Skip to main content
Key Specialties
Cardiology Diabetology Endocrinology Gastroenterology Geriatrics and Gerontology Gynecology and Obstetrics Hematology Infectious Disease Internal Medicine Nephrology Neurology Oncology Pediatrics Respiratory Medicine Rheumatology Surgery
Congress Coverage
2024 ACC Congress 2023 ESMO Congress 2023 EASD Congress 2023 ERS Congress 2023 ESC Congress
Clinical Collections
Advances in Alzheimer’s

At a glance: The STEP trials

A round-up of the STEP phase 3 clinical trials evaluating semaglutide for weight loss in people with overweight or obesity.
ADVANCED SEARCH
Log in
Top
European Journal of Nuclear Medicine and Molecular Imaging
Published in: European Journal of Nuclear Medicine and Molecular Imaging 12/2016

Open Access 01-11-2016 | Guidelines

Guidelines to PET measurements of the target occupancy in the brain for drug development

Authors: Akihiro Takano, Andrea Varrone, Balázs Gulyás, Piero Salvadori, Antony Gee, Albert Windhorst, Johnny Vercouillie, Guy Bormans, Adriaan A. Lammertsma, Christer Halldin

Published in: European Journal of Nuclear Medicine and Molecular Imaging | Issue 12/2016

