title: (177) Lu-5-Fluorouracil a potential theranostic radiopharmaceutical: radiosynthesis, quality control, biodistribution, and scintigraphy.
abstract: 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.
authors.affiliation: Institute of Nuclear Oncology and Radiology (INOR), Abbottabad, Pakistan.
authors.forename: Rashid
authors.initials: R
authors.lastname: Rasheed
authors.affiliation: Department of Chemistry, Government College University, Faisalabad, Pakistan.
authors.forename: Saleha
authors.initials: S
authors.lastname: Tariq
authors.affiliation: Department of Chemistry, Government College University, Faisalabad, Pakistan.
authors.forename: Syed Ali Raza
authors.identifier: 0000-0002-2172-9066
authors.initials: SA
authors.lastname: Naqvi
authors.affiliation: Institute of Nuclear Oncology and Radiology (INOR), Abbottabad, Pakistan.
authors.forename: Syed Jawad Hussain
authors.initials: SJ
authors.lastname: Gillani
authors.affiliation: Department of Chemistry, Government College University, Faisalabad, Pakistan.
authors.forename: Faheem Askari
authors.initials: FA
authors.lastname: Rizvi
authors.affiliation: Pakistan Institute of Nuclear Science and Technology (PINSTECH), Nilore, Islamabad, Pakistan.
authors.forename: Muhammad
authors.initials: M
authors.lastname: Sajid
authors.affiliation: Institute of Nuclear Oncology and Radiology (INOR), Abbottabad, Pakistan.
authors.forename: Shahid
authors.initials: S
authors.lastname: Rasheed
mesh_terms: D000818:Animals; D004355:Drug Stability; D005472:Fluorouracil / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics* / Q000627:therapeutic use; D006207:Half-Life; D007553:Isotope Labeling; D008187:Lutetium / Q000627:therapeutic use*; D008297:Male; D011786:Quality Control; D011817:Rabbits; D011854:Radiochemistry; D011868:Radioisotopes; D011877:Radionuclide Imaging / Q000379:methods*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics* / Q000627:therapeutic use; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution
chemical_list: D011868:Radioisotopes; D019275:Radiopharmaceuticals; D008187:Lutetium; D005472:Fluorouracil
keywords: 177Lu-5-Flourouracil; GFR analysis; anticancer drugs; nuclear medicine; radiopharmaceuticals; tumor imaging