Chelating Systems for 99mTc/188Re in the Development of Radiolabeled Peptide Pharmaceuticals

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Chelating Systems for 99mTc/188Re in the Development of Radiolabeled Peptide Pharmaceuticals

Anti-Cancer Agents in Medicinal Chemistry, 12(5): 428-461.

Author(s): Cristina Bolzati, Davide Carta, Nicola Salvarese and Fiorenzo Refosco.

Affiliation: ICIS-CNR, Corso Stati Uniti, 4, 35127 Padova, Italy.


Currently, receptor based radiopharmaceuticals have received great attention in molecular imaging and radiotherapy of cancer, and provide a unique tool for target-specific delivery of radionuclides to pathological tissues. In this context, receptor binding peptides represent an attractive class of target vectors for Nuclear Medicine purposes. The rich chemistry of the group 7 elements elaborated in past years, has allowed the development of different procedures for the preparation of radiolabeled peptides in high yield. This, joint to the use of solid-phase peptide synthesis, has opened the possibility to explore new strategies for approaching the design of new class of radiolabeled receptor-targeted peptides, and to create new versatilities in targeting vehicle design e.g. in synthesis of metal-cyclized peptides or of multivalent targeting agents.

This review provides an overview on several aspects of the development of new 99mTc/188Re-peptide based target specific radiopharmaceuticals, in particular on the synthetic strategies employed for modifying molecular vectors, and the application of the different metal-cores and/or building block for preparing high specific activity agents.


Technetium, Rhenium, Peptide, Theragnostic, Maximum Tolerated Dose, RADIOLABELED PEPTIDES, Target-Molecules, Direct Labeling, octapeptide lanreotide, Phosphine.

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Article Details

Volume: 12
Issue Number: 5
First Page: 428
Last Page: 461
Page Count: 34
DOI: 10.2174/187152012800617821
Price: $58
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