirect.com/science/article/pii/S1878747924001855Positron emission tomographyNeuroimagingRadiochemistrySmall molecule drug developmentCarbon-11Fluorine-18 |
| spellingShingle | Melissa Chassé Neil Vasdev PET in neurotherapeutic discovery and development Neurotherapeutics Positron emission tomography Neuroimaging Radiochemistry Small molecule drug development Carbon-11 Fluorine-18 |
| title | PET in neurotherapeutic discovery and development |
| title_full | PET in neurotherapeutic discovery and development |
| title_fullStr | PET in neurotherapeutic discovery and development |
| title_full_unstemmed | PET in neurotherapeutic discovery and development |
| title_short | PET in neurotherapeutic discovery and development |
| title_sort | pet in neurotherapeutic discovery and development |
| topic | Positron emission tomography Neuroimaging Radiochemistry Small molecule drug development Carbon-11 Fluorine-18 |
| url | http://www.sciencedirect.com/science/article/pii/S1878747924001855 |
| work_keys_str_mv | AT melissachasse petinneurotherapeuticdiscoveryanddevelopment AT neilvasdev petinneurotherapeuticdiscoveryanddevelopment |