Login to get access

Abstract

This guideline summarizes the current view of the European Association of Nuclear Medicine Drug Development Committee. The purpose of this guideline is to guarantee a high standard of PET studies that are aimed at measuring target occupancy in the brain within the framework of development programs of drugs that act within the central nervous system (CNS drugs). This guideline is intended to present information specifically adapted to European practice. The information provided should be applied within the context of local conditions and regulations.
Literature
1.
DiMasi JA, Hansen RW, Grabowski HG. The price of innovation: new estimates of drug development costs. J Health Econ. 2003;22:151–85.CrossRefPubMed
2.
Lee CM, Farde L. Using positron emission tomography to facilitate CNS drug development. TRENDS Pharmacol Sci. 2006;27:310–6.CrossRefPubMed
3.
Halldin C, Gulyás B, Farde L. PET studies with carbon-11 radioligands in neuropsychopharmacological drug development. Curr Pharm Des. 2001;7:1907–29.CrossRefPubMed
4.
Innis RB, Cunningham VJ, Delforge J, Fujita M, Gjedde A, Gunn RN, et al. Consensus nomenclature for in vivo imaging of reversibly binding radioligands. J Cereb Blood Flow Metab. 2007;27:1533–9.CrossRefPubMed
5.
ICRP Publication 106. Radiation dose to patients from radiopharmaceuticals. Ann. ICRP 2008, 38: 61–65 and 81–84.
6.
Zanotti-Fregonara P, Innis RB. Suggested pathway to assess radiation safety of 11C-labeled PET tracers for first-in-human studies. Eur J Nucl Med Mol Imaging. 2012;39:544–7.CrossRefPubMed
7.
Zanotti-Fregonara P, Lammertsma AA, Innis RB. Suggested pathway to assess radiation safety of 18F-labeled PET tracers for first-in-human studies. Eur J Nucl Med Mol Imaging. 2013;40:1781–3.CrossRefPubMed
8.
ICRP publication 103. The 2007 recommendations of the international commission on radiological protection. Ann ICRP. 2007; 37: 116–117.
9.
Logan J, Fowler JS, Volkow ND, Wang GJ, Ding YS, Alexoff DL. Distribution volume ratios without blood sampling from graphical analysis of PET data. J Cereb Blood Flow Metab. 1996;16:834–40.CrossRefPubMed
10.
Lammertsma AA, Hume SP. Simplified reference tissue model for PET receptor studies. Neuroimage. 1996;4:153–8.CrossRefPubMed
11.
Ichise M, Liow JS, Lu JQ, Takano A, Model K, Toyama H, et al. Linearized reference tissue parametric imaging methods: application to [11C]DASB positron emission tomography studies of the serotonin transporter in human brain. J Cereb Blood Flow Metab. 2003;23:1096–112.CrossRefPubMed
12.
Terry GE, Liow JS, Zoghbi SS, Hirvonen J, Farris AG, Lerner A, et al. Quantitation of cannabinoid CB1 receptors in healthy human brain using positron emission tomography and an inverse agonist radioligand. Neuroimage. 2009;48:362–70.CrossRefPubMedPubMedCentral
13.
Lassen NA, Bartenstein PA, Lammertsma AA, Prevett MC, Turton DR, Luthra SK, et al. Benzodiazepine receptor quantification in vivo in humans using [11C]flumazenil and PET: Application of the steady-state principle. J Cereb Blood Flow Metab. 1995;15:152–65.CrossRefPubMed
14.
Bench CJ, Price GW, Lammertsma AA, Cremer JC, Luthra SK, Turton D, et al. Eur J Clin Pharmacol. 1991;40:169–73.CrossRefPubMed
15.
Fowler JS, Wang GJ, Logan J, Xie S, Volkow ND, MacGregor RR, et al. Selective reduction of radiotracer trapping by deuterium substitution: comparison of carbon-11-L-deprenyl and carbon-11-deprenyl-D2 for MAO B mapping. J Nucl Med. 1995;36:1255–62.PubMed
16.
Hill AV. The possible effects of the aggregation of the molecules of haemoglobin on its dissociation curves. J Physiol. 1910;40:iv–vii.
17.
Farde L, Nordström AL, Wiesel FA, Pauli S, Halldin C, Sedvall G. Positron emission tomographic analysis of central D1 and D2 dopamine receptor occupancy in patients treated with classical neuroleptics and clozapine. relation to extrapyramidal side effects. Arch Gen Psychiatry. 1992;49:538–44.CrossRefPubMed
18.
Bench CJ, Lammertsma AA, Dolan RJ, Grasby PM, Warrington SJ, Gunn K, et al. Dose dependent occupancy of central dopamine D2 receptors by the novel neuroleptic CP-88,059-01: a study using positron emission tomography and 11C-raclopride. Psychopharmacol (Berl). 1993;112(2–3):308–14.CrossRef
19.
Meyer JH, Wilson AA, Sagrati S, Hussey D, Carella A, Potter WZ, et al. Serotonin transporter occupancy of five selective serotonin reuptake inhibitors at different doses: an [11C]DASB positron emission tomography study. Am J Psychiatry. 2004;161:826–35.CrossRefPubMed
20.
Bench CJ, Lammertsma AA, Grasby PM, Dolan RJ, Warrington SJ, Boyce M, et al. The time course of binding to striatal dopamine D2 receptors by the neuroleptic ziprasidone (CP-88,059-01) determined by positron emission tomography. Psychopharmacol (Berl). 1996;124:141–7.CrossRef
21.
Takano A, Suzuki K, Kosaka J, Ota M, Nozaki S, Ikoma Y, et al. A dose-finding study of duloxetine based on serotonin transporter occupancy. Psychopharmacol (Berl). 2006;185:395–9.CrossRef
Metadata
Title
Guidelines to PET measurements of the target occupancy in the brain for drug development
Authors
Akihiro Takano
Andrea Varrone
Balázs Gulyás
Piero Salvadori
Antony Gee
Albert Windhorst
Johnny Vercouillie
Guy Bormans
Adriaan A. Lammertsma
Christer Halldin
Publication date
01-11-2016
Publisher
Springer Berlin Heidelberg
Published in
European Journal of Nuclear Medicine and Molecular Imaging / Issue 12/2016
Print ISSN: 1619-7070
Electronic ISSN: 1619-7089
DOI
https://doi.org/10.1007/s00259-016-3476-4

Other articles of this Issue 12/2016

European Journal of Nuclear Medicine and Molecular Imaging 12/2016 Go to the issue

Original Article

Decreased in vivo availability of the cannabinoid type 2 receptor in Alzheimer’s disease

Letter to the Editor

Strategy based on kinetics of O-(2-[18F] fluoroethyl)-L-tyrosine ([18F] FET)

Original Article

ImmunoPET for assessing the differential uptake of a CD146-specific monoclonal antibody in lung cancer

Editorial Commentary

PET/CT imaging for evaluating response to therapy in castration-resistant prostate cancer

Editorial Commentary

ImmunoPET to help stratify patients for targeted therapies and to improve drug development

Editorial Commentary

How reliable is 18FDG PET for predicting the onset of Huntington’s disease?