open access

Vol 57, No 4 (2006)
Original paper
Submitted: 2013-02-15
Published online: 2006-07-07
Get Citation

The use of a new analogue DGlu-Octagastrin in scintigraphy of medullary thyroid carcinoma

Jerzy Kosowicz, Rafał Czepczyński, Katarzyna Ziemnicka, Maria Gryczyńska, Jerzy Sowiński
Endokrynol Pol 2006;57(4):427-430.

open access

Vol 57, No 4 (2006)
Original Paper
Submitted: 2013-02-15
Published online: 2006-07-07

Abstract

Introduction: Medullary thyroid carcinomas (MTC) reveal overexpression of several peptide receptors particularly of gastrin and cholecystokinin 2 (CCK2). Experimental studies of various CCK-2/gastrin analogues found that a C-terminal, 8-aminoacid peptide, DGlu-octagastrin, has optimal properties. Thus, the aim of our studies was to prepare 99mTc-labelled HYNIC-octagastrin, to evaluate its biologic tolerance in animals and introduce for scintigraphy in patients with MTC.
Material and methods: HYNIC-DGlu-octagastrin was from piCHEM (Graz, Austria), 99mTc generator from Amersham (Health), other reagents were purchased from Sigma. Labelling of the peptide was performed in phosphate buffer of pH 6.0 for 10 minutes at 100oC using EDDA and tricine as coligands.
Results: The labeling yields were high (above 95%); the specific activity amounted to 1200 to 1430 μCi/μg. Radiochemical purity on SepPak cartridge and ITLC ranged from 94 to 98%. No adverse effects were observed in mice after administration of 10 to 50 times greater doses that those used in patients. Clinical studies comprised 20 patients with MTC and high serum calcitonin. 99mTc-EDDA/HYNIC-DGlu-octagastrin, 500 to 700 MBq, was administered iv and whole body scintigraphy was performed using a double head gamma-camera (Varicam, Elscint) 2 and 4 hours later. Increased accumulation of the tracer in foci of MTC and its metastases was found in 8 patients.
Conclusions: Scintigraphy with a new gastrin analogue (DGlu-octagastrin) makes it possible to detect MTC with overexpression of CCK-2/gastrin receptors and to select patients for receptor-mediated radiopeptide therapy using DOTA-gastrin analogues labelled with 177Lu and 90Y.

Abstract

Introduction: Medullary thyroid carcinomas (MTC) reveal overexpression of several peptide receptors particularly of gastrin and cholecystokinin 2 (CCK2). Experimental studies of various CCK-2/gastrin analogues found that a C-terminal, 8-aminoacid peptide, DGlu-octagastrin, has optimal properties. Thus, the aim of our studies was to prepare 99mTc-labelled HYNIC-octagastrin, to evaluate its biologic tolerance in animals and introduce for scintigraphy in patients with MTC.
Material and methods: HYNIC-DGlu-octagastrin was from piCHEM (Graz, Austria), 99mTc generator from Amersham (Health), other reagents were purchased from Sigma. Labelling of the peptide was performed in phosphate buffer of pH 6.0 for 10 minutes at 100oC using EDDA and tricine as coligands.
Results: The labeling yields were high (above 95%); the specific activity amounted to 1200 to 1430 μCi/μg. Radiochemical purity on SepPak cartridge and ITLC ranged from 94 to 98%. No adverse effects were observed in mice after administration of 10 to 50 times greater doses that those used in patients. Clinical studies comprised 20 patients with MTC and high serum calcitonin. 99mTc-EDDA/HYNIC-DGlu-octagastrin, 500 to 700 MBq, was administered iv and whole body scintigraphy was performed using a double head gamma-camera (Varicam, Elscint) 2 and 4 hours later. Increased accumulation of the tracer in foci of MTC and its metastases was found in 8 patients.
Conclusions: Scintigraphy with a new gastrin analogue (DGlu-octagastrin) makes it possible to detect MTC with overexpression of CCK-2/gastrin receptors and to select patients for receptor-mediated radiopeptide therapy using DOTA-gastrin analogues labelled with 177Lu and 90Y.
Get Citation

Keywords

medullary carcinoma; gastrin analogues; radiopeptide scintigraphy; 99mTc-HYNIC-Octagastrin

About this article
Title

The use of a new analogue DGlu-Octagastrin in scintigraphy of medullary thyroid carcinoma

Journal

Endokrynologia Polska

Issue

Vol 57, No 4 (2006)

Article type

Original paper

Pages

427-430

Published online

2006-07-07

Page views

605

Article views/downloads

816

Bibliographic record

Endokrynol Pol 2006;57(4):427-430.

Keywords

medullary carcinoma
gastrin analogues
radiopeptide scintigraphy
99mTc-HYNIC-Octagastrin

Authors

Jerzy Kosowicz
Rafał Czepczyński
Katarzyna Ziemnicka
Maria Gryczyńska
Jerzy Sowiński

Regulations

Important: This website uses cookies. More >>

The cookies allow us to identify your computer and find out details about your last visit. They remembering whether you've visited the site before, so that you remain logged in - or to help us work out how many new website visitors we get each month. Most internet browsers accept cookies automatically, but you can change the settings of your browser to erase cookies or prevent automatic acceptance if you prefer.

Via MedicaWydawcą jest  VM Media Group sp. z o.o., Grupa Via Medica, ul. Świętokrzyska 73, 80–180 Gdańsk

tel.:+48 58 320 94 94, faks:+48 58 320 94 60, e-mail:  viamedica@viamedica.pl