The synthesis of fluorine-18 lomefloxacin and its preliminary use in human studies.
Lomefloxacin is a new fluorine-containing antibiotic that has recently been approved for general use. Fluorine-18 lomefloxacin has been prepared by fluoride exchange between fluorine-18 fluoride and lomefloxacin in DMSO. Both time and temperature of the reaction have been optimized and conditions developed for the isolation and purification of the labeled product in a form suitable for oral administration. The exchange reaction provides sufficient labeled material for human studies with pharmacologically relevant quantities of the drug. We have performed preliminary human studies with this compound using positron emission tomography to estimate the tissue distribution of the compound and show the distribution of the compound into the liver and lungs.
Tewson
T J
TJ
Positron Diagnostic and Research Center, University of Texas Health Science Center at Houston, USA.
Yang
D
D
Wong
G
G
Macy
D
D
DeJesus
O J
OJ
Nickles
R J
RJ
Perlman
S B
SB
Taylor
M
M
Frank
P
P
D000818:Animals; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D005462:Fluorine Radioisotopes / Q000737:chemistry*; D024841:Fluoroquinolones; D006801:Humans; D007553:Isotope Labeling / Q000379:methods; D008297:Male; D015363:Quinolones / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D011854:Radiochemistry; D013552:Swine; D014018:Tissue Distribution; D014915:Whole-Body Counting
D000890:Anti-Infective Agents; D005462:Fluorine Radioisotopes; D024841:Fluoroquinolones; D015363:Quinolones; C053091:lomefloxacin