Literature DB >> 28126682

A multi species evaluation of the radiation dosimetry of [11C]erlotinib, the radiolabeled analog of a clinically utilized tyrosine kinase inhibitor.

J Ryan Petrulli1, Søren B Hansen2, Galith Abourbeh3, Maqsood Yaqub4, Idris Bahce5, Daniel Holden6, Yiyun Huang6, Nabeel B Nabulsi6, Joseph N Contessa7, Eyal Mishani8, Adriaan A Lammertsma9, Evan D Morris10.   

Abstract

INTRODUCTION: Erlotinib is a tyrosine kinase inhibitor prescribed for non-small cell lung cancer (NSCLC) patients bearing epidermal growth factor receptor mutations in the kinase domain. The objectives of this study were to (1) establish a human dosimetry profile of [11C]erlotinib and (2) assess the consistency of calculated equivalent dose across species using the same dosimetry model.
METHODS: Subjects examined in this multi-species study included: a stage IIIa NSCLC patient, 3 rhesus macaque monkeys, a landrace pig, and 4 athymic nude-Fox1nu mice. [11C]erlotinib PET data of the whole body were acquired dynamically for up to 120min. Regions of interest (ROIs) were manually drawn to extract PET time activity curves (TACs) from identifiable organs. TACs were used to calculate time-integrated activity coefficients (residence times) in each ROI, which were then used to calculate the equivalent dose in OLINDA. Subject data were used to predict the equivalent dose to the organs of a 73.7kg human male.
RESULTS: In three of four species, the liver was identified as the organ receiving the highest equivalent dose (critical organ). The mean equivalent doses per unit of injected activity to the liver based on human, monkey, and mouse data were 29.4μSv/MBq, 17.4±6.0μSv/MBq, and 5.27±0.25μSv/MBq, respectively. The critical organ based on the pig data was the gallbladder wall (20.4μSv/MBq) but the liver received a nearly identical equivalent dose (19.5μSv/MBq).
CONCLUSIONS: (1) When designing PET studies using [11C]erlotinib, the liver should be considered the critical organ. (2) In organs receiving the greatest equivalent dose, mouse data underestimated the dose in comparison to larger species. However, the effective dose of [11C]erlotinib to the whole body of a 73.7kg man was predicted with good consistency based on mice (3.14±0.05μSv/MBq) or the larger species (3.46±0.25μSv/MBq).
Copyright © 2017 Elsevier Inc. All rights reserved.

Entities:  

Keywords:  Dosimetry; Erlotinib; OLINDA; Radiation; TKI

Mesh:

Substances:

Year:  2017        PMID: 28126682      PMCID: PMC5360653          DOI: 10.1016/j.nucmedbio.2016.12.009

Source DB:  PubMed          Journal:  Nucl Med Biol        ISSN: 0969-8051            Impact factor:   2.408


  22 in total

1.  Physical models and dose factors for use in internal dose assessment.

Authors:  Michael G Stabin; Jeffry A Siegel
Journal:  Health Phys       Date:  2003-09       Impact factor: 1.316

2.  Genetic variation in liver mass, body mass, and liver:body mass in mice.

Authors:  L D Jones; M K Nielsen; R A Britton
Journal:  J Anim Sci       Date:  1992-10       Impact factor: 3.159

3.  The 2007 Recommendations of the International Commission on Radiological Protection. ICRP publication 103.

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Journal:  Ann ICRP       Date:  2007

4.  MIRD pamphlet No. 21: a generalized schema for radiopharmaceutical dosimetry--standardization of nomenclature.

Authors:  Wesley E Bolch; Keith F Eckerman; George Sgouros; Stephen R Thomas
Journal:  J Nucl Med       Date:  2009-03       Impact factor: 10.057

5.  The ECAT EXACT HR: performance of a new high resolution positron scanner.

Authors:  K Wienhard; M Dahlbom; L Eriksson; C Michel; T Bruckbauer; U Pietrzyk; W D Heiss
Journal:  J Comput Assist Tomogr       Date:  1994 Jan-Feb       Impact factor: 1.826

6.  OLINDA/EXM: the second-generation personal computer software for internal dose assessment in nuclear medicine.

Authors:  Michael G Stabin; Richard B Sparks; Eric Crowe
Journal:  J Nucl Med       Date:  2005-06       Impact factor: 10.057

Review 7.  First-generation epidermal growth factor receptor tyrosine kinase inhibitors in EGFR mutation: positive non-small cell lung cancer patients.

Authors:  Lecia V Sequist
Journal:  J Thorac Oncol       Date:  2008-06       Impact factor: 15.609

8.  Comparison of docetaxel- and vinca alkaloid-based chemotherapy in the first-line treatment of advanced non-small cell lung cancer: a meta-analysis of seven randomized clinical trials.

Authors:  Jean-Yves Douillard; Silvy Laporte; Frank Fossella; Vassilis Georgoulias; Jean-Louis Pujol; Kaoru Kubota; Alain Monnier; Shinzoh Kudoh; Jaime Ernesto Rubio; Michel Cucherat
Journal:  J Thorac Oncol       Date:  2007-10       Impact factor: 15.609

9.  Quantitative and Simplified Analysis of 11C-Erlotinib Studies.

Authors:  Maqsood Yaqub; Idris Bahce; Charlotte Voorhoeve; Robert C Schuit; Albert D Windhorst; Otto S Hoekstra; Ronald Boellaard; N Harry Hendrikse; Egbert F Smit; Adriaan A Lammertsma
Journal:  J Nucl Med       Date:  2016-02-04       Impact factor: 10.057

10.  Development of [(11)C]erlotinib positron emission tomography for in vivo evaluation of EGF receptor mutational status.

Authors:  Idris Bahce; Egbert F Smit; Mark Lubberink; Astrid A M van der Veldt; Maqsood Yaqub; Albert D Windhorst; Robert C Schuit; Erik Thunnissen; Daniëlle A M Heideman; Pieter E Postmus; Adriaan A Lammertsma; N Harry Hendrikse
Journal:  Clin Cancer Res       Date:  2012-11-07       Impact factor: 12.531

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  3 in total

Review 1.  The Development of Positron Emission Tomography Tracers for In Vivo Targeting the Kinase Domain of the Epidermal Growth Factor Receptor.

Authors:  Antonia Högnäsbacka; Alex J Poot; Danielle J Vugts; Guus A M S van Dongen; Albert D Windhorst
Journal:  Pharmaceuticals (Basel)       Date:  2022-04-05

2.  Development of a Fluorinated Analogue of Erlotinib for PET Imaging of EGFR Mutation-Positive NSCLC.

Authors:  Ofer Shamni; Hilbert Grievink; Batel Itamar; Eyal Mishani; Galith Abourbeh
Journal:  Mol Imaging Biol       Date:  2019-08       Impact factor: 3.488

3.  Human biodistribution and dosimetry of [11C]-UCB-J, a PET radiotracer for imaging synaptic density.

Authors:  Koen Van Laere; Michel Koole; Christopher Cawthorne; Paul Maguire; Joel Mercier; David Sciberras; Kim Serdons; Guy Bormans; Jan de Hoon
Journal:  EJNMMI Phys       Date:  2021-04-23
  3 in total

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