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The potential of radiolabeled chemotherapeutics in tumor diagnosis: Preliminary investigations with 68 Ga‐gemcitabine
Author(s) -
Ghosh Subhajit,
Das Tapas,
D. Sarma Haladhar,
Dash Ashutosh
Publication year - 2018
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.21423
Subject(s) - gemcitabine , biodistribution , nucleoside analogue , chemistry , deoxycytidine , dota , positron emission tomography , nuclear medicine , nucleoside , pharmacology , cancer research , medicine , chemotherapy , chelation , in vitro , stereochemistry , biochemistry , organic chemistry
Preclinical Research & DevelopmentGemcitabine, a nucleoside analog, is a well‐known chemotherapeutic drug that is used either alone or with other agents to treat a wide variety of cancers. The aim of the present work was to evaluate the potential of 68 Ga‐labeled gemcitabine for its application in positron emission tomography (PET) imaging of tumorous lesions. Gemcitabine was coupled with p ‐NCS‐benzyl‐DOTA in order to facilitate radiolabeling with 68 Ga. The gemcitabine‐ p ‐NCS‐benzyl‐DOTA was radiolabeled with 68 Ga, obtained from a 68 Ge/ 68 Ga radionuclide generator. The radiolabeled product was characterized by high performance liquid chromatography (HPLC) and its tumor specificity was evaluated by biodistribution studies in Swiss mice bearing fibrosarcoma tumors. Preliminary bioevaluation study showed good tumor uptake within 1 hr post‐administration [2.5% Injected Activity (IA) per g of tumor] with rapid renal clearance (>90% IA) and a high tumor to muscle ratio. 68 Ga‐gemcitabine may have potential as a PET agent for tumor imaging.