(177) Lu-5-Fluorouracil a potential theranostic radiopharmaceutical: radiosynthesis, quality control, biodistribution, and scintigraphy

The aim of this study is to develop (177) Lu-5-Flourouracil as a potential cancer therapeutic radiopharmaceutical. 5-Flourouracil (5-FU) is widely accepted as an anticancer drug of broad spectrum fame. The labeling of 5-FU was carried out at different set of experimental conditions using high specif...

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Bibliographic Details
Published in:Journal of labelled compounds & radiopharmaceuticals 2016-08, Vol.59 (10), p.398-403
Main Authors: Rasheed, Rashid, Tariq, Saleha, Naqvi, Syed Ali Raza, Gillani, Syed Jawad Hussain, Rizvi, Faheem Askari, Sajid, Muhammad, Rasheed, Shahid
Format: Article
Language:English
Subjects:
Animals
Drug Stability
Fluorouracil - chemical synthesis
Fluorouracil - chemistry
Fluorouracil - pharmacokinetics
Fluorouracil - therapeutic use
Half-Life
Isotope Labeling
Lutetium - therapeutic use
Male
Quality Control
Rabbits
Radiochemistry
Radioisotopes
Radionuclide Imaging - methods
Radiopharmaceuticals - chemical synthesis
Radiopharmaceuticals - chemistry
Radiopharmaceuticals - pharmacokinetics
Radiopharmaceuticals - therapeutic use
Rats
Rats, Sprague-Dawley
Tissue Distribution
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Summary:The aim of this study is to develop (177) Lu-5-Flourouracil as a potential cancer therapeutic radiopharmaceutical. 5-Flourouracil (5-FU) is widely accepted as an anticancer drug of broad spectrum fame. The labeling of 5-FU was carried out at different set of experimental conditions using high specific activity of (177) LuCl3 . The optimum conditions for maximum radiochemical yield was set: 5-FU (5 mg), (177) LuCl3 (185 MBq), diethylenetriaminepentaacetic acid (10 µg), reaction volume (2 mL), pH (5.5), temperature (80°C), and reaction time (20 min). The radiochemical labeling was assessed with Whatman No. 2 paper, instant thin layer chromatographic, and radio-HPLC, which revealed >94% labeling results with sufficient stability up to 6 h. Serum stability study also showed (177) Lu-5-FU promising stability. Biodistribution study in normal rats and rabbits showed liver, stomach, kidney, and heart as area of increased tracer accumulation just after injection, which decreased to 1.4%, 0.4%, 0.2%, and 0.39% ID/g, respectively, after 72 h. Glomerular filtration rate and cytotoxicity study results of (177) Lu-5-FU showed it had no adverse effect on renal function and nontoxic to blood cells. The promising characteristics of (177) Lu-5-FU, that is, clever elimination from kidney and nontoxic nature toward blood cells make it the radiopharmaceutical for further testing in patients for therapeutic purposes.
ISSN:1099-1344
DOI:10.1002/jlcr.3423