WO2004098652A1 - Radiolabelled thyroid stimulating hormone (tsh) and use thereof for the diagnosis and therapy of the differentiated thyroid tumors - Google Patents

Radiolabelled thyroid stimulating hormone (tsh) and use thereof for the diagnosis and therapy of the differentiated thyroid tumors Download PDF

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Publication number
WO2004098652A1
WO2004098652A1 PCT/IT2004/000234 IT2004000234W WO2004098652A1 WO 2004098652 A1 WO2004098652 A1 WO 2004098652A1 IT 2004000234 W IT2004000234 W IT 2004000234W WO 2004098652 A1 WO2004098652 A1 WO 2004098652A1
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WO
WIPO (PCT)
Prior art keywords
tsh
thyroid
diagnosis
therapy
tumors
Prior art date
Application number
PCT/IT2004/000234
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English (en)
French (fr)
Inventor
Alberto Signore
Marco Chianelli
Original Assignee
Universita' Degli Studi Di Roma La Sapienza
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Universita' Degli Studi Di Roma La Sapienza filed Critical Universita' Degli Studi Di Roma La Sapienza
Publication of WO2004098652A1 publication Critical patent/WO2004098652A1/en

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/08Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • A61K51/08Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/088Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins conjugates with carriers being peptides, polyamino acids or proteins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

Definitions

  • radiolabelled recombinant TSH retains the ability to bind its own receptor and accordingly it can be advantageously employed as scintigraphic tracer and as radiomedicament, respectively in the diagnosis and therapy of differentiated thyroid tumors and related metastases, bypassing disadvantages of currently available techniques in this field.
  • radiolabelled TSH intravenously injected, allows the imaging by scintigraphy with ⁇ room of the tumor and normal thyroid tissue, consequently to tissue build-up of the thyroid-stimulating hormone due to the binding with the receptor thereof.
  • the authors have developed a protocol for efficient preparation of the scintigraphic tracer according to the invention, which allows to maintain an elevated specific activity and stability of the protein even subsequently to the delicate labelling process with 99m TC.
  • the same labelling method can be used, with slight changes, for the proteinlabelling with Rhenium radioisotopes ( 186 Re and 188 Re) that, even emitting beta-type radiations, have chemical characteristic similar to those of 99m Tc.
  • the recombinant human TSH is already employed in humans in a non-radioactive form and its systemic administration is safe and does not produce side effects.
  • the labelling has been performed through enzymatic method (Burrin JM; Comparison between human 125 l-labelled TSH labelled with lactoperoxidase or chloramine-T advantages in the use of enzymically labelled antigen in a RIA for human TSH. Clinica Chimica Acta 1976; 70:153-159), because comparative studies of several iodination methods (Kermode JC, Thompson BD; lodination of TSH for receptor-binding studies with human thyroid membranes: effects of specific activity and method of iodination. J Endocr 1980; 84:439-447) have shown that the protein does not suffer damages, maintaining affinity for its receptor.
  • TPC-1 deriving from the papillary carcinoma of the thyroid, which expresses the receptor for TSH
  • ARO deriving from the anaplastic carcinoma of the thyroid, that does not express the TSH receptor.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
PCT/IT2004/000234 2003-05-05 2004-04-27 Radiolabelled thyroid stimulating hormone (tsh) and use thereof for the diagnosis and therapy of the differentiated thyroid tumors WO2004098652A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ITRM2003A000214 2003-05-05
IT000214A ITRM20030214A1 (it) 2003-05-05 2003-05-05 Ormone stimolante la tiroide (tsh) radiomarcato e suo uso

Publications (1)

Publication Number Publication Date
WO2004098652A1 true WO2004098652A1 (en) 2004-11-18

Family

ID=29765796

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IT2004/000234 WO2004098652A1 (en) 2003-05-05 2004-04-27 Radiolabelled thyroid stimulating hormone (tsh) and use thereof for the diagnosis and therapy of the differentiated thyroid tumors

Country Status (2)

Country Link
IT (1) ITRM20030214A1 (it)
WO (1) WO2004098652A1 (it)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022023419A1 (fr) * 2020-07-30 2022-02-03 Assistance Publique Des Hopitaux De Paris Procede et dispositif de traitement d'images en scintigraphie thyroïdienne

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990008528A1 (en) * 1989-01-11 1990-08-09 The United States Of America, Represented By The Secretary, United States Department Of Commerce Biologically active synthetic thyrotropin and cloned gene for producing same
WO1994009814A1 (en) * 1992-11-05 1994-05-11 B.R.A.H.M.S Diagnostica Gmbh Purified tsh preparation, process for its production and its use for the production of tsh tracers for tsh receptor assays and in tsh receptor assays
WO1999040116A1 (en) * 1998-02-03 1999-08-12 The University Of Melbourne Process for expression of thyroid stimulating hormone receptor

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990008528A1 (en) * 1989-01-11 1990-08-09 The United States Of America, Represented By The Secretary, United States Department Of Commerce Biologically active synthetic thyrotropin and cloned gene for producing same
WO1994009814A1 (en) * 1992-11-05 1994-05-11 B.R.A.H.M.S Diagnostica Gmbh Purified tsh preparation, process for its production and its use for the production of tsh tracers for tsh receptor assays and in tsh receptor assays
WO1999040116A1 (en) * 1998-02-03 1999-08-12 The University Of Melbourne Process for expression of thyroid stimulating hormone receptor

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
CORSETTI F ET AL: "Radioiodinated Recombinant Human TSH: A Novel Radiopharmaceutical for Thyroid Cancer Metastases Detection", CANCER BIOTHERAPY AND RADIOPHARMACEUTICALS 2004 UNITED STATES, vol. 19, no. 1, 2004, pages 57 - 63, XP009035972, ISSN: 1084-9785 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022023419A1 (fr) * 2020-07-30 2022-02-03 Assistance Publique Des Hopitaux De Paris Procede et dispositif de traitement d'images en scintigraphie thyroïdienne
FR3113163A1 (fr) * 2020-07-30 2022-02-04 Assistance Publique Des Hopitaux De Paris Procede et dispositif de traitement d’images en scintigraphie thyroïdienne

Also Published As

Publication number Publication date
ITRM20030214A1 (it) 2004-11-06
ITRM20030214A0 (it) 2003-05-05

